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Beta-adrenergic agonist
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Beta adrenergic receptor agonists
Drug class
Skeletal structure formula of salbutamol (albuterol) — a widely used medication to treat asthma attacks
Class identifiers
Use
Bradycardia, Asthma, heart failure, etc.
ATC code
R03
Biological target
Adrenergic receptors (β subtype)
External links
MeSH
D000318
In Wikidata
Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, which widen the airways and result in easier breathing.[1] They are a class of sympathomimetic agents which act upon the beta adrenoceptors.[2] In general, pure beta-adrenergic agonists have the opposite function of beta blockers. Beta adrenoreceptor agonist ligands mimic the action of epinephrine and norepinephrine signaling in the heart, lungs, and smooth muscle tissue, with epinephrine expressing the highest affinity. The activation of β1, β2 and β3 activates the enzyme, adenylate cyclase. This, in turn, leads to the activation of the secondary messenger cyclic adenosine monophosphate (cAMP), cAMP then activates protein kinase A (PKA) which phosphorylates target proteins, ultimately inducing smooth muscle relaxation and contraction of the cardiac tissue.[3]
Contents
1 Function
2 Medical uses
3 Side effects
4 Receptor selectivity
4.1 β1 agonists
4.2 β2 agonists
4.3 Undetermined/unsorted
5 See also
6 References
Function[edit]
Epinephrine (adrenaline)
Activation of β1 receptors induces positive inotropic, chronotropic output of the cardiac muscle, leading to increased heart rate and blood pressure, secretion of ghrelin from the stomach, and renin release from the kidneys.[4]
Activation of β2 receptors induces smooth muscle relaxation in the lungs, gastrointestinal tract, uterus, and various blood vessels. Increased heart rate and heart muscle contraction are also associated with the β2 receptors.
β3 receptors are mainly located in adipose tissue.[5] Activation of the β3 receptors induces the metabolism of lipids.[6]
Medical uses[edit]
Indications of administration for β agonists include:
Bradycardia (slow heart rate)
Asthma
Chronic obstructive pulmonary disease (COPD)
Heart failure
Allergic reactions
Hyperkalemia
Beta blocker poisoning
Premature labor (this is an off-label use and could be detrimental)<https://www.fda.gov/Drugs/DrugSafety/ucm243539.htm>
Side effects[edit]
Although minor compared to those of epinephrine, beta agonists usually have mild to moderate adverse effects, which include anxiety, hypertension, increased heart rate, and insomnia. Other side effects include headaches and essential tremor. Hypoglycemia was also reported due to increased secretion of insulin in the body from activation of β2 receptors.
In 2013, zilpaterol, a β agonist sold by Merck, was temporarily withdrawn due to signs of sickness in some cattle that were fed the drug.[7]
Receptor selectivity[edit]
Most agonists of the beta receptors are selective for one or more beta-adrenoreceptors. For example, patients with low heart rate are given beta agonist treatments that are more "cardio-selective" such as dobutamine, which increases the force of contraction of the heart muscle. Patients who are suffering from a chronic inflammatory lung diseases such as asthma or COPD are treated with salbutamol (albuterol), which mainly induces smooth muscle relaxation in the lungs and less contraction of the heart.[8]
β3 agonists are currently in clinical research and are thought to increase the breakdown of lipids in obese patients.[9]
β1 agonists[edit]
Main article: Beta-1_adrenergic_receptor § Agonists
β1 agonists stimulate adenylyl cyclase activity and opening of calcium channel (cardiac stimulants; used to treat cardiogenic shock, acute heart failure, bradyarrhythmias). Selected examples are:
Denopamine
Dobutamine
Dopexamine (β1 and β2)
Epinephrine (non-selective)
Isoprenaline (INN), isoproterenol (USAN) (β1 and β2)
Prenalterol
Xamoterol
β2 agonists[edit]
Main article: Beta2-adrenergic agonist
β2 agonists stimulate adenylyl cyclase activity and closing of calcium channel (smooth muscle relaxants; used to treat asthma and COPD). Selected examples are:
Arformoterol
Buphenine
Clenbuterol
Dopexamine (β1 and β2)
Epinephrine (non-selective)
Fenoterol
Formoterol
Isoetarine
Isoprenaline (INN), isoproterenol (USAN) (β1 and β2)
Levosalbutamol (INN), levalbuterol (USAN)
Orciprenaline (INN), metaproterenol (USAN)
Pirbuterol
Procaterol
Ritodrine
Salbutamol (INN), albuterol (USAN)
Salmeterol
Terbutaline
Undetermined/unsorted[edit]
These agents are also listed as agonists by MeSH.[10]
Arbutamine
Befunolol
Bromoacetylalprenololmenthane
Broxaterol
Cimaterol
Cirazoline
Etilefrine
Hexoprenaline
Higenamine
Isoxsuprine
Mabuterol
Methoxyphenamine
Oxyfedrine
Ractopamine
Reproterol
Rimiterol
Tretoquinol
Tulobuterol
Zilpaterol
Zinterol
See also[edit]
Alpha-adrenergic agonist
References[edit]
Jump up ^ "WHAT ARE BETA-AGONISTS?". Thoracic.org. American Thoracic Society. Retrieved 17 October 2014.
