Beta Adrenergic receptor agonists |
Drug class |
Skeletal structor formula of Salbutamol. A widely used medication to treat asthma attacks
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Use |
Bradycardia, Asthma, heart failure, etc. |
Biological target |
Adrenergic receptors (β subtype) |
ATC code |
R03 |
External links |
MeSH |
D000318 |
Beta-adrenergic agonists or Beta-agonists are medications that relax muscles of the airways, which widens the airways and results 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 being 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 and induces 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
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 is 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
Indications of administration for beta agonists include the following:
- Bradycardia (slow heart rate)
- Asthma
- Chronic obstructive pulmonary disease (COPD)
- Heart failure
- allergic reactions
- hyperkalemia
- an antidote to beta blocker poisoning
Side effects
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. Indications of hypoglycemia were also reported due to secretion of insulin in the body from activation of beta-2 receptors.
In 2013, Zilpaterol, a beta-agonist sold by Merck was temporarily withdrawn due to signs of sickness in some cattle that were fed the drug.[7]
Receptor selectivity
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 chronic obstructive pulmonary disease are treated with albuterol, which mainly induces smooth muscle relaxation in the lungs and less contraction of the heart.[8]
Beta-3 agonists are currently in clinical research and are thought to increase the breakdown of lipids in obese patients.[9]
β1 agonists
Main article: Beta-1 adrenergic receptor § agonists
β1 agonists: stimulates adenylyl cyclase activity; opening of calcium channel. (cardiac stimulants; used to treat cardiogenic shock, acute heart failure, bradyarrhythmias). Selected examples are:
- Dobutamine
- Isoproterenol (β1 and β2)
- Xamoterol
- epinephrine (non-selective)
β2 agonists
Main article: Beta2-adrenergic agonist
β2 agonists: stimulates adenylyl cyclase activity; closing of calcium channel (smooth muscle relaxants; used to treat asthma and COPD). Selected examples are:
- salbutamol (albuterol in USA)
- Levosalbutamol (Levalbuterol in USA)
- Fenoterol
- Formoterol
- Isoproterenol (β1 and β2)
- Metaproterenol
- Salmeterol
- Terbutaline
- Clenbuterol
- Isoetarine
- pirbuterol
- procaterol
- ritodrine
- epinephrine (non-selective)
Undetermined/unsorted
The following agents are also listed as agonists by MeSH.[10]
- arbutamine
- befunolol
- bromoacetylalprenololmenthane
- broxaterol
- cimaterol
- cirazoline
- denopamine
- dopexamine
- etilefrine
- hexoprenaline
- higenamine
- isoxsuprine
- mabuterol
- methoxyphenamine
- nylidrin
- oxyfedrine
- prenalterol
- ractopamine
- reproterol
- rimiterol
- tretoquinol
- tulobuterol
- zilpaterol
- zinterol
See also
References
- ^ "WHAT ARE BETA-AGONISTS?". Thoracic.org. American Thoracic Society. Retrieved 17 October 2014.
- ^ Adrenergic beta-Agonists at the US National Library of Medicine Medical Subject Headings (MeSH)
- ^ Delbruck, Max. "The beta-adrenergic receptors".
- ^ Yoo, B. et al. "Beta1-adrenergic receptors stimulate cardiac contractility and CaMKII activation in vivo and enhance cardiac dysfunction following myocardial infarction".
- ^ Johnson, M. "Molecular mechanisms of beta(2)-adrenergic receptor function, response, and regulation".
- ^ Lowell, B.B.; Flier, J.S. (1997). "Brown adipose tissue, beta 3-adrenergic receptors, and obesity". Annu. Rev. Med. 48. pp. 307–16.
- ^ http://news.yahoo.com/exclusive-fda-says-working-merck-usda-cattle-drug-160545615.html
- ^ Pias, M.T. "The Pharmacology of Adrenergic Receptors".
- ^ 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.
