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Tricyclic antidepressant
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Tricyclic antidepressant
Drug class
Chemical structure of the prototypical and first marketed tricyclic antidepressant imipramine. Notice its three rings.
Class identifiers
Chemical class
Tricyclic
External links
MeSH
D000929
In Wikidata
Tricyclic antidepressants (TCAs) are a class of medications that are used primarily as antidepressants. TCAs were discovered in the early 1950s and were marketed later in the decade.[1] They are named after their chemical structure, which contains three rings of atoms. Tetracyclic antidepressants (TeCAs), which contain four rings of atoms, are a closely related group of antidepressant compounds.
Although TCAs are sometimes prescribed for depressive disorders, they have been largely replaced in clinical use in most parts of the world by newer antidepressants such as selective serotonin reuptake inhibitors (SSRIs), serotonin–norepinephrine reuptake inhibitors (SNRIs) and norepinephrine reuptake inhibitors (NRIs). Adverse effects have been found to be of a similar level between TCAs and SSRIs.[2]
Contents
[hide]
1 Medical uses
1.1 Clinical depression
1.2 Attention-deficit hyperactivity disorder
1.3 Chronic pain
2 Side effects
2.1 Discontinuation
3 Overdose
4 Interactions
5 Pharmacology
5.1 Binding profiles
6 Chemistry
7 History
8 Society and culture
8.1 Recreational use
9 List of TCAs
10 References
11 Further reading
12 External links
Medical uses[edit]
The TCAs are used primarily in the clinical treatment of mood disorders such as major depressive disorder (MDD), dysthymia, and treatment-resistant variants. They are also used in the treatment of a number of other medical disorders, including anxiety disorders such as generalized anxiety disorder (GAD), social phobia (SP) also known as social anxiety disorder (SAD), obsessive-compulsive disorder (OCD), and panic disorder (PD), post-traumatic stress disorder (PTSD), body dysmorphic disorder (BDD), eating disorders like anorexia nervosa and bulimia nervosa, certain personality disorders such as borderline personality disorder (BPD), Neurological disorders such as attention-deficit hyperactivity disorder (ADHD),[3] Parkinson's disease[4] as well as chronic pain, neuralgia or neuropathic pain, and fibromyalgia, headache, or migraine, smoking cessation, tourette syndrome, trichotillomania, irritable bowel syndrome (IBS), interstitial cystitis (IC), nocturnal enuresis (NE),[5] narcolepsy, insomnia, pathological crying and/or laughing, chronic hiccups, ciguatera poisoning, and as an adjunct in schizophrenia.
Clinical depression[edit]
For many years the TCAs were the first choice for pharmacological treatment of clinical depression. Although they are still considered to be highly effective, they have been increasingly replaced by antidepressants with an improved safety and side effect profile, such as the SSRIs and other newer antidepressants such as the novel reversible MAOI moclobemide. However, tricyclic antidepressants are possibly more effective in treating melancholic depression than other antidepressant drug classes.[6] Newer antidepressants are thought to have fewer and less severe side effects and are also thought to be less likely to result in injury or death if used in a suicide attempt, as the doses required for clinical treatment and potentially lethal overdose (see therapeutic index) are far wider in comparison.
Nonetheless, the TCAs are still occasionally used for treatment-resistant depression that has failed to respond to therapy with newer antidepressants.[7] They are not considered addictive and are somewhat preferable to the monoamine oxidase inhibitors (MAOIs). The side effects of the TCAs usually come to prominence before the therapeutic benefits against depression and/or anxiety do, and for this reason, they may potentially be somewhat dangerous, as volition can be increased, possibly giving the patient a greater desire to attempt or commit suicide.[8]
Attention-deficit hyperactivity disorder[edit]
The TCAs were used in the past in the clinical treatment of ADHD,[9] though they are not typically used anymore, having been replaced by more effective agents with fewer side effects such as atomoxetine (Strattera, Tomoxetin) and stimulants like methylphenidate (Ritalin, Focalin, Concerta), and amphetamine (Adderall, Attentin, Dexedrine, Vyvanse). ADHD is thought to be caused by an insufficiency of dopamine and norepinephrine activity in the prefrontal cortex of the brain.[10] Most of the TCAs inhibit the reuptake of norepinephrine, though not dopamine, and as a result, they show some efficacy in remedying the disorder.[11] Notably, the TCAs are more effective in treating the behavioral aspects of ADHD than the cognitive deficits, as they help limit hyperactivity and impulsivity, but have little to no benefits on attention.[12]
Chronic pain[edit]
The TCAs show efficacy in the clinical treatment of a number of different types of chronic pain, notably neuralgia or neuropathic pain and fibromyalgia.[13][14] The precise mechanism of action in explanation of their analgesic efficacy is unclear, but it is thought that they indirectly modulate the opioid system in the brain downstream via serotonergic and noradrenergic neuromodulation, among other properties.[15][16][17] They are also effective in migraine prophylaxis, though not in the instant relief of an acute migraine attack. They may also be effective to prevent chronic tension headaches.
Side effects[edit]
Many side effects may be related to the antimuscarinic properties of the TCAs. Such side effects are relatively common and may include dry mouth, dry nose, blurry vision, lowered gastrointestinal motility or constipation, urinary retention, cognitive and/or memory impairment, and increased body temperature.
Other side effects may include drowsiness, anxiety, emotional blunting (apathy/anhedonia), confusion, restlessness, dizziness, akathisia, hypersensitivity, changes in appetite and weight, sweating, sexual dysfunction, muscle twitches, weakness, nausea and vomiting, hypotension, tachycardia, and rarely, irregular heart rhythms. Twitching, hallucinations, delirium and coma are also some of the toxic effects caused by overdose.[18] Rhabdomyolysis or muscle breakdown has been rarely reported with this class of drugs as well.[19]
Tolerance to these adverse effects of these drugs often develops if treatment is continued. Side effects may also be less troublesome if treatment is initiated with low doses and then gradually increased, although this may also delay the beneficial effects.
TCAs can behave like class 1A antiarrhythmics, as such, they can theoretically terminate ventricular fibrillation, decrease cardiac contractility and increase collateral blood circulation to ischemic heart muscle. Naturally, in overdose, they can be cardiotoxic, prolonging heart rhythms and increasing myocardial irritability.
New research has also revealed compelling evidence of a link between long-term use of anticholinergic medications like TCAs and dementia.[20] Although many studies have investigated this link, this was the first study to use a long-term approach (over seven years) to find that dementias associated with anticholinergics may not be reversible even years after drug use stops.[21] Anticholinergic drugs block the action of acetylcholine, which transmits messages in the nervous system. In the brain, acetylcholine is involved in learning and memory.
Discontinuation[edit]
Antidepressants in general may produce a withdrawal. However, since the term "withdrawal" has been linked to addiction to recreational drugs like opioids, the medical profession and pharmaceutical public relations prefer that a different term be used, hence "discontinuation syndrome."[22] Discontinuation symptoms can be managed by a gradual reduction in dosage over a period of weeks or months to minimise symptoms.[23] In tricyclics, discontinuation syndrome symptoms include anxiety, insomnia, headache, nausea, malaise, or motor disturbance.[24]
Overdose[edit]
Main article: Tricyclic antidepressant overdose
TCA overdose is a significant cause of fatal drug poisoning. The severe morbidity and mortality associated with these drugs is well documented due to their cardiovascular and neurological toxicity. Additionally, it is a serious problem in the pediatric population due to their inherent toxicity[25] and the availability of these in the home when prescribed for bed-wetting and depression. In the event of a known or suspected overdose, medical assistance should be sought immediately.
A number of treatments are effective in a TCA overdose.
An overdose on TCA is especially fatal as it is rapidly absorbed from the GI tract in the alkaline conditions of the small intestines. As a result, toxicity often becomes apparent in the first hour after an overdose. However, symptoms may take several hours to appear if a mixed overdose has caused delayed gastric emptying.
Many of the initial signs are those associated to the anticholinergic effects of TCAs such as dry mouth, blurred vision, urinary retention, constipation, dizziness, and emesis (or vomiting). Due to the location of norepinephrine receptors all over the body, many physical signs are also associated with a TCA overdose:[26]
Anticholinergic effects: altered mental status (e.g., agitation, confusion, lethargy, etc.), resting sinus tachycardia, dry mouth, mydriasis (pupil dilation), fever
Cardiac effects: hypertension (early and transient, should not be treated), tachycardia, orthostasis and hypotension, arrhythmias (including ventricular tachycardia and ventricular fibrillation, most serious consequence) / ECG changes (prolonged QRS, QT, and PR intervals)
CNS effects: syncope, seizure, coma, myoclonus, hyperreflexia
Pulmonary effects: hypoventilation resulting from CNS depression
Gastrointestinal effects: decreased or absent bowel sounds
Treatment of TCA overdose depends on severity of symptoms:
Initially, gastric decontamination of the patient is achieved by administering, either orally or via a nasogastric tube, activated charcoal pre-mixed with water, which adsorbs the drug in the gastrointestinal tract (most useful if given within 2 hours of drug ingestion). Other decontamination methods such as stomach pumps, gastric lavage, whole bowel irrigation, or (ipecac induced) emesis, are not recommended in TCA poisoning.
If there is metabolic acidosis, intravenous infusion of sodium bicarbonate is recommended by Toxbase.org, the UK and Ireland poisons advice database (TCAs are protein bound and become less bound in more acidic conditions, so by reversing the acidosis, protein binding increases and bioavailability thus decreases – the sodium load may also help to reverse the Na+ channel blocking effects of the TCA).
Interactions[edit]
The TCAs are highly metabolised by the cytochrome P450 hepatic enzymes. Drugs that inhibit cytochrome P450 (for example cimetidine, methylphenidate, fluoxetine, antipsychotics, and calcium channel blockers) may produce decreases in the TCAs' metabolism, leading to increases in their blood concentrations and accompanying toxicity.[27] Drugs that prolong the QT interval including antiarrhythmics such as quinidine, the antihistamines astemizole and terfenadine, and some antipsychotics may increase the chance of ventricular dysrhythmias. TCAs may enhance the response to alcohol and the effects of barbiturates and other CNS depressants. Side effects may also be enhanced by other drugs that have antimuscarinic properties.