Jump up ^ Adrenergic+beta-Agonists at the US National Library of Medicine Medical Subject Headings (MeSH)
Jump up ^ Delbruck, Max. "The beta-adrenergic receptors". PMID 12439640.
Jump up ^ Yoo, B.; et al. "Beta1-adrenergic receptors stimulate cardiac contractility and CaMKII activation in vivo and enhance cardiac dysfunction following myocardial infarction". PMID 19633206.
Jump up ^ Johnson, M. "Molecular mechanisms of beta(2)-adrenergic receptor function, response, and regulation". PMID 16387578.
Jump up ^ Lowell, B.B.; Flier, J.S. (1997). "Brown adipose tissue, beta 3-adrenergic receptors, and obesity". Annu. Rev. Med. 48. pp. 307–16. PMID 9046964.
Jump up ^ "Archived copy". Archived from the original on 2013-08-27. Retrieved 2013-08-16.
Jump up ^ Pias, M.T. "The Pharmacology of Adrenergic Receptors".
Jump up ^ Meyers, D.S.; Skwish, S.; Dickinson, K.E.; Kienzle, B.; Arbeeny, C.M. (Feb 1997). "Beta 3-adrenergic receptor-mediated lipolysis and oxygen consumption in brown adipocytes from cynomolgus monkeys". J. Clin. Endocrinol. Metab. 82 (2). pp. 395–401. PMID 9024225.
Jump up ^ MeSH list of agents 82000318
show
v
t
e
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
Pharmacomodulation
Types
♦ Enzyme: Inducer
Inhibitor
♦ Ion channel: Opener
Blocker
♦ Receptor: Agonist
Partial agonist
Antagonist
Inverse agonist
Positive allosteric modulator (PAM)
Negative allosteric modulator (NAM)
♦ Transporter [Reuptake vs Efflux]: Enhancer (RE)
Inhibitor (RI)
Releaser (RA)
♦ Miscellaneous: Precursor
Cofactor
Classes
Enzyme
see Enzyme inhibition
Ion channel
Calcium channel blocker (CCB)
Potassium channel blocker (PCB)
Sodium channel blocker (SCB)
Potassium channel opener (PCO)
Receptor &
transporter
BA/M
Adrenergic
Adrenergic receptor agonist (α
β (1
2))
Adrenergic receptor antagonist (α (1
2)
β)
Norepinephrine reuptake inhibitor (NRI)
Dopaminergic
Dopamine receptor agonist
Dopamine receptor antagonist
Dopamine reuptake inhibitor (DRI)
Histaminergic
Histamine receptor agonist
Histamine receptor antagonist (H1
H2
H3)
Serotonergic
Serotonin receptor agonist
Serotonin receptor antagonist (5-HT3)
Serotonin reuptake inhibitor (SRI)
AA
GABAergic
GABA receptor agonist
GABA receptor antagonist
GABA reuptake inhibitor (GRI)
Glutamatergic
Glutamate receptor agonist (AMPA)
Glutamate receptor antagonist (NMDA)
Glutamate reuptake inhibitor
Cholinergic
Acetylcholine receptor agonist (Muscarinic
Nicotinic)
Acetylcholine receptor antagonist (Muscarinic
Nicotinic (Ganglionic
Muscular))
Cannabinoidergic
Cannabinoid receptor agonist
Cannabinoid receptor antagonist
Endocannabinoid enhancer (eCBE)
Endocannabinoid reuptake inhibitor (eCBRI)
Opioidergic
Opioid modulator
Opioid receptor agonist
Opioid receptor antagonist
Enkephalinase inhibitor
Other
Adenosine reuptake inhibitor (AdoRI)
Angiotensin II receptor antagonist
Endothelin receptor antagonist
NK1 receptor antagonist
Vasopressin receptor antagonist
Miscellaneous
Cofactor (see Enzyme cofactors)
Precursor (see Amino acids)
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