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TargetMol | Tags GPCR/G Protein
TargetMol | Tags Neuroscience

Adrenergic Receptor

The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, β2 agonists and α2 agonists, which are used to treat high blood pressure and asthma, for example.

CL 316243
T10830138908-40-4In house
CL316243 is a highly potent selective agonist of β3-adrenoceptor, with a EC50 of 3 nM. CL316243 is an effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence.
  • $48
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Ecastolol
T1114877695-52-4In house
Ecastolol has