Pharmacology[edit]
The majority of the TCAs act primarily as SNRIs by blocking the serotonin transporter (SERT) and the norepinephrine transporter (NET), respectively, which results in an elevation of the synaptic concentrations of these neurotransmitters, and therefore an enhancement of neurotransmission.[28][29] Notably, with the sole exception of amineptine, the TCAs have negligible affinity for the dopamine transporter (DAT), and therefore have no efficacy as dopamine reuptake inhibitors (DRIs).[28] Both serotonin and norepinephrine have been highly implicated in depression and anxiety, and it has been shown that facilitation of their activity has beneficial effects on these mental disorders.[30]
In addition to their reuptake inhibition, many TCAs also have high affinity as antagonists at the 5-HT2[31] (5-HT2A[32] and 5-HT2C[32]), 5-HT6,[33] 5-HT7,[34] α1-adrenergic,[31] and NMDA receptors,[35] and as agonists at the sigma receptors[36] (σ1[36] and σ2[37]), some of which may contribute to their therapeutic efficacy, as well as their side effects.[38] The TCAs also have varying but typically high affinity for antagonising the H1[31] and H2[39][40] histamine receptors, as well as the muscarinic acetylcholine receptors.[31] As a result, they also act as potent antihistamines and anticholinergics. These properties are often beneficial in antidepressants, especially with comorbid anxiety, as it provides a sedative effect.[41]
Most, if not all, of the TCAs also potently inhibit sodium channels and L-type calcium channels, and therefore act as sodium channel blockers and calcium channel blockers, respectively.[42][43] The former property is responsible for the high mortality rate upon overdose seen with the TCAs via cardiotoxicity.[44] It may also be involved in their efficacy as analgesics, however.[45]
Binding profiles[edit]
See also: Tetracyclic antidepressant § Binding profiles
The binding profiles of various TCAs and some metabolites in terms of their affinities (Ki, nM) for various receptors and transporters are as follows:[46]
Compound
SERT
NET
DAT
5-HT1A
5-HT2A
5-HT2C
5-HT6
5-HT7
α1
α2
D2
H1
H2
mACh
σ1
σ2
Amineptine >100,000 10,000 1,000–1,400 >100,000 74,000 ND ND ND >100,000 >100,000 >100,000 ≥13,000 ND >100,000 ND ND
Amitriptyline 2.8–4.3 19–35 3,250 ≥450 18–23 4.0 65–141 93–123 4.4–24 114–690 196–1,460 0.5–1.1 66 9.6 300 ND
Amoxapine 58 16 4,310 ND 0.5 2.0 6.0–50 41 50 2,600 3.6–160 7.9–25 ND 1,000 ND ND
Butriptyline ≥1,360 5,100 3,940 7,000 380 ND ND ND 570 4,800 ND 1.1 ND 35 ND ND
Clomipramine 0.14–0.28 38–54 ≥2,190 ≥7,000 27–36 65 54 127 3.2–38 ≥535 78–190 13–31 209 37 546 ND
Desipramine 18–163 0.63–3.5 3,190 ≥6,400 115–350 244–748 ND >1,000 23–130 ≥1,379 3,400 60–110 1,550 66–198 ≥1,990 ≥1,610
Dibenzepin ND ND >10,000 >10,000 ≥1,500 ND ND ND >10,000 >10,000 >10,000 23 1,950 1,750 ND ND
Dosulepin 8.6–78 46–70 5,310 4,000 152 ND ND ND 419 2,400 ND 3.6–4.0 ND 25–26 ND ND
Doxepin 68–210 13–58 ≥4,600 276 11–27 8.8–200 136 ND 24 28–1,270 360 0.09–1.23 174 23–80 ND ND
Imipramine 1.3–1.4 20–37 8,500 ≥5,800 80–150 120 190–209 >1,000 32 3,100 620–726 7.6–37 550 46 332–520 327–2,100
Iprindole ≥1,620 1,260 6,530 2,800 217–280 206 ND ND 2,300 8,600 6,300 100–130 200–8,300 2,100 >10,000 ND
Lofepramine 70 5.4 >10,000 4,600 200 ND ND ND 100 2,700 2,000 245–360 4,270 67 2,520 ND
Maprotiline 5,800 11–12 1,000 ND 51 122 ND 50 90 9,400 350–665 0.79–2.0 776 570 ND ND
Norclomipramine 40 0.45 2,100 19,000 130 ND ND ND 190 1,800 1,200 450 ND 92 ND ND
Northiaden 192 25 2,539 2,623 141 ND ND ND 950 ND ND 25 ND 110 ND ND
Nortriptyline 15–18 1.8–4.4 1,140 294 5.0–41 8.5 148 ND 55 2,030 2,570 3.0–15 646 37 2,000 ND
Opipramol ≥2,200 ≥700 ≥3,000 >10,000 120 ND ND ND 200 6,100 120–300 6.0 4,470 3,300 0.2–50 110
Protriptyline 19.6 1.41 2,100 3,800 70 ND ND ND 130 6,600 2,300 7.2–25 398 25 ND ND
Tianeptine >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000
Trimipramine 149–2,110 ≥2,450 ≥3,780 8,000 32 537 ND ND 24 680 143–210 0.27–1.5 41 58 ND ND
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. For assay species and references, see the individual drug articles. Most but not all values are for human proteins.
With the exception of the sigma receptors, the TCAs act as antagonists or inverse agonists of the receptors and as inhibitors of the transporters. Tianeptine is included in this list due to it technically being a TCA, but with a vastly different pharmacology.
Therapeutic levels of TCAs are generally in the range of about 100 to 300 ng/mL, or 350 to 1,100 nM.[47] Plasma protein binding is generally 90% or greater.[47]
Chemistry[edit]
There are two major groups of TCAs in terms of chemical structure, which most, but not all, TCAs fall into.[48][49][50] The groupings are based on the tricyclic ring system.[48][49][50] They are the dibenzazepines (imipramine, desipramine, clomipramine, trimipramine, lofepramine) and the dibenzocycloheptadienes (amitriptyline, nortriptyline, protriptyline, butriptyline).[48][49] Minor TCA groups based on ring system include the dibenzoxepins (doxepin), the dibenzothiepines (dosulepin), and the dibenzoxazepines (amoxapine).[48][49] In addition to classification based on the ring system, TCAs can also be usefully grouped based on the number of substitutions of the side chain amine.[50][51] These groups include the tertiary amines (imipramine, clomipramine, trimipramine, amitriptyline, butriptyline, doxepin, dosulepin) and the secondary amines (desipramine, nortriptyline, protriptyline).[50][51] Lofepramine is technically a tertiary amine, but acts largely as a prodrug of desipramine, a secondary amine, and hence is more similar in profile to the secondary amines than to the tertiary amines.[51] Amoxapine does not have the TCA side chain and hence is neither a tertiary nor secondary amine, although it is often grouped with the secondary amines due to sharing more in common with them.[52]
History[edit]
The TCAs were developed amid the "explosive birth" of psychopharmacology in the early 1950s. The story begins with the synthesis of chlorpromazine in December 1950 by Rhône-Poulenc's chief chemist, Paul Charpentier, from synthetic antihistamines developed by Rhône-Poulenc in the 1940s.[53] Its psychiatric effects were first noticed at a hospital in Paris in 1952. The first widely used psychiatric drug, by 1955 it was already generating significant revenue as an antipsychotic.[54] Research chemists quickly began to explore other derivatives of chlorpromazine.
The first TCA reported for the treatment of depression was imipramine, a dibenzazepine analogue of chlorpromazine code-named G22355. It was not originally targeted for the treatment of depression. The drug's tendency to induce manic effects was "later described as 'in some patients, quite disastrous'". The paradoxical observation of a sedative inducing mania led to testing with depressed patients. The first trial of imipramine took place in 1955 and the first report of antidepressant effects was published by Swiss psychiatrist Roland Kuhn in 1957.[53] Some testing of Geigy’s imipramine, then known as Tofranil, took place at the Münsterlingen Hospital near Konstanz.[54] Geigy later became Ciba-Geigy and eventually Novartis.
Dibenzazepine derivatives are described in U.S. patent 3,074,931 issued 1963-01-22 by assignment to Smith Kline & French Laboratories. The compounds described share a tricyclic backbone different from the backbone of the TCA amitriptyline.
Merck introduced the second member of the TCA family, amitriptyline (Elavil), in 1961.[54] This compound has a different three-ring structure than imipramine.
Society and culture[edit]
Recreational use[edit]
A very small number of cases involving non-medical use of antidepressants have been reported over the past 30 years.[55] According to the US government classification of psychiatric medications, TCAs are "non-abusable"[56] and generally have low abuse potential.[57] Nonetheless due to their atypical MOA, amineptine and tianeptine (dopamine reuptake inhibition and μ-opioid receptor agonism, respectively) are the two TCAs with the highest addiction and abuse potential. Several cases of the misuse[58] of amitriptyline alone[59][60] or together with methadone[58][61] or in other drug dependent patients[62][63] and of dosulepin with alcohol[64] or in methadone patients[65] have been reported.
List of TCAs[edit]
Those that preferentially inhibit the reuptake of serotonin (by at least 10-fold over norepinephrine) include:
Butriptyline† (Evadyne) (relatively weak serotonin reuptake inhibitor)
Clomipramine (Anafranil)
Imipramine (Tofranil, Janimine, Praminil)
Trimipramine (Surmontil) (relatively weak serotonin reuptake inhibitor)
Those that preferentially inhibit the reuptake of norepinephrine (by at least 10-fold over serotonin) include:
Desipramine (Norpramin, Pertofrane)
Dibenzepin‡ (Noveril, Victoril)
Lofepramine§ (Lomont, Gamanil)
Maprotiline (Ludiomil) – can be classed with the TCAs though more frequently classed with the TeCAs
Nortriptyline (Pamelor, Aventyl, Norpress)
Protriptyline (Vivactil)
Whereas either fairly balanced reuptake inhibitors of serotonin and norepinephrine or unspecified inhibitors include:
Amitriptyline (Elavil, Endep)
Amitriptylinoxide (Amioxid, Ambivalon, Equilibrin)
Amoxapine (Asendin) – can be classed with the TeCAs but more frequently classed with the TCAs
Demexiptiline† (Deparon, Tinoran)
Dimetacrine† (Istonil, Istonyl, Miroistonil)
Dosulepin§ (Prothiaden)
Doxepin (Adapin, Sinequan)
Fluacizine† (Phtorazisin)
Imipraminoxide† (Imiprex, Elepsin)
Melitracen§ (Deanxit, Dixeran, Melixeran, Trausabun)
Metapramine† (Timaxel)
Nitroxazepine‡ (Sintamil)
Noxiptiline‡ (Agedal, Elronon, Nogedal)
Pipofezine‡ (Azafen/Azaphen)
Propizepine† (Depressin, Vagran)
Quinupramine† (Kevopril, Kinupril, Adeprim, Quinuprine)
And the following are TCAs that act via main mechanisms other than serotonin or norepinephrine reuptake inhibition:
Amineptine‡ (Survector, Maneon, Directim) – norepinephrine–dopamine reuptake inhibitor
Iprindole† (Prondol, Galatur, Tetran) – 5-HT2 receptor antagonist
Opipramol‡ (Insidon, Pramolan, Ensidon, Oprimol) – σ receptor agonist
Tianeptine‡ (Stablon, Coaxil, Tatinol) – atypical μ-opioid receptor agonist
Legend:
† indicates products that have been withdrawn from the market worldwide.
‡ indicates products that are not available in any country in which English is an official language.
§ indicates products that are not available in the United States, but are available in other English-speaking countries such as Australia, Canada, United Kingdom, etc.
Bolded names indicates products that are available in at least three countries in which English is an official language.
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Jump up ^ Uher R.; Farmer A.; Henigsberg N.; Rietschel M.; Mors O.; Maier W.; Aitchison K. J. (2009). "Adverse reactions to antidepressants". The British Journal of Psychiatry. 195 (3): 202–210. doi:10.1192/bjp.bp.108.061960. PMID 19721108.
Jump up ^ Pancrazio JJ, Kamatchi GL, Roscoe AK, Lynch C (January 1998). "Inhibition of neuronal Na+ channels by antidepressant drugs". The Journal of Pharmacology and Experimental Therapeutics. 284 (1): 208–14. PMID 9435180.
Jump up ^ Zahradník I, Minarovic I, Zahradníková A (March 2008). "Inhibition of the cardiac L-type calcium channel current by antidepressant drugs". The Journal of Pharmacology and Experimental Therapeutics. 324 (3): 977–84. doi:10.1124/jpet.107.132456. PMID 18048694.
Jump up ^ Harrigan RA, Brady WJ (July 1999). "ECG abnormalities in tricyclic antidepressant ingestion". The American Journal of Emergency Medicine. 17 (4): 387–93. doi:10.1016/S0735-6757(99)90094-3. PMID 10452441.
Jump up ^ Brian E. Cairns (1 September 2009). Peripheral Receptor Targets for Analgesia: Novel Approaches to Pain Management. John Wiley & Sons. pp. 66–68. ISBN 978-0-470-52221-9.
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Further reading[edit]
Gillman PK (2007). "Tricyclic antidepressant pharmacology and therapeutic drug interactions updated". Br. J. Pharmacol. 151 (6): 737–48. doi:10.1038/sj.bjp.0707253. PMC 2014120  . PMID 17471183.