- ^ MeSH list of agents 82000318
Neuromodulation
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Types |
- ♦ Enzyme: Inducer
- Inhibitor
- ♦ Ion channel: Opener
- Blocker
- ♦ Receptor: Agonist
- Antagonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
- Inverse agonist
- ♦ Transporter [Reuptake]: Enhancer (RE)
- Inhibitor (RI)
- Releaser (RA)
- ♦ Miscellaneous: Precursor
- Cofactor
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Classes |
Enzyme
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see Enzyme inhibition
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Ion channel
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- Calcium channel blocker (CCB)
- Potassium channel blocker (PCB)
- Sodium channel blocker (SCB)
- Potassium channel opener (PCO)
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Receptor &
transporter
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BA/M
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Adrenergic
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- Adrenergic receptor agonist (α
- β (1
- 2))
- Adrenergic receptor antagonist (α (1
- 2), β)
- Adrenergic reuptake inhibitor (ARI)
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Dopaminergic
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- Dopamine receptor agonist
- Dopamine receptor antagonist
- Dopamine reuptake inhibitor (DRI)
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Histaminergic
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- Histamine receptor agonist
- Histamine receptor antagonist (H1
- H2
- H3)
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Serotonergic
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- Serotonin receptor agonist
- Serotonin Receptor Antagonist (5-HT3)
- Serotonin reuptake inhibitor (SRI)
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AA
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GABAergic
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- GABA receptor agonist
- GABA receptor antagonist
- GABA reuptake inhibitor (GRI)
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Glutamatergic
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- Glutamate receptor agonist (AMPA)
- Glutamate receptor antagonist (NMDA)
- Glutamate reuptake inhibitor
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Cholinergic
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- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
- Acetylcholine receptor antagonist (Muscarinic
- Nicotinic (Ganglionic
- Muscular))
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Endocannabinoid
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- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
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Opioidergic
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- Opioid modulator
- Opioid receptor agonist
- Opioid receptor antagonist
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Other
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- Adenosine reuptake inhibitor (AdoRI)
- Angiotensin II receptor antagonist
- Endothelin receptor antagonist
- NK1 receptor antagonist
- Vasopressin receptor antagonist
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Miscellaneous
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- Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
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Adrenergics
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Receptor ligands
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α1 |
- Agonists
- 6-FNE
- Amidephrine
- Anisodamine
- Anisodine
- Buspirone
- Cirazoline
- Corbadrine
- Dipivefrine
- Dopamine
- Ephedrine
- Epinephrine
- Etilefrine
- Ethylnorepinephrine
- Indanidine
- Metaraminol
- Methoxamine
- Methyldopa
- Midodrine
- Naphazoline
- Norepinephrine
- Octopamine
- Oxymetazoline
- Phenylephrine
- Phenylpropanolamine
- Pseudoephedrine
- Synephrine
- Tetrahydrozoline
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- Antagonists
- Abanoquil
- Adimolol
- Ajmalicine
- Alfuzosin
- Amosulalol
- Arotinolol
- Atiprosin
- Atypical antipsychotics (e.g., 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
- Nefazodone
- Neldazosin
- Niaprazine
- Nicergoline
- Niguldipine
- Pardoprunox
- Pelanserin
- Phendioxan
- Phenoxybenzamine
- Phentolamine
- Piperoxan
- Prazosin
- Quinazosin
- Ritanserin
- Silodosin
- Spiperone
- Talipexole
- Tamsulosin
- Terazosin