External links[edit]
Tricyclic Antidepressive Agents at the US National Library of Medicine Medical Subject Headings (MeSH)
[show]
v
t
e
Antidepressants (N06A)
[hide]
Specific reuptake inhibitors and/or receptor modulators
SSRIs
Citalopram
Escitalopram
Fluoxetine#
Fluvoxamine
Indalpine‡
Paroxetine
Sertraline
Zimelidine‡
SNRIs
Desvenlafaxine
Duloxetine
Levomilnacipran
Milnacipran
Tofenacin
Venlafaxine
NRIs
Atomoxetine
Reboxetine
Viloxazine
NDRIs
Amineptine‡
Bupropion
Nomifensine‡
NaSSAs
Mianserin
Mirtazapine
Setiptiline
SARIs
Etoperidone
Nefazodone
Trazodone
SMS
Vilazodone
Vortioxetine
Others
Agomelatine
Amisulpride
Esketamine†
Etryptamine‡
Indeloxazine
flupentixol
Ketamine†
Medifoxamine‡
Metryptamine‡
Oxaflozane‡
Pivagabine‡
Tandospirone
Teniloxazine
Tianeptine
[hide]
Tricyclic and tetracyclic antidepressants
TCAs
Amineptine‡
Amitriptyline#
Amitriptylinoxide
Butriptyline‡
Clomipramine#
Demexiptiline‡
Desipramine
Dibenzepin
Dimetacrine‡
Dosulepin
Doxepin
Imipramine
Imipraminoxide‡
Iprindole‡
Lofepramine
Melitracen
Metapramine‡
Nitroxazepine
Nortriptyline
Noxiptiline
Opipramol
Pipofezine
Propizepine‡
Protriptyline
Quinupramine‡
Tianeptine
Trimipramine
TeCAs
Amoxapine
Maprotiline
Mianserin
Mirtazapine
Setiptiline
Others
Tiazesim
[hide]
Monoamine oxidase inhibitors
Non-selective
Irreversible: Benmoxin‡
Iproclozide‡
Iproniazid‡
Isocarboxazid
Isoniazid#
Linezolid#
Mebanazine‡
Nialamide‡
Octamoxin‡
Phenelzine
Pheniprazine‡
Phenoxypropazine‡
Pivhydrazine‡
Safrazine‡
Tedizolid
Tranylcypromine
Reversible: Caroxazone‡
Mixed: Bifemelane
MAOA-selective
Reversible: Eprobemide
Metralindole
Minaprine‡
Moclobemide
Pirlindole
Tetrindole
Toloxatone
MAOB-selective
Irreversible: Selegiline
[hide]
Adjunctive therapies
Atypical antipsychotics (aripiprazole, brexpiprazole, lurasidone, olanzapine, quetiapine, risperidone)
Buspirone
Lithium (lithium carbonate, lithium citrate)
Thyroid hormones (triiodothyronine (T3), levothyroxine (T4))
[hide]
Miscellaneous
Ademetionine (SAMe)
Hypericum perforatum (St. John's Wort)
Oxitriptan (5-HTP)
Rubidium chloride (RbCl)
Tryptophan
#WHO-EM
‡Withdrawn from market
Clinical trials:
†Phase III
§Never to phase III
[show]
Pharmacodynamics
[show]
v
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Adrenergic receptor modulators
α1
Agonists: 6-FNE
Amidephrine
Anisodine
Buspirone
Cirazoline
Corbadrine
Desglymidodrine
Dexisometheptene
Dipivefrine
Dopamine
Droxidopa (L-DOPS)
Ephedrine
Epinephrine
Etilefrine
Etilevodopa
Ethylnorepinephrine
Indanidine
Isometheptene
L-DOPA (levodopa)
L-Phenylalanine
L-Tyrosine
Melevodopa
Metaraminol
Methoxamine
Methyldopa
Midodrine
Naphazoline
Norepinephrine
Octopamine (drug)
Oxymetazoline
Phenylephrine
Phenylpropanolamine
Pseudoephedrine
Synephrine
Tetryzoline
Tiamenidine
XP21279
Xylometazoline
Antagonists: Abanoquil
Adimolol
Ajmalicine
Alfuzosin
Amosulalol
Anisodamine
Arotinolol
Atiprosin
Atypical antipsychotics (e.g., brexpiprazole, clozapine, olanzapine, quetiapine, risperidone)
Benoxathian
Buflomedil
Bunazosin
Carvedilol
Corynanthine
Dapiprazole
Domesticine
Doxazosin
Ergolines (e.g., ergotamine, dihydroergotamine, lisuride, terguride)
Etoperidone
Eugenodilol
Fenspiride
Hydroxyzine
Indoramin
Ketanserin
L-765,314
Labetalol
mCPP
Mepiprazole
Metazosin
Monatepil
Moxisylyte
Naftopidil
Nantenine
Neldazosin
Niaprazine
Nicergoline
Niguldipine
Pardoprunox
Pelanserin
Perlapine
Phendioxan
Phenoxybenzamine
Phentolamine
Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione)
Piperoxan
Prazosin
Quinazosin
Quinidine
Ritanserin
Silodosin
Spiperone
Talipexole
Tamsulosin
Terazosin
Tiodazosin
Tolazoline
Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin)
Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, imipramine, trimipramine)
Trimazosin
Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine)
Urapidil
WB-4101
Zolertine
α2
Agonists: (R)-3-Nitrobiphenyline
4-NEMD
6-FNE
Amitraz
Apraclonidine
Brimonidine
Cannabivarin
Clonidine
Corbadrine
Detomidine
Dexmedetomidine
Dihydroergotamine
Dipivefrine
Dopamine
Droxidopa (L-DOPS)
Etilevodopa
Ephedrine
Ergotamine
Epinephrine
Etilefrine
Ethylnorepinephrine
Guanabenz
Guanfacine
Guanoxabenz
L-DOPA (levodopa)
L-Phenylalanine
L-Tyrosine
Lofexidine
Medetomidine
Melevodopa
Methyldopa
Mivazerol
Naphazoline
Norepinephrine
Oxymetazoline
Phenylpropanolamine
Piperoxan
Pseudoephedrine
Rezatomidine
Rilmenidine
Romifidine
Talipexole
Tasipimidine
Tetrahydrozoline
Tiamenidine
Tizanidine
Tolonidine
Urapidil
Vatinoxan
XP21279
Xylazine
Xylometazoline
Antagonists: 1-PP
Adimolol
Amesergide
Aptazapine
Atipamezole
Atypical antipsychotics (e.g., asenapine, brexpiprazole, clozapine, lurasidone, paliperidone, quetiapine, risperidone, zotepine)
Azapirones (e.g., buspirone, gepirone, ipsapirone, tandospirone)
BRL-44408
Buflomedil
Cirazoline
Efaroxan
Esmirtazapine
Fenmetozole
Fluparoxan
Idazoxan
mCPP
Mianserin
Mirtazapine
NAN-190
Olanzapine
Pardoprunox
Phentolamine
Phenoxybenzamine
Piperoxan
Piribedil
Rauwolscine
Rotigotine
SB-269970
Setiptiline
Spiroxatrine
Sunepitron
Tolazoline
Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine)
Yohimbine
β
Agonists: Abediterol
Alifedrine
Amibegron
Arbutamine
Arformoterol
Arotinolol
BAAM
Bambuterol
Befunolol
Bitolterol
Broxaterol
Buphenine
Carbuterol
Carmoterol
Cimaterol
Clenbuterol
Colterol
Corbadrine
Denopamine
Dipivefrine
Dobutamine
Dopamine
Dopexamine
Droxidopa (L-DOPS)
Ephedrine
Epinephrine
Etafedrine
Etilefrine
Etilevodopa
Ethylnorepinephrine
Fenoterol
Formoterol
Hexoprenaline
Higenamine
Indacaterol
Isoetarine
Isoprenaline
Isoxsuprine
L-DOPA (levodopa)
L-Phenylalanine
L-Tyrosine
Levosalbutamol
Mabuterol
Melevodopa
Methoxyphenamine
Methyldopa
Mirabegron
Norepinephrine
Orciprenaline
Oxyfedrine
PF-610355
Phenylpropanolamine
Pirbuterol
Prenalterol
Ractopamine
Procaterol
Pseudoephedrine
Reproterol
Rimiterol
Ritodrine
Salbutamol
Salmeterol
Solabegron
Terbutaline
Tretoquinol
Tulobuterol
Vilanterol
Xamoterol
XP21279
Zilpaterol
Zinterol
Antagonists: Acebutolol
Adaprolol
Adimolol
Afurolol
Alprenolol
Alprenoxime
Amosulalol
Ancarolol
Arnolol
Arotinolol
Atenolol
Befunolol
Betaxolol
Bevantolol
Bisoprolol
Bopindolol
Bornaprolol
Brefonalol
Bucindolol
Bucumolol
Bufetolol
Bufuralol
Bunitrolol
Bunolol
Bupranolol
Butaxamine
Butidrine
Butofilolol
Capsinolol
Carazolol
Carpindolol
Carteolol
Carvedilol
Celiprolol
Cetamolol
Cicloprolol
Cinamolol
Cloranolol
Cyanopindolol
Dalbraminol
Dexpropranolol
Diacetolol
Dichloroisoprenaline
Dihydroalprenolol
Dilevalol
Diprafenone
Draquinolol
Ecastolol
Epanolol
Ericolol
Ersentilide
Esatenolol
Esprolol
Eugenodilol
Exaprolol
Falintolol
Flestolol
Flusoxolol
Hydroxycarteolol
Hydroxytertatolol
ICI-118,551
Idropranolol
Indenolol
Indopanolol
Iodocyanopindolol
Iprocrolol
Isoxaprolol
Isamoltane
Labetalol
Landiolol
Levobetaxolol
Levobunolol
Levomoprolol
Medroxalol
Mepindolol
Metipranolol
Metoprolol
Moprolol
Nadolol
Nadoxolol
Nebivolol
Nifenalol
Nipradilol
Oxprenolol
Pacrinolol
Pafenolol
Pamatolol
Pargolol
Penbutolol
Pindolol
Practolol
Primidolol
Procinolol
Pronethalol
Propafenone
Propranolol
Ridazolol
Ronactolol
Soquinolol
Sotalol
Spirendolol
SR 59230A
Sulfinalol
Talinolol
Tazolol
Tertatolol
Tienoxolol
Tilisolol
Timolol
Tiprenolol
Tolamolol
Toliprolol
Xibenolol
Xipranolol
[show]
v
t
e
Dopamine receptor modulators
D1-like
Agonists
Benzazepines: 6-Br-APB
Fenoldopam
SKF-38,393
SKF-77,434
SKF-81,297
SKF-82,958
SKF-83,959
Trepipam
Zelandopam
Ergolines: Cabergoline
CY-208,243
Dihydroergocryptine
LEK-8829
Lisuride
Pergolide
Terguride
Dihydrexidine derivatives: A-77636
A-86929
Adrogolide (ABT-431, DAS-431)
Dihydrexidine
Dinapsoline
Dinoxyline
Doxanthrine
Phenethylamines: BCO-001
Deoxyepinephrine (N-methyldopamine, epinine)
Dopexamine
Etilevodopa
Ibopamine
L-DOPA (levodopa)
Melevodopa
L-Phenylalanine
L-Tyrosine
XP21279
Others: A-68930
Apomorphine
Isocorypalmine
Nuciferine
PF-6649751
PF 6669571
Propylnorapomorphine
Rotigotine
SKF-89,145
SKF-89,626
Stepholidine
Tetrahydropalmatine
Antagonists
Typical antipsychotics: Butaclamol
Chlorpromazine
Chlorprothixene
Flupentixol (flupenthixol) (+melitracen)
Fluphenazine
Loxapine
Perphenazine (+amitriptyline)
Pifluthixol
Thioridazine
Thiothixene
Trifluoperazine (+tranylcypromine)
Zuclopenthixol
Atypical antipsychotics: Asenapine
Clorotepine
Clotiapine
Clozapine
DHA-clozapine
Fluperlapine
Iloperidone
Norclozapine
Norquetiapine
Olanzapine (++fluoxetine)
Paliperidone
Quetiapine
Risperidone
Tefludazine
Zicronapine
Ziprasidone
Zotepine
Others: Berupipam
Ecopipam
EEDQ
Metitepine (methiothepin)
Odapipam
Perlapine
SCH-23390
D2-like
Agonists
Adamantanes: Amantadine
Memantine
Rimantadine
Aminotetralins: 5-OH-DPAT
7-OH-DPAT
8-OH-PBZI
Rotigotine
UH-232
Ergolines: Bromocriptine
Cabergoline
Dihydroergocryptine
Epicriptine
Ergocornine
Lisuride
LSD
Pergolide
Terguride
Dihydrexidine derivatives: 2-OH-NPA
Ciladopa
Dihydrexidine
Dinoxyline
N,N-Propyldihydrexidine
Phenethylamines: Deoxyepinephrine (N-methyldopamine, epinine)
Dopexamine
Etilevodopa
Ibopamine
L-DOPA (levodopa)
L-Phenylalanine
L-Tyrosine
Melevodopa
XP21279
Atypical antipsychotics: Alentemol (U-66444B)
Aripiprazole (+sertraline)
Aripiprazole lauroxil
Bifeprunox
Brexpiprazole
Cariprazine
F-15063
Lumateperone
Norclozapine
RP-5063
Others: 3-PPP
A-412997
ABT-670
ABT-724
Adrafinil
Aplindore
Apomorphine
Arketamine
Armodafinil
BP-897
Captodiame
CP-226,269
Dizocilpine
Esketamine
Flibanserin
GSK-789,472
Ketamine
Mesulergine
Modafinil
OSU-6162
Pardoprunox
PD-128,907
PD-168,077
PF-219,061
PF-592,379
Phencyclidine
Piribedil
Pramipexole
Preclamol
Propylnorapomorphine
Pukateine
Quinagolide
Quinelorane
Quinpirole
RDS-127
Ro10-5824
Ropinirole
Roxindole
Salvinorin A
SKF-83,959
Sumanirole
Talipexole
Umespirone
WAY-100,635
Antagonists
Typical antipsychotics: Acepromazine
Acetophenazine
Azaperone
Benperidol
Bromperidol
Butaclamol
Butaperazine
Chloracizine
Chlorproethazine
Chlorpromazine
Chlorprothixene
Ciclindole
Clopenthixol
Clothixamide
Clopimozide
Droperidol
Fluacizine
Fluanisone
Flucindole
Fluotracen
Flupentixol (flupenthixol) (+melitracen)
Fluphenazine
Fluprothixene
Fluspirilene
Haloperidol
Homopipramol
Lenperone
Levomepromazine (methotrimeprazine)
Levosulpiride
Loxapine
Mesoridazine
Moperone
Naranol
Nemonapride
Penfluridol
Perathiepin
Perazine
Pericyazine (periciazine)
Perphenazine (+amitriptyline)
Piflutixol (pifluthixol)
Pimozide
Pipamperone
Preclamol
Prochlorperazine
Promazine
Prothipendyl
Spiperone (spiroperidol)
Sulforidazine
Sulpiride
Sultopride
Teflutixol
Thiopropazate
Thioproperazine
Thioridazine
Thiothixene
Timiperone
Trifluoperazine (+tranylcypromine)
Triflupromazine
Trifluperidol
Zetidoline
Zuclopenthixol
Atypical antipsychotics: Amisulpride
Asenapine
BL-1020
Blonanserin
Carpipramine
Cinuperone
Clocapramine
Clorotepine
Clotiapine (clothiapine)
Clozapine
Cyamemazine
DHA-clozapine
Dixyrazine
Elopiprazole
Flumezapine
Fluperlapine
Gevotroline
Iloperidone
Lurasidone
Mazapertine
Melperone
Molindone
Mosapramine
Ocaperidone
Olanzapine (+fluoxetine)
Paliperidone
Perospirone
Piperacetazine
Pipotiazine
Piquindone
Quetiapine
Remoxipride
Risperidone
Sertindole
Tefludazine
Tenilapine
Tiospirone
Veralipride
Zicronapine
Ziprasidone
Zotepine
Antiemetics/gastroprokinetics/sedatives: Aceprometazine
AS-8112
Alimemazine
Alizapride
Benzquinamide
Bromopride
Clebopride
Domperidone
Eticlopride
Hydroxyzine
Itopride
Metoclopramide
Metopimazine
Promethazine
Thiethylperazine
Trimethobenzamide
Antidepressants: Amoxapine
Nefazodone
Opipramol
Propiomazine
Trimipramine
Others: 3-PPP
Alpiropride
Azapride
Buspirone
Desmethoxyfallypride
EEDQ
F-15063
Fallypride
Fananserin
Fenfluramine
GSK-789,472
Iodobenzamide
Isocorypalmine
L-741,626
L-745,870
Levofenfluramine
LEK-8829
Metergoline
Metitepine (methiothepin)
N-Methylspiperone
Nafadotride
Nuciferine
PNU-99,194
Pridopidine
Raclopride
Sarizotan
SB-277,011-A
Seridopidine
Sonepiprazole
Spiroxatrine
Stepholidine
SV-293
Tetrahydropalmatine
Tiapride
UH-232
Yohimbine
See also: Receptor/signaling modulators
Adrenergics
Serotonergics
Monoamine reuptake inhibitors
Monoamine releasing agents
Monoamine metabolism modulators
Monoamine neurotoxins
[show]
v
t
e
Histamine receptor modulators
H1
Agonists: 2-Pyridylethylamine
Betahistine
Histamine
HTMT
L-Histidine
UR-AK49
Antagonists: First-generation: 4-Methyldiphenhydramine
Alimemazine
Antazoline
Azatadine
Bamipine
Benzatropine (benztropine)
Bepotastine
Bromazine
Brompheniramine
Buclizine
Captodiame
Carbinoxamine
Chlorcyclizine
Chloropyramine
Chlorothen
Chlorphenamine
Chlorphenoxamine
Cinnarizine
Clemastine
Clobenzepam
Clocinizine
Cloperastine
Cyclizine
Cyproheptadine
Dacemazine
Decloxizine
Deptropine
Dexbrompheniramine
Dexchlorpheniramine
Dimenhydrinate
Dimetindene
Diphenhydramine
Diphenylpyraline
Doxylamine
Embramine
Etodroxizine
Etybenzatropine (ethylbenztropine)
Etymemazine
Fenethazine
Flunarizine
Histapyrrodine
Homochlorcyclizine
Hydroxyethylpromethazine
Hydroxyzine
Isopromethazine
Isothipendyl
Meclozine
Medrylamine
Mepyramine (pyrilamine)
Mequitazine
Methafurylene
Methapyrilene
Methdilazine
Moxastine
Orphenadrine
Oxatomide
Oxomemazine
Perlapine
Phenindamine
Pheniramine
Phenyltoloxamine
Pimethixene
Piperoxan
Pipoxizine
Promethazine
Propiomazine
Pyrrobutamine
Talastine
Thenalidine
Thenyldiamine
Thiazinamium
Thonzylamine
Tolpropamine
Tripelennamine
Triprolidine
Second/third-generation: Acrivastine
Alinastine
Astemizole
Azelastine
Bamirastine
Barmastine
Bepiastine
Bepotastine
Bilastine
Cabastinen
Carebastine
Cetirizine
Clemastine
Clemizole
Clobenztropine
Desloratadine
Dorastine
Ebastine
Efletirizine
Emedastine
Epinastine
Fexofenadine
Flezelastine
Ketotifen
Latrepirdine
Levocabastine
Levocetirizine
Linetastine
Loratadine
Mapinastine
Mebhydrolin
Mizolastine
Moxastine
Noberastine
Octastine
Olopatadine
Perastine
Pibaxizine
Piclopastine
Quifenadine (phencarol)
Rocastine
Rupatadine
Setastine
Sequifenadine (bicarphen)
Talastine
Temelastine
Terfenadine
Vapitadine
Zepastine
Others: Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, RP-5063, ziprasidone, zotepine)
Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione)
Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline)
Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine)
Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene)
Unknown/unsorted: Azanator
Belarizine
Elbanizine
Flotrenizine
GSK1004723
Napactadine
Tagorizine
Trelnarizine
Trenizine
H2
Agonists: Amthamine
Betazole
Dimaprit
Histamine
HTMT
Impromidine
L-Histidine
UR-AK49
Antagonists: Bisfentidine
Burimamide
Cimetidine
Dalcotidine
Donetidine
Ebrotidine
Etintidine
Famotidine
Isolamtidine
Lafutidine
Lamtidine
Lavoltidine (loxtidine)
Lupitidine
Metiamide
Mifentidine
Niperotidine
Nizatidine
Osutidine
Oxmetidine
Pibutidine
Quisultazine (quisultidine)
Ramixotidine
Ranitidine
Roxatidine
Sufotidine
Tiotidine
Tuvatidine
Venritidine
Xaltidine
Zolantidine
H3
Agonists: α-Methylhistamine
Cipralisant
Histamine
Imetit
Immepip
Immethridine
L-Histidine
Methimepip
Proxyfan
Antagonists: A-349,821
A-423,579
ABT-239
ABT-652
AZD5213
Bavisant
Betahistine
Burimamide
Ciproxifan
Clobenpropit
Conessine
Enerisant
GSK-189,254
Impentamine
Iodophenpropit
Irdabisant
JNJ-5207852
MK-0249
NNC 38-1049
PF-03654746
Pitolisant
SCH-79687
Thioperamide
VUF-5681
H4
Agonists: 4-Methylhistamine
α-Methylhistamine
Histamine
L-Histidine
OUP-16
VUF-8430
Antagonists: JNJ-7777120
Mianserin
Seliforant
Thioperamide
Toreforant
VUF-6002
See also: Receptor/signaling modulators • Monoamine metabolism modulators • Monoamine reuptake inhibitors
[show]
v
t
e
Ion channel modulators
Calcium
VDCCs
Blockers
L-type-selective: Dihydropyridines: Amlodipine
Aranidipine
Azelnidipine
Barnidipine
Clevidipine
Cronidipine
Darodipine
Dexniguldipine
Elgodipine
Elnadipine
Felodipine
Flordipine
Furnidipine
Iganidipine
Isradipine
Lacidipine
Lemildipine
Lercanidipine
Levamlodipine
Levniguldipine
Manidipine
Mepirodipine
Mesudipine
Nicardipine
Nifedipine
Niguldipine
Niludipine
Nilvadipine
Nimodipine
Nisoldipine
Nitrendipine
Olradipine
Oxodipine
Palonidipine
Pranidipine
Ryodipine (riodipine)
Sagandipine
Sornidipine
Teludipine
Tiamdipine
Trombodipine
Vatanidipine; Diltiazem derivatives: Clentiazem
Diltiazem
Iprotiazem
Nictiazem
Siratiazem; Phenylalkylamines: Anipamil
Dagapamil
Devapamil
Dexverapamil
Emopamil
Etripamil
Falipamil
Gallopamil
Levemopamil
Nexopamil
Norverapamil
Ronipamil
Tiapamil
Verapamil; Others: AH-1058
Brinazarone
Budiodarone
Celivarone
Cyproheptadine
Dronedarone
Fantofarone
SR-33805
Tetrahydropalmatine
N-type-selective: ω-Conotoxins
ω-Conotoxin GVIA
Caroverine
Huwentoxin XVI
Leconotide (ω-conotoxin CVID)
PD-173212
Ralfinamide
Safinamide
Z160
Ziconotide (ω-conotoxin MVIIA)
P-type-selective: ω-Agatoxin IVA
ω-Agatoxin IVB
R-type-selective: SNX-482
T-type-selective: ABT-639
ML-218
Niflumic acid
NNC 55-0396
ProTx I
Z944
Zonisamide
Non-selective: ω-Agatoxin TK
ω-Conotoxin MVIIC
Benidipine
Bepridil
Cilnidipine
Cinnarizine
Dotarizine
Efonidipine
Flunarizine
Lamotrigine
Levetiracetam
Lomerizine
Loperamide
Mibefradil
NP078585
Ruthenium red
TROX-1
α2δ subunit-selective (gabapentinoids): 4-Methylpregabalin
Arbaclofen
Arbaclofen placarbil
Atagabalin
Baclofen
Gabapentin
Gabapentin enacarbil
Imagabalin
Mirogabalin
PD-200,347
PD-217,014
PD-299,685
Phenibut
Pregabalin
Others/unsorted: Bencyclane
Berbamine
Bevantolol
Canadine
Carboxyamidotriazole
Cycleanine
Dauricine
Dimeditiapramine
Diproteverine
Enpiperate
Eperisone
Elpetrigine
Ethadione
Ethanol (alcohol)
Ethosuximide
Fasudil
Fendiline
Fostedil
Imepitoin
JTV-519
Lidoflazine
Magnesium
Manoalide
Mesuximide
Monatepil
Naftopidil
Ochratoxin A
Osthol
Otilonium bromide
Paramethadione
Phensuximide
Pinaverium bromide
Prenylamine
Rhynchophylline
Sesamodil
Silperisone
Sipatrigine
Terodiline
Tetrandrine
Tolperisone
Trimethadione
Valperinol
Activators
L-type-selective: Bay K8644
Potassium
VGKCs
Blockers
3,4-Diaminopyridine (amifampridine)
4-Aminopyridine (fampridine/dalfampridine)
Adekalant
Almokalant
Amiodarone
Azimilide
Bretylium
Bunaftine
Charybdotoxin
Clamikalant
Conotoxins
Dalazatide
Dendrotoxin
Dofetilide
Dronedarone
E-4031
Hanatoxin
HgeTx1
HsTx1
Ibutilide
Inakalant
Kaliotoxin
Linopirdine
Lolitrem B
Maurotoxin
Nifekalant
Notoxin
Paxilline
Pinokalant
Quinidine
ShK-186
Sotalol
Tedisamil
Terikalant
Tetraethylammonium
Vernakalant
hERG (KCNH2, Kv11.1)-specific: Ajmaline
Amiodarone
AmmTX3
Astemizole
Azaspiracid
AZD1305
Azimilide
Bedaquiline
BeKm-1
BmTx3
BRL-32872
Chlorpromazine
Cisapride
Clarithromycin
Darifenacin
Dextropropoxyphene
Diallyl trisulfide
Domperidone
E-4031
Ergtoxins
Erythromycin
Gigactonine
Haloperidol
Ketoconazole
Norpropoxyphene
Orphenadrine
Pimozide
PNU-282,987
Promethazine
Quinidine
Ranolazine
Roxithromycin
Sertindole
Solifenacin
Tamulotoxin
Terodiline
Terfenadine
Thioridazine
Tolterodine
Vanoxerine
Vernakalant
KCNQ (Kv7)-specific: Linopirdine
XE-991
Spooky toxin (SsTx)
Activators
KCNQ (Kv7)-specific: Flupirtine
Retigabine
IRKs
Blockers
KATP-specific: Acetohexamide
Carbutamide
Chlorpropamide
Glibenclamide (glyburide)
Glibornuride
Glicaramide
Gliclazide
Glimepiride
Glipizide
Gliquidone
Glisoxepide
Glyclopyramide
Glycyclamide
Metahexamide
Mitiglinide
Nateglinide
Repaglinide
Tolazamide
Tolbutamide
GIRK-specific: Barium
Caramiphen
Cloperastine
Clozapine
Dextromethorphan
Ethosuximide
Ifenprodil
Tertiapin
Tipepidine
Activators
KATP-specific: Aprikalim
Bimakalim
Cromakalim
Diazoxide
Emakalim
Levcromakalim
Mazokalim
Minoxidil
Naminidil
Nicorandil
Pinacidil
Rilmakalim
Sarakalim
GIRK-specific: ML-297 (VU0456810)
KCa
Blockers
BKCa-specific: Ethanol (alcohol)
GAL-021
Activators
BKCa-specific: Flufenamic acid
Meclofenamic acid
Niflumic acid
Nimesulide
Rottlerin (mallotoxin)
Tolfenamic acid
K2Ps
Blockers
12-O-Tetradecanoylphorbol-13-acetate
Arachidonic acid
Fluoxetine
Norfluoxetine
Activators
Riluzole
Sodium
VGSCs
Blockers
Antianginals: Ranolazine
Antiarrhythmics (class I): Ajmaline
Aprindine
Disopyramide
Dronedarone
Encainide
Flecainide
Lidocaine
Lorajmine
Lorcainide
Mexiletine
Moricizine
Pilsicainide
Prajmaline
Procainamide
Propafenone
Quinidine
Sparteine
Tocainide
Anticonvulsants: Acetylpheneturide
Carbamazepine
Cenobamate
Chlorphenacemide
Elpetrigine
Eslicarbazepine acetate
Ethotoin
Fosphenytoin
Lacosamide
Licarbazepine
Mephenytoin
Oxcarbazepine
Oxitriptyline
Phenacemide
Pheneturide
Phenytoin
Rufinamide
Sipatrigine
Topiramate
Sodium valproate
Valnoctamide
Valproate pivoxil
Valproate semisodium
Valproic acid
Valpromide
Zonisamide
Local anesthetics: pFBT
Amylocaine
Articaine
Benzocaine
Bupivacaine (Levobupivacaine, Ropivacaine)
Butacaine
Butamben
Chloroprocaine
Cinchocaine
Cocaine
Cyclomethycaine
Dimethocaine
Diphenhydramine
Etidocaine
Hexylcaine
Iontocaine
Lidocaine
Mepivacaine
Meprylcaine
Metabutoxycaine
Orthocaine
Piperocaine
Prilocaine
Procaine
Propoxycaine
Proxymetacaine
Risocaine
Tetracaine
Trimecaine
Analgesics: AZD-3161
DSP-2230
Funapide
GDC-0276
NKTR-171
PF-04531083
PF-05089771
Ralfinamide
Raxatrigine
RG7893 (GDC-0287)
Toxins: Conotoxins
Neosaxitoxin
Saxitoxin
Tetrodotoxin
Zetekitoxin AB
Others: Buprenorphine
Evenamide
Menthol (mint)
Safinamide
Tricyclic antidepressants
Activators
Aconitine
Atracotoxins (Robustoxin, Versutoxin)
Batrachotoxin
Ciguatoxins
Grayanotoxins
Poneratoxin
ENaC
Blockers
Amiloride
Benzamil
Triamterene
Activators
Solnatide
ASICs
Blockers
A-317567
Amiloride
Aspirin
Ibuprofen
PcTX1
Chloride
CaCCs
Blockers
Crofelemer
DIDS
Ethacrynic acid
Flufenamic acid
Fluoxetine
Furosemide
Glibenclamide
Mefloquine
Mibefradil
Niflumic acid
Activators
Carbachol
CFTR
Blockers
Glibenclamide
Lonidamine
Piretanide
Activators
1,7-Phenanthroline
1,10-Phenanthroline
4,7-Phenanthroline
7,8-Benzoquinoline
Ivacaftor
Phenanthridine
Unsorted
Blockers
Bumetanide
Flufenamic acid
Meclofenamic acid
Mefenamic acid
Mepacrine
Niflumic acid
Talniflumate
Tolfenamic acid
Trifluoperazine
Others
TRPs
See here instead.
See also: Receptor/signaling modulators • Transient receptor potential channel modulators
[show]
v
t
e
Monoamine reuptake inhibitors
DAT
(DRIs)
Piperazines: DBL-583
GBR-12783
GBR-12935
GBR-13069
GBR-13098
Nefazodone
Vanoxerine
Piperidines: 4-Fluoropethidine
Benocyclidine (BTCP)
Desoxypipradrol
Dexmethylphenidate
Difemetorex
Ethylphenidate
HDMP-28
Methylphenidate
Pethidine (meperidine)
Phencyclidine
Pipradrol
Tenocyclidine
Pyrrolidines: Diphenylprolinol
MDPV
Naphyrone
Prolintane
Pyrovalerone
Tropanes: Altropane
Benzatropine (benztropine)
Brasofensine
CFT
Cocaine
Dichloropane
Difluoropine
Etybenzatropine (ethybenztropine)
FE-β-CPPIT
FP-β-CPPIT
Ioflupane (123I)
RTI-55
RTI-112
RTI-113
RTI-121
RTI-126
RTI-150
RTI-177
RTI-229
RTI-336
Tesofensine
Troparil
Tropoxane
WF-11
WF-23
WF-31
WF-33
Others: Adrafinil
Amifitadine
Armodafinil
Amfonelic acid
Amineptine
Ansofaxine
BTQ
BTS 74,398
Bupropion
Chaenomeles speciosa
Ciclazindol
Dasotraline
Desmethylsertraline
Desmethylsibutramine
Diclofensine
Didesmethylsibutramine
Dimethocaine
Diphenylpyraline
Dizocilpine (MK-801)
DOV-102,677
DOV-216,303
Efavirenz
Ephenidine
Esketamine
EXP-561
Fencamfamin
Fezolamine
Fluorenol
GYKI-52895
Indatraline
Ketamine
Lefetamine
Levophacetoperane
Liafensine
LR-5182
Manifaxine
Mazindol
Medifoxamine
Mesocarb
Metaphit
MIN-117 (WF-516)
Modafinil
Nefopam
Nomifensine
NS-2359
O-2172
Oroxylin A
Perafensine
Pridefine
Radafaxine
Rimcazole
Sertraline
Sibutramine
Solriamfetol
Tametraline
Tedatioxetine
Tripelennamine
Venlafaxine
NET
(NRIs)
Selective norepinephrine reuptake inhibitors: Amedalin
Alseroxylon
Ciclazindol
Daledalin
Edivoxetine
Esreboxetine
Lortalamine
Mazindol
Nisoxetine
Reboxetine
Talopram
Talsupram
Tandamine
Teniloxazine
Viloxazine
Norepinephrine–dopamine reuptake inhibitors: Amineptine
Bupropion
Fencamine
Fencamfamin
Hydroxybupropion
Lefetamine
Levophacetoperane
LR-5182
Manifaxine
Methylphenidate
Nomifensine
O-2172
Radafaxine
Solriamfetol
Serotonin–norepinephrine reuptake inhibitors: Atomoxetine (tomoxetine)
BTS-54505
CP-39,332
Desvenlafaxine
Duloxetine
Eclanamine
Levomilnacipran
McN-5652
Milnacipran
N-Methyl-PPPA
Nafenodone
PPPA
Tofenacin
Venlafaxine
WY-45233
Serotonin–norepinephrine–dopamine reuptake inhibitors: 3,3-Diphenylcyclobutanamine
Amifitadine
Ansofaxine
Bicifadine
Brasofensine
Centanafadine
Cocaine
Dasotraline
Desmethylsertraline
Desmethylsibutramine
Diclofensine
Didesmethylsibutramine
DOV-102677
DOV-216303
EXP-561
Fezolamine
HDMP-28
Indatraline
JNJ-7925476
JZ-IV-10
Liafensine
Mazindol
Naphyrone
Nefazodone
Nefopam
NS-2359
Perafensine
PRC200
Pridefine
SEP-228431
SEP-228432
Sibutramine
Tedatioxetine
Tesofensine
Tropanes (e.g., cocaine)
Tricyclic antidepressants: Amitriptyline
Butriptyline
Cianopramine
Clomipramine
Desipramine
Dosulepin (dothiepin)
Doxepin
Imipramine
Lofepramine
Melitracen
Nortriptyline
Protriptyline
Trimipramine
Tetracyclic antidepressants: Amoxapine
Maprotiline
Mianserin
Oxaprotiline
Setiptiline
Others: Antihistamines (e.g., brompheniramine, chlorphenamine, pheniramine, tripelennamine)
Antipsychotics (e.g., loxapine, ziprasidone)
Arylcyclohexylamines (e.g., ketamine, phencyclidine)
Dopexamine
Ephenidine
Ginkgo biloba
Indeloxazine
Nefazodone
Opioids (e.g., desmetramadol, methadone, pethidine (meperidine), tapentadol, tramadol, levorphanol)
SERT
(SRIs)
Selective serotonin reuptake inhibitors: Alaproclate
Centpropazine
Cericlamine
Citalopram
Dapoxetine
Desmethylcitalopram
Didesmethylcitalopram
Escitalopram
Femoxetine
Fluoxetine
Fluvoxamine
Indalpine
Ifoxetine
Norfluoxetine
Omiloxetine
Panuramine
Paroxetine
PIM-35
Pirandamine
RTI-353
Seproxetine
Sertraline
Zimelidine
Selective serotonin reuptake inhibitors and serotonin receptor modulators: Etoperidone
Litoxetine
Lubazodone
LY-393558
SB-649915
TGBA01AD
Trazodone
Vilazodone
Vortioxetine
Serotonin–norepinephrine reuptake inhibitors: Atomoxetine (tomoxetine)
Bicifadine
BTS-54505
CP-39332
Desvenlafaxine
Duloxetine
Eclanamine
Levomilnacipran
McN-5652
Milnacipran
N-Methyl-PPPA
PPPA
Tofenacin
Venlafaxine
WY-45233
Serotonin–norepinephrine–dopamine reuptake inhibitors: 3,3-Diphenylcyclobutanamine
Amifitadine
Ansofaxine
Bicifadine
Brasofensine
Centanafadine
Cocaine
Dasotraline
Desmethylsertraline
Desmethylsibutramine
Diclofensine
Didesmethylsibutramine
DOV-102677
DOV-216303
EXP-561
Fezolamine
HDMP-28
Indatraline
JNJ-7925476
JZ-IV-10
Liafensine
Mazindol
Naphyrone
Nefazodone
Nefopam
NS-2359
Perafensine
PRC200
Pridefine
SEP-228431
SEP-228432
Sibutramine
Tedatioxetine
Tesofensine
Tropanes (e.g., cocaine)
Tricyclic antidepressants: Amitriptyline
Cianopramine
Clomipramine
Cyanodothiepin
Desipramine
Dosulepin (dothiepin)
Doxepin
Imipramine
Lofepramine
Nortriptyline
Pipofezine
Protriptyline
Others: A-80426
Amoxapine
Antihistamines (e.g., brompheniramine, chlorphenamine, dimenhydrinate, diphenhydramine, mepyramine (pyrilamine), pheniramine, tripelennamine)
Antipsychotics (e.g., loxapine, ziprasidone)
Arylcyclohexylamines (e.g., 3-MeO-PCP, esketamine, ketamine, methoxetamine, phencyclidine)
Cyclobenzaprine
Delucemine
Dextromethorphan
Dextrorphan
Efavirenz
Medifoxamine
Mesembrine
Mifepristone
MIN-117 (WF-516)
N-Me-5-HT
Opioids (e.g., dextropropoxyphene, methadone, pethidine (meperidine), levorphanol, tapentadol, tramadol)
Roxindole
VMATs
Amiodarone
Amphetamines (e.g., amphetamine, methamphetamine, MDMA)
APP
AZIK
Bietaserpine
Deserpidine
Deutetrabenazine
Dihydrotetrabenazine
Efavirenz
GBR-12935
GZ-793A
Ibogaine
Ketanserin
Lobeline
Methoxytetrabenazine
Reserpine
Rose bengal
Tetrabenazine
Valbenazine
Vanoxerine (GBR-12909)
Others
DAT enhancers: Luteolin
DAT modulators: Agonist-like: SoRI-9804
SoRI-20040; Antagonist-like: SoRI-20041
See also: Receptor/signaling modulators • Monoamine releasing agents • Adrenergics • Dopaminergics • Serotonergics • Monoamine metabolism modulators • Monoamine neurotoxins
[show]
v
t
e
Muscarinic acetylcholine receptor modulators
mAChRs
Agonists
77-LH-28-1
AC-42
AC-260,584
Aceclidine
Acetylcholine
AF30
AF150(S)
AF267B
Alvameline
AQRA-741
Arecoline
Bethanechol
Bevonium
Butyrylcholine
Carbachol
CDD-0034
CDD-0078
CDD-0097
CDD-0098
CDD-0102
Cevimeline
Choline
cis-Dioxolane
Clozapine
Desmethylclozapine (norclozapine)
Ethoxysebacylcholine
Itameline
LY-593,039
L-689,660
LY-2,033,298
McNA343
Methacholine
Milameline
Muscarine
NGX-267
Ocvimeline
Oxotremorine
PD-151,832
Pilocarpine
RS86
Sabcomeline
SDZ 210-086
Sebacylcholine
Suberyldicholine
Talsaclidine
Tazomeline
Thiopilocarpine
Vedaclidine
VU-0029767
VU-0090157
VU-0152099
VU-0152100
VU-0238429
WAY-132,983
Xanomeline
YM-796
Antagonists
3-Quinuclidinyl benzilate
4-DAMP
Aclidinium bromide (+formoterol)
Abediterol
AF-DX 250
AF-DX 384
Ambutonium bromide
Anisodamine
Anisodine
Antihistamines (first-generation) (e.g., brompheniramine, buclizine, captodiame, chlorphenamine (chlorpheniramine), cinnarizine, clemastine, cyproheptadine, dimenhydrinate, dimetindene, diphenhydramine, doxylamine, meclizine, mepyramine (pyrilamine), mequitazine, perlapine, phenindamine, pheniramine, phenyltoloxamine, promethazine, propiomazine, triprolidine)
AQ-RA 741
Atropine
Atropine methonitrate
Atypical antipsychotics (e.g., clozapine, fluperlapine, olanzapine (+fluoxetine), rilapine, quetiapine, tenilapine, zotepine)
Benactyzine
Benzatropine (benztropine)
Benzilone
Benzilylcholine mustard
Benzydamine
BIBN 99
Biperiden
Bornaprine
Camylofin
CAR-226,086
CAR-301,060
CAR-302,196
CAR-302,282
CAR-302,368
CAR-302,537
CAR-302,668
Caramiphen
Cimetropium bromide
Clidinium bromide
Cloperastine
CS-27349
Cyclobenzaprine
Cyclopentolate
Darifenacin
DAU-5884
Desfesoterodine
Dexetimide
DIBD
Dicycloverine (dicyclomine)
Dihexyverine
Difemerine
Diphemanil metilsulfate
Ditran
EA-3167
EA-3443
EA-3580
EA-3834
Emepronium bromide
Etanautine
Etybenzatropine (ethybenztropine)
Fenpiverinium
Fentonium
Fesoterodine
Flavoxate
Glycopyrronium bromide (+beclometasone/formoterol, +indacaterol)
Hexahydrodifenidol
Hexahydrosiladifenidol
Hexbutinol
Hexocyclium
Himbacine
HL-031,120
Homatropine
Imidafenacin
Ipratropium bromide (+salbutamol)
Isopropamide
J-104,129
Hyoscyamine
Mamba toxin 3
Mamba toxin 7
Mazaticol
Mebeverine
Meladrazine
Mepenzolate
Methantheline
Methoctramine
Methylatropine
Methylhomatropine
Methylscopolamine
Metixene
Muscarinic toxin 7
N-Ethyl-3-piperidyl benzilate
N-Methyl-3-piperidyl benzilate
Nefopam
Octatropine methylbromide (anisotropine methylbromide)
Orphenadrine
Otenzepad (AF-DX 116)
Otilonium bromide
Oxapium iodide
Oxitropium bromide
Oxybutynin
Oxyphencyclimine
Oxyphenonium bromide
PBID
PD-102,807
PD-0298029
Penthienate
Pethidine
pFHHSiD
Phenglutarimide
Phenyltoloxamine
Pipenzolate bromide
Piperidolate
Pirenzepine
Piroheptine
Pizotifen
Poldine
Pridinol
Prifinium bromide
Procyclidine
Profenamine (ethopropazine)
Propantheline bromide
Propiverine
Quinidine
Revefenacin
Rociverine
RU-47,213
SCH-57,790
SCH-72,788
SCH-217,443
Scopolamine (hyoscine)
Scopolamine butylbromide (hyoscine butylbromide)
Silahexacyclium
Sofpironium bromide
Solifenacin
SSRIs (e.g., femoxetine, paroxetine)
Telenzepine
Terodiline
Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin, mirtazapine)
Tiemonium iodide
Timepidium bromide
Tiotropium bromide
Tiquizium bromide
Tofenacin
Tolterodine
Tricyclic antidepressants (e.g., amitriptyline (+perphenazine), amitriptylinoxide, butriptyline, cidoxepin, clomipramine, desipramine, desmethyldesipramine, dibenzepin, dosulepin (dothiepin), doxepin, imipramine, lofepramine, nitroxazepine, northiaden (desmethyldosulepin), nortriptyline, protriptyline, quinupramine, trimipramine)
Tridihexethyl
Trihexyphenidyl
Trimebutine
Tripitamine (tripitramine)
Tropacine
Tropatepine
Tropicamide
Trospium chloride
Typical antipsychotics (e.g., chlorpromazine, chlorprothixene, cyamemazine (cyamepromazine), loxapine, mesoridazine, thioridazine)
Umeclidinium bromide (+vilanterol)
WIN-2299
Xanomeline
Zamifenacin
Precursors
(and prodrugs)
Acetyl-coA
Adafenoxate
Choline (lecithin)
Citicoline
Cyprodenate
Dimethylethanolamine
Glycerophosphocholine
Meclofenoxate (centrophenoxine)
Phosphatidylcholine
Phosphatidylethanolamine
Phosphorylcholine
Pirisudanol
See also: Receptor/signaling modulators • Nicotinic acetylcholine receptor modulators • Acetylcholine metabolism/transport modulators
[show]
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e
Serotonin receptor modulators
5-HT1
5-HT1A
Agonists: 8-OH-DPAT
Adatanserin
Amphetamine
Antidepressants (e.g., etoperidone, hydroxynefazodone, nefazodone, trazodone, triazoledione, vilazodone, vortioxetine)
Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, cariprazine, clozapine, lurasidone, quetiapine, ziprasidone)
Azapirones (e.g., buspirone, eptapirone, gepirone, perospirone, tandospirone)
Bay R 1531
Befiradol
BMY-14802
Cannabidiol
Dimemebfe
Dopamine
Ebalzotan
Eltoprazine
Enciprazine
Ergolines (e.g., bromocriptine, cabergoline, dihydroergotamine, ergotamine, lisuride, LSD, methylergometrine (methylergonovine), methysergide, pergolide)
F-11461
F-12826
F-13714
F-14679
F-15063
F-15599
Flesinoxan
Flibanserin
Flumexadol
Lesopitron
LY-293284
LY-301317
mCPP
MKC-242
Naluzotan
NBUMP
Osemozotan
Oxaflozane
Pardoprunox
Piclozotan
Rauwolscine
Repinotan
Roxindole
RU-24969
S-14506
S-14671
S-15535
Sarizotan
Serotonin (5-HT)
SSR-181507
Sunepitron
Tryptamines (e.g., 5-CT, 5-MeO-DMT, 5-MT, bufotenin, DMT, indorenate, N-Me-5-HT, psilocin, psilocybin)
TGBA01AD
U-92016A
Urapidil
Vilazodone
Xaliproden
Yohimbine
Antagonists: Atypical antipsychotics (e.g., iloperidone, risperidone, sertindole)
AV965
Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, pindolol, propranolol, tertatolol)
BMY-7378
CSP-2503
Dotarizine
Ergolines (e.g., metergoline)
Flopropione
GR-46611
Isamoltane
Lecozotan
Mefway
Metitepine (methiothepin)
MIN-117 (WF-516)
MPPF
NAN-190
Robalzotan
S-15535
SB-649915
SDZ 216-525
Spiperone
Spiramide
Spiroxatrine
UH-301
WAY-100135
WAY-100635
Xylamidine
Unknown/unsorted: Acetryptine
Ergolines (e.g., ergometrine (ergonovine))
5-HT1B
Agonists: CGS-12066A
CP-93129
CP-94253
CP-122,288
CP-135807
Eltoprazine
Ergolines (e.g., bromocriptine, dihydroergotamine, ergotamine, methylergometrine (methylergonovine), methysergide, pergolide)
mCPP
RU-24969
Serotonin (5-HT)
Triptans (e.g., avitriptan, donitriptan, eletriptan, sumatriptan, zolmitriptan)
TFMPP
Tryptamines (e.g., 5-BT, 5-CT, 5-MT, DMT)
Vortioxetine
Antagonists: AR-A000002
Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, tertatolol)
Elzasonan
Ergolines (e.g., metergoline)
GR-127935
Isamoltane
LY-393558
Metitepine (methiothepin)
SB-216641
SB-224289
SB-236057
Yohimbine
Unknown/unsorted: Ergolines (e.g., cabergoline, ergometrine (ergonovine), lisuride)
5-HT1D
Agonists: CP-122,288