- Tiodazosin
- Tolazoline
- Trazodone
- 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
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α2 |
- Agonists
- (R)-3-Nitrobiphenyline
- 4-NEMD
- 6-FNE
- Amitraz
- Apraclonidine
- Brimonidine
- Cannabivarin
- Clonidine
- Corbadrine
- Detomidine
- Dexmedetomidine
- Dihydroergotamine
- Dipivefrine
- Dopamine
- Ephedrine
- Ergotamine
- Epinephrine
- Etilefrine
- Ethylnorepinephrine
- Guanabenz
- Guanfacine
- Guanoxabenz
- Lofexidine
- Medetomidine
- Methamphetamine
- Methyldopa
- Mivazerol
- Naphazoline
- Norepinephrine
- Oxymetazoline
- Phenylpropanolamine
- Piperoxan
- Pseudoephedrine
- Rilmenidine
- Romifidine
- Talipexole
- Tetrahydrozoline
- Tizanidine
- Tolonidine
- Urapidil
- Xylazine
- Xylometazoline
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- Antagonists
- 1-PP
- Adimolol
- Aptazapine
- Atipamezole
- Atypical antipsychotics (e.g., asenapine, clozapine, lurasidone, paliperidone, quetiapine, risperidone, zotepine)
- Azapirones (e.g., buspirone, 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
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β |
- Agonists
- Amibegron
- Arbutamine
- Arformoterol
- Arotinolol
- BAAM
- Bambuterol
- Befunolol
- Bitolterol
- Broxaterol
- Buphenine
- Carbuterol
- Cimaterol
- Clenbuterol
- Corbadrine
- Denopamine
- Dipivefrine
- Dobutamine
- Dopamine
- Dopexamine
- Ephedrine
- Epinephrine
- Etafedrine
- Etilefrine
- Ethylnorepinephrine
- Fenoterol
- Formoterol
- Hexoprenaline
- Higenamine
- Indacaterol
- Isoetarine
- Isoprenaline
- Isoxsuprine
- Levosalbutamol
- Mabuterol
- Methoxyphenamine
- Methyldopa
- Mirabegron
- Norepinephrine
- Orciprenaline
- Oxyfedrine
- Phenylpropanolamine
- Pirbuterol
- Prenalterol
- Ractopamine
- Procaterol
- Pseudoephedrine
- Reproterol
- Rimiterol
- Ritodrine
- Salbutamol
- Salmeterol
- Solabegron
- Terbutaline
- Tretoquinol
- Tulobuterol
- Vilanterol
- Xamoterol
- Zilpaterol
- Zinterol
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- 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
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Reuptake inhibitors
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NET |
- Selective norepinephrine reuptake inhibitors
- Amedalin
- Atomoxetine (tomoxetine)
- Ciclazindol
- Daledalin
- Edivoxetine
- Esreboxetine
- Lortalamine
- Mazindol
- Nisoxetine
- Reboxetine
- Talopram
- Talsupram
- Tandamine
- Viloxazine
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- Norepinephrine-dopamine reuptake inhibitors
- Amineptine
- Bupropion
- Fencamine
- Fencamfamine
- Hydroxybupropion
- Lefetamine
- Levophacetoperane
- LR-5182
- Manifaxine
- Methylphenidate
- Nomifensine
- O-2172
- Radafaxine
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- Serotonin-norepinephrine reuptake inhibitors
- Bicifadine
- Desvenlafaxine
- Duloxetine
- Eclanamine
- Levomilnacipran
- Milnacipran
- N-Methyl-PPPA
- PPPA
- Sibutramine
- Venlafaxine
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- Serotonin-norepinephrine-dopamine reuptake inhibitors
- Brasofensine
- Dasotraline
- Desmethylsertraline
- Diclofensine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- HDMP-28
- JNJ-7925476
- JZ-IV-10
- Liafensine
- Naphyrone
- NS-2359
- Perafensine
- PRC200
- Tesofensine
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- Tricyclic antidepressants
- Amitriptyline
- Butriptyline
- Cianopramine
- Clomipramine
- Desipramine
- Dosulepin
- Doxepin
- Imipramine
- Lofepramine
- Melitracen
- Nortriptyline
- Protriptyline
- Trimipramine
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- Tetracyclic antidepressants
- Amoxapine
- Maprotiline
- Mianserin
- Oxaprotiline
- Setiptiline
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- Others
- Antihistamines (e.g., brompheniramine, chlorphenamine, pheniramine, tripelennamine)
- Arylcyclohexylamines (e.g., ketamine, phencyclidine)
- CP-39,332
- Ethanol
- EXP-561
- Fezolamine
- Ginkgo biloba
- Indeloxazine
- Loxapine
- Nefazodone
- Nefopam
- Opioids (e.g., methadone, pethidine (meperidine), tapentadol, tramadol)
- Pridefine
- Tedatioxetine
- Teniloxazine
- Tofenacin
- Tropanes (e.g., cocaine)
- Ziprasidone
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VMATs |
- Amiodarone
- Amphetamines (e.g., amphetamine, methamphetamine, MDMA)
- Bietaserpine
- Deserpidine
- Efavirenz
- GBR-12935
- Ibogaine
- Ketanserin
- Lobeline
- Reserpine
- Rose bengal
- Tetrabenazine
- Vanoxerine (GBR-12909)
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Releasing agents
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- Morpholines
- Fenbutrazate
- Fenmetramide
- Morazone
- Morforex
- Phendimetrazine
- Phenmetrazine
- Pseudophenmetrazine
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- Oxazolines
- 4-MAR
- Aminorex
- Clominorex
- Cyclazodone
- Fenozolone
- Fluminorex
- Pemoline
- Thozalinone
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- Phenethylamines (also amphetamines, cathinones, etc)
- 2-OH-PEA
- 4-CAB
- 4-FA
- 4-FMA
- 4-MA
- 4-MMA
- Alfetamine
- Amfecloral
- Amfepentorex
- Amfepramone
- Amphetamine
- Dextroamphetamine
- Levoamphetamine
- Amphetaminil
- β-Me-PEA
- BDB
- Benzphetamine
- BOH
- Buphedrone
- Bupropion
- Butylone
- Cathine
- Cathinone
- Clobenzorex
- Clortermine
- Dimethylamphetamine
- DMA
- DMMA
- EBDB
- Ephedrine
- Ethcathinone
- Ethylone
- Etilamfetamine
- Famprofazone
- Fenethylline
- Fenproporex
- Flephedrone
- Fludorex
- Furfenorex
- Hordenine
- 4-Hydroxyamphetamine
- 5-APDI (IAP)
- 5-MAPDI (IMP)
- Iofetamine (123I)
- Lisdexamfetamine
- Lophophine
- MBDB
- MDA
- MDEA
- MDMA
- Metamfepramone
- MDMPEA
- MDOH
- MDPEA
- Mefenorex
- Mephedrone
- Mephentermine
- Methamphetamine
- Dextromethamphetamine
- Levomethamphetamine
- Methcathinone
- Methedrone
- Methylone
- Morforex
- Naphthylaminopropane
- Ortetamine
- pBA
- pCA
- Pentorex
- Phenethylamine
- Pholedrine
- Phenpromethamine
- Phentermine
- Phenylpropanolamine
- pIA
- Prenylamine
- Propylamphetamine
- Pseudoephedrine
- Selegiline (also D-Deprenyl)
- Tiflorex
- Tyramine
- Xylopropamine
- Zylofuramine
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- Piperazines
- 2C-B-BZP
- BZP
- MBZP
- mCPP
- MDBZP
- MeOPP
- pFPP
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- Others
- 2-ADN
- 2-AI
- 2-AT
- 2-BP
- 4-BP
- 5-IAI
- Clofenciclan
- Cyclopentamine
- Cypenamine
- Cyprodenate
- Feprosidnine
- Gilutensin
- Heptaminol
- Hexacyclonate
- Indanorex
- Isometheptene
- Methylhexanamine
- Octodrine
- Phthalimidopropiophenone
- Propylhexedrine (Levopropylhexedrine)
- Tuaminoheptane
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Enzyme inhibitors
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PAH |
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TH |
- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
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AAAD |
- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
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DBH |
- Bupicomide
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Phenopicolinic acid
- Tropolone
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PNMT |
- CGS-19281A
- SKF-64139
- SKF-7698
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MAO |
- Nonselective
- Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine
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- MAO-A selective
- Amiflamine
- Bazinaprine
- Befloxatone
- Brofaromine
- Cimoxatone
- Clorgiline
- CX157 (Tyrima)
- Eprobemide
- Esuprone
- Harmala alkaloids
- Harmine
- Harmaline
- Tetrahydroharmine
- Harman
- Methylene blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
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- MAO-B selective
- Ladostigil
- Lazabemide
- Milacemide
- Mofegiline
- Pargyline
- Rasagiline
- Safinamide
- Selegiline (also D-Deprenyl)
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COMT |
- Entacapone
- Nitecapone
- Tolcapone
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Others
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Precursors |
- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine
- L-DOPS (Droxidopa)
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Cofactors |
- Ferrous Iron (Fe2+)
- S-Adenosyl-L-Methionine
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal Phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
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Neurotoxins |
- DSP-4
- Oxidopamine (6-OHDA)
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Others |
- Activity enhancers
- BPAP
- PPAP
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- Release blockers
- Bethanidine
- Bretylium
- Guanadrel
- Guanazodine
- Guanethidine
- Guanoxan
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- See also:
- Dopaminergics
- Melatonergics
- Serotonergics
- List of adrenergic drugs
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