CP-135807
CP-286601
Ergolines (e.g., bromocriptine, cabergoline, dihydroergotamine, ergotamine, LSD, methysergide)
GR-46611
L-694247
L-772405
mCPP
PNU-109291
PNU-142633
Serotonin (5-HT)
TGBA01AD
Triptans (e.g., almotriptan, avitriptan, donitriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan)
Tryptamines (e.g., 5-BT, 5-CT, 5-Et-DMT, 5-MT, 5-(nonyloxy)tryptamine, DMT)
Antagonists: Alniditan
BRL-15572
Elzasonan
Ergolines (e.g., metergoline)
GR-127935
Ketanserin
LY-310762
LY-367642
LY-393558
LY-456219
LY-456220
Metitepine (methiothepin)
Mianserin
Ritanserin
Yohimbine
Ziprasidone
Unknown/unsorted: Acetryptine
Ergolines (e.g., lisuride, lysergol, pergolide)
5-HT1E
Agonists: BRL-54443
Ergolines (e.g., methysergide)
Serotonin (5-HT)
Triptans (e.g., eletriptan)
Tryptamines (e.g., tryptamine)
Antagonists: Metitepine (methiothepin)
Unknown/unsorted: Ergolines (e.g., ergometrine (ergonovine), lysergol, methylergometrine (methylergonovine)
5-HT1F
Agonists: BRL-54443
CP-122,288
Ergolines (e.g., bromocriptine, lysergol, methylergometrine (methylergonovine) methysergide)
Lasmiditan
LY-334370
Serotonin (5-HT)
Triptans (e.g., eletriptan, naratriptan, sumatriptan)
Tryptamines (e.g., 5-MT)
Antagonists: Mianserin
Metitepine (methiothepin)
5-HT2
5-HT2A
Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN-NBOH, 2CBFly-NBOMe)
2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21)
2C-B-FLY
2CB-Ind
5-Methoxytryptamines (5-MeO-DET, 5-MeO-DiPT, 5-MeO-DMT, 5-MeO-DPT, 5-MT)
α-Alkyltryptamines (e.g., 5-Cl-αMT, 5-Fl-αMT, 5-MeO-αET, 5-MeO-αMT, α-Me-5-HT, αET, αMT)
AL-34662
AL-37350A
Bromo-DragonFLY
Dimemebfe
DMBMPP
DOx (e.g., DOB, DOC, DOI, DOM)
Efavirenz
Ergolines (e.g., 1P-LSD, ALD-52, bromocriptine, cabergoline, ergine (LSA), ergometrine (ergonovine), ergotamine, lisuride, LA-SS-Az, LSB, LSD, LSD-Pip, LSH, LSP, methylergometrine (methylergonovine), pergolide)
Flumexadol
Jimscaline
Lorcaserin
MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA)
O-4310
Oxaflozane
PHA-57378
PNU-22394
PNU-181731
RH-34
Phenethylamines (e.g., lophophine, mescaline)
Piperazines (e.g., BZP, quipazine, TFMPP)
Serotonin (5-HT)
TCB-2
TFMFly
Tryptamines (e.g., 5-BT, 5-CT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)
Antagonists: 5-I-R91150
5-MeO-NBpBrT
AC-90179
Adatanserin
Altanserin
Antihistamines (e.g., cyproheptadine, hydroxyzine, ketotifen, perlapine)
AMDA
Atypical antipsychotics (e.g., amperozide, aripiprazole, asenapine, blonanserin, brexpiprazole, carpipramine, clocapramine, clorotepine, clozapine, fluperlapine, gevotroline, iloperidone, lurasidone, melperone, mosapramine, ocaperidone, olanzapine, paliperidone, quetiapine, risperidone, sertindole, zicronapine, ziprasidone, zotepine)
Cinanserin
CSP-2503
Deramciclane
Dotarizine
Eplivanserin
Ergolines (e.g., amesergide, LY-53857, LY-215840, mesulergine, metergoline, methysergide, sergolexole)
Fananserin
Flibanserin
Glemanserin
Irindalone
Ketanserin
KML-010
Landipirdine
LY-393558
mCPP
Medifoxamine
Metitepine (methiothepin)
MIN-101
MIN-117 (WF-516)
Naftidrofuryl
Nantenine
Nelotanserin
Opiranserin (VVZ-149)
Pelanserin
Phenoxybenzamine
Pimavanserin
Pirenperone
Pizotifen
Pruvanserin
Rauwolscine
Ritanserin
S-14671
Sarpogrelate
Serotonin antagonists and reuptake inhibitors (e.g., etoperidone, hydroxynefazodone, lubazodone, mepiprazole, nefazodone, triazoledione, trazodone)
SR-46349B
TGBA01AD
Teniloxazine
Temanogrel
Tetracyclic antidepressants (e.g., amoxapine, aptazapine, esmirtazapine, maprotiline, mianserin, mirtazapine)
Tricyclic antidepressants (e.g., amitriptyline)
Typical antipsychotics (e.g., chlorpromazine, fluphenazine, haloperidol, loxapine, perphenazine, pimozide, pipamperone, prochlorperazine, setoperone, spiperone, spiramide, thioridazine, thiothixene, trifluoperazine)
Volinanserin
Xylamidine
Yohimbine
Unknown/unsorted: Ergolines (e.g., dihydroergotamine, nicergoline)
5-HT2B
Agonists: 4-Methylaminorex
Aminorex
Amphetamines (e.g., chlorphentermine, cloforex, dexfenfluramine, fenfluramine, levofenfluramine, norfenfluramine)
BW-723C86
DOx (e.g., DOB, DOC, DOI, DOM)
Ergolines (e.g., cabergoline, dihydroergocryptine, dihydroergotamine, ergotamine, methylergometrine (methylergonovine), methysergide, pergolide)
Lorcaserin
MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, [MMDA (drug)
Antagonists: Agomelatine
Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, clozapine, N-desalkylquetiapine (norquetiapine), N-desmethylclozapine (norclozapine), olanzapine, pipamperone, quetiapine, risperidone, ziprasidone)
Cyproheptadine
EGIS-7625
Ergolines (e.g., amesergide, bromocriptine, lisuride, LY-53857, LY-272015, mesulergine)
Ketanserin
LY-393558
mCPP
Metadoxine
Metitepine (methiothepin)
Pirenperone
Pizotifen
Propranolol
PRX-08066
Rauwolscine
Ritanserin
RS-127445
Sarpogrelate
SB-200646
SB-204741
SB-206553
SB-215505
SB-221284
SB-228357
SDZ SER-082
Tegaserod
Tetracyclic antidepressants (e.g., amoxapine, mianserin, mirtazapine)
Trazodone
Typical antipsychotics (e.g., chlorpromazine)
TIK-301
Yohimbine
Unknown/unsorted: Ergolines (e.g., ergometrine (ergonovine))
5-HT2C
Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21)
5-Methoxytryptamines (5-MeO-DET, 5-MeO-DiPT, 5-MeO-DMT, 5-MeO-DPT, 5-MT)
α-Alkyltryptamines (e.g., 5-Cl-αMT, 5-Fl-αMT, 5-MeO-αET, 5-MeO-αMT, α-Me-5-HT, αET, αMT)
A-372159
AL-38022A
Alstonine
CP-809101
Dimemebfe
DOx (e.g., DOB, DOC, DOI, DOM)
Ergolines (e.g., ALD-52, cabergoline, dihydroergotamine, ergine (LSA), ergotamine, lisuride, LA-SS-Az, LSB, LSD, LSD-Pip, LSH, LSP, pergolide)
Flumexadol
Lorcaserin
MDxx (e.g., MDA (tenamfetamine), MDMA (midomafetamine), MDOH, MMDA)
MK-212
Org 12962
Org 37684
Oxaflozane
PHA-57378
Phenethylamines (e.g., lophophine, mescaline)
Piperazines (e.g., aripiprazole, BZP, mCPP, quipazine, TFMPP)
PNU-22394
PNU-181731
Ro60-0175
Ro60-0213
Serotonin (5-HT)
Tryptamines (e.g., 5-BT, 5-CT, bufotenin, DET, DiPT, DMT, DPT, psilocin, psilocybin, tryptamine)
Vabicaserin
WAY-629
WAY-161503
YM-348
Antagonists: Adatanserin
Agomelatine
Atypical antipsychotics (e.g., asenapine, clorotepine, clozapine, fluperlapine, iloperidone, melperone, olanzapine, paliperidone, quetiapine, risperidone, sertindole, ziprasidone, zotepine)
Captodiame
CEPC
Cinanserin
Cyproheptadine
Deramciclane
Desmetramadol
Dotarizine
Eltoprazine
Ergolines (e.g., amesergide, bromocriptine, LY-53857, LY-215840, mesulergine, metergoline, methysergide, sergolexole)
Etoperidone
Fluoxetine
FR-260010
Irindalone
Ketanserin
Ketotifen
Latrepirdine (dimebolin)
Medifoxamine
Metitepine (methiothepin)
Nefazodone
Pirenperone
Pizotifen
Propranolol
Ritanserin
RS-102221
S-14671
SB-200646
SB-206553
SB-221284
SB-228357
SB-242084
SB-243213
SDZ SER-082
Tedatioxetine
Tetracyclic antidepressants (e.g., amoxapine, aptazapine, esmirtazapine, maprotiline, mianserin, mirtazapine)
TIK-301
Tramadol
Trazodone
Tricyclic antidepressants (e.g., amitriptyline, nortriptyline)
Typical antipsychotics (e.g., chlorpromazine, loxapine, pimozide, pipamperone, thioridazine)
Xylamidine
Unknown/unsorted: Efavirenz
Ergolines (e.g., ergometrine (ergonovine), methylergometrine (methylergonovine))
5-HT3–7
5-HT3
Agonists: Alcohols (e.g., butanol, ethanol (alcohol), trichloroethanol)
m-CPBG
Phenylbiguanide
Piperazines (e.g., BZP, mCPP, quipazine)
RS-56812
Serotonin (5-HT)
SR-57227
SR-57227A
Tryptamines (e.g., 2-Me-5-HT, 5-CT, bufotenidine (5-HTQ))
Volatiles/gases (e.g., halothane, isoflurane, toluene, trichloroethane)
YM-31636
Antagonists: Alosetron
AS-8112
Atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine)
Azasetron
Batanopride
Bemesetron (MDL-72222)
Bupropion
Cilansetron
CSP-2503
Dazopride
Dolasetron
Galanolactone
Granisetron
Hydroxybupropion
ICS-205930
Lerisetron
Memantine
Ondansetron
Palonosetron
Ramosetron
Renzapride
Ricasetron
Tedatioxetine
Tetracyclic antidepressants (e.g., amoxapine, mianserin, mirtazapine)
Thujone
Tropanserin
Tropisetron
Typical antipsychotics (e.g., loxapine)
Volatiles/gases (e.g., nitrous oxide, sevoflurane, xenon)
Vortioxetine
Zacopride
Zatosetron
Unknown/unsorted: LY-53857
Piperazines (e.g., naphthylpiperazine)
5-HT4
Agonists: 5-MT
BIMU8
Capeserod
Cinitapride
Cisapride
CJ-033466
Dazopride
Metoclopramide
Minesapride
Mosapride
Prucalopride
PRX-03140
Renzapride
RS-67333
RS-67506
Serotonin (5-HT)
Tegaserod
Velusetrag
Zacopride
Antagonists: GR-113808
GR-125487
L-Lysine
Piboserod
RS-39604
RS-67532
SB-203186
SB-204070
5-HT5A
Agonists: Ergolines (e.g., 2-Br-LSD (BOL-148), ergotamine, LSD)
Serotonin (5-HT)
Tryptamines (e.g., 5-CT)
Valerenic Acid
Antagonists: Asenapine
Latrepirdine (dimebolin)
Metitepine (methiothepin)
Ritanserin
SB-699551
Unknown/unsorted: Ergolines (e.g., metergoline, methysergide)
Piperazines (e.g., naphthylpiperazine)
5-HT6
Agonists: Ergolines (e.g., dihydroergocryptine, dihydroergotamine, ergotamine, lisuride, LSD, mesulergine, metergoline, methysergide)
Serotonin (5-HT)
Tryptamines (e.g., 2-Me-5-HT, 5-BT, 5-CT, 5-MT, Bufotenin, E-6801, E-6837, EMD-386088, EMDT, LY-586713, N-Me-5-HT, tryptamine)
WAY-181187
WAY-208466
Antagonists: ABT-354
Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, iloperidone, olanzapine, tiospirone)
AVN-101
AVN-211
AVN-322
AVN-397
BGC20-760
BVT-5182
BVT-74316
Cerlapirdine
EGIS-12233
GW-742457
Idalopirdine
Ketanserin
Landipirdine
Latrepirdine (dimebolin)
Metitepine (methiothepin)
MS-245
PRX-07034
Ritanserin
Ro 04-6790
Ro 63-0563
SB-258585
SB-271046
SB-357134
SB-399885
SB-742457
Tetracyclic antidepressants (e.g., amoxapine, mianserin)
Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, nortriptyline)
Typical antipsychotics (e.g., chlorpromazine, loxapine)
Unknown/unsorted: Ergolines (e.g., 2-Br-LSD (BOL-148), bromocriptine, lergotrile, pergolide)
Piperazines (e.g., naphthylpiperazine)
5-HT7
Agonists: 8-OH-DPAT
AS-19
Bifeprunox
E-55888
Ergolines (e.g., LSD)
LP-12
LP-44
RU-24969
Sarizotan
Serotonin (5-HT)
Triptans (e.g., frovatriptan)
Tryptamines (e.g., 5-CT, 5-MT, bufotenin, N-Me-5-HT)
Antagonists: Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, clorotepine, clozapine, fluperlapine, olanzapine, risperidone, sertindole, tiospirone, ziprasidone, zotepine)
Butaclamol
DR-4485
EGIS-12233
Ergolines (e.g., 2-Br-LSD (BOL-148), amesergide, bromocriptine, cabergoline, dihydroergotamine, ergotamine, LY-53857, LY-215840, mesulergine, metergoline, methysergide, sergolexole)
JNJ-18038683
Ketanserin
LY-215840
Metitepine (methiothepin)
Ritanserin
SB-258719
SB-258741
SB-269970
SB-656104
SB-656104A
SB-691673
SLV-313
SLV-314
Spiperone
SSR-181507
Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin, mirtazapine)
Tricyclic antidepressants (e.g., amitriptyline, clomipramine, imipramine)
Typical antipsychotics (e.g., acetophenazine, chlorpromazine, chlorprothixene, fluphenazine, loxapine, pimozide)
Vortioxetine
Unknown/unsorted: Ergolines (e.g., lisuride, pergolide)
Piperazines (e.g., naphthylpiperazine)
See also: Receptor/signaling modulators
Adrenergics
Dopaminergics
Melatonergics
Monoamine reuptake inhibitors and releasing agents
Monoamine metabolism modulators
Monoamine neurotoxins
[show]
v
t
e
Sigma receptor modulators
σ1
Agonists: 3-PPP
4-PPBP
5-MeO-DMT
Alazocine (SKF-10047)
Amantadine
ANAVEX2-73
Arketamine
BD-737
BD-1052
Captodiame
Citalopram
CGRP
Cloperastine
Cocaine
Cutamesine (SA-4503)
Cyclazocine
Dehydroepiandrosterone (DHEA) (prasterone)
Dehydroepiandrosterone sulfate (DHEA-S) (prasterone sulfate)
Dextrallorphan
Dextromethorphan (DXM)
Dextrorphan (DXO)
Dimemorfan
Dimethyltryptamine (DMT)
Ditolylguanidine (DTG)
Donepezil
Eliprodil
Escitalopram
Fabomotizole (afobazole)
Fluoxetine
Fluvoxamine
Ifenprodil
Igmesine (JO-1784)
IPAB
Ketamine
L-687384
MDMA (midomafetamine)
Memantine
Methamphetamine
Methoxetamine
Methylphenidate
Nepinalone
Neuropeptide Y
Noscapine
OPC-14523
Opipramol
Pentazocine
Pentoxyverine (carbetapentane)
PRE-084
Pregnenolone
Pregnenolone sulfate
Pridopidine
Racemethorphan (methorphan)
Racemorphan (morphanol)
UMB-23
UMB-82
Antagonists: 3-PPP
AC-927
BD-1008
BD-1031
BD-1047
BD-1060
BD-1063
BD-1067
BMY-14802 (BMS-181100)
CM-156
Dup-734
E-5842
E-52862 (S1RA)
Haloperidol
LR-132
LR-172
MS-377
NE-100
NPC-16377
Panamesine (EMD-57455)
PD-144418
Pentazocine
Progesterone
Rimcazole (BW-234U)
Sertraline
SR-31742A
Allosteric modulators: Phenytoin; Positive: Methylphenylpiracetam
SOMCL-668
Unknown/unsorted: 3-Methoxydextrallorphan
3-MeO-PCP
4C-T-2
4-IBP
4-IPBS
4-MeO-PCP
5-MeO-DALT
5-MeO-DiPT
Amitriptyline
Azidopamil
Chlorpromazine
Clemastine
Clomipramine
Clorgiline
D-Deprenyl
DiPT
DPT
Ibogaine
Imipramine
KCR-12-83.1
Nemonapride
Noribogaine
RHL-033
RS-67,333
RTI-55
Saffron
Safinamide
Selegiline
Spipethiane
Trifluoperazine
W-18
YKP10A
σ2
Agonists: 3-PPP
Arketamine
BD-1047
BD1063
Ditolylguanidine (DTG)
DKR-1005
DKR-1051
Haloperidol
Ifenprodil
Ketamine
MDMA (midomafetamine)
Methamphetamine
OPC-14523
Opipramol
PB-28
Phencyclidine
Siramesine (Lu 28-179)
UKH-1114
Antagonists: AC-927
BD-1008
BD-1067
CM-156
CT-1812
LR-172
MIN-101
Panamesine (EMD-57455)
SAS-0132
Unknown/unsorted: 3-Methoxydextrallorphan
3-MeO-PCE
4-MeO-PCP
5-MeO-DALT
5-MeO-DiPT
Clemastine
DiPT
DPT
Ibogaine
Nemonapride
Nepinalone
Noribogaine
Pentazocine
RS-67,333
Safinamide
TMA
UMB-23
UMB-82
W-18
Unsorted
Agonists: Berberine
Ethylketazocine
Fourphit
Metaphit
Nalbuphine
Naluzotan
Tapentadol
Tenocyclidine
Antagonists: AHD1
AZ66
Lamotrigine
Naloxone
SM-21
UMB-100
UMB-101
UMB-103
UMB-116
YZ-011
YZ-069
YZ-185
Allosteric modulators: SKF-83959
Unknown/unsorted: 18-Methoxycoronaridine
BMY-13980
Butaclamol
Caramiphen
Carvotroline
Chlorphenamine (chlorpheniramine)
Chlorpromazine
Cinnarizine
Cinuperone
Clocapramine
Dezocine
EMD-59983
Hypericin (St. John's wort)
Fluphenazine
Gevotroline (WY-47384)
Mepyramine (pyrilamine)
Molindone
Perphenazine
Pimozide
Proadifen
Promethazine
Propranolol
Quinidine
Remoxipride
SL 82.0715
SR-31747A
Tiospirone (BMY-13859)
Venlafaxine
See also: Receptor/signaling modulators
[show]
v
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Tricyclics
Classes
Acridine
Anthracene
Dibenzazepine
Dibenzocycloheptene
Dibenzodiazepine
Dibenzothiazepine
Dibenzothiepin
Dibenzoxazepine
Dibenzoxepin
Phenothiazine
Pyridazinobenzoxazine
Pyridinobenzodiazepine
Thioxanthene
Antidepressants
(TCAs and TeCAs)
7-OH-Amoxapine
Amezepine
Amineptine
Amitriptyline
Amitriptylinoxide
Amoxapine
Aptazapine
Azepindole
Azipramine
Batelapine
Butriptyline
Cianopramine
Ciclazindol
Ciclopramine
Cidoxepin
Clomipramine
Cotriptyline
Cyanodothiepin
Demexiptiline
Depramine (balipramine)
Desipramine (desmethylimipramine)
Desmethylclomipramine
Desmethyltrimipramine
Dibenzepin
Dimetacrine
Dosulepin (dothiepin)
Doxepin
Enprazepine
Esmirtazapine
Fantridone
Fluotracen
Hepzidine
Homopipramol
Imipramine
Imipraminoxide
Intriptyline
Iprindole
Ketipramine
Litracen
Lofepramine
Losindole
Loxapine
Maprotiline
Mariptiline
Mazindol
Melitracen
Metapramine
Mezepine
Mianserin
Mirtazapine
Monometacrine
Naranol
Nitroxazepine
Norbutriptyline
Nordoxepin
Northiaden (nordosulepin)
Nortriptyline (noramitriptyline)
Noxiptiline
Octriptyline
Opipramol
Oxaprotiline
Pipofezine
Pirandamine
Propizepine
Protriptyline
Quinupramine
Setiptiline (teciptiline)
Spiroxepin
Tandamine
Tampramine
Tianeptine
Tienopramine
Trimipramine
Antihistamines
Azatadine
Clobenzepam
Cyproheptadine
Dacemazine
Deptropine
Desloratadine
Epinastine
Etymemazine
Fenethazine
Hydroxyethylpromethazine
Isopromethazine
Isothipendyl
Ketotifen
Latrepirdine
Loratadine
Mebhydrolin
Mequitazine
Methdilazine
Olopatadine
Oxomemazine
Phenindamine
Pimethixene
Promethazine
Propiomazine
Rupatadine
Thiazinamium
Antipsychotics
Acetophenazine
Alimemazine
Amoxapine
Asenapine
Butaclamol
Butaperazine
Carfenazine (carphenazine)
Carpipramine
Chlorpromazine
Chlorprothixene
Ciclindole
Citatepine
Clocapramine
Clomacran
Clorotepine
Clotiapine
Clozapine
Cyanothepin
Doclothepin
Docloxythepin
Erizepine
Flucindole
Flumezapine
Fluotracen
Flupentixol
Fluphenazine
Gevotroline
Homopipramol
Isofloxythepin
Levomepromazine/Methotrimeprazine
Loxapine
Lurasidone
Maroxepin
Meperathiepin
Mesoridazine
Metiapine
Metitepine
Metoxepin
Mosapramine
Naranol
Octomethothepin
Olanzapine
Oxyclothepin
Oxyprothepin
Pentiapine
Peradithiepin
Perathiepin
Perazine
Perphenazine
Periciazine
Pinoxepin
Piperacetazine
Pipotiazine
Piquindone
Prochlorperazine
Promazine
Prothipendyl
Quetiapine
Savoxepin/Cipazoxapine
Sulforidazine
Tenilapine
Thiethylperazine
Thiopropazate
Thioridazine
Thiothixene
Tilozepine
Traboxopine
Trifluoperazine
Triflupromazine
Trifluthepin
Zotepine
Zuclopenthixol
Anticonvulsants
Carbamazepine
Dizocilpine
Eslicarbazepine
Eslicarbazepine acetate
Etazepine
Licarbazepine
Oxcarbazepine
Oxitriptyline
Rispenzepine
Others
Adosopine
Aminopromazine
Atiprosin
Beloxepin
Benzoctamine
Carvedilol
Cidoxepin
Cyclobenzaprine
Damotepine
Darenzepine
Elanzepine
Fluradoline
Methylene blue
Monatepil
Nuvenzepine
Oxetorone
Perlapine
P7C3
Pinadoline
Pirenzepine
Pirolate
Pitrazepin
Pizotifen
Profenamine
Serazapine
Siltenzepine
Telenzepine
Tipindole
Tropatepine
Zolenzepine
Retrieved from "https://en.wikipedia.org/w/index.php?title=Tricyclic_antidepressant&oldid=843530543"
Categories:
Chemical classes of psychoactive drugs
Tricyclic antidepressants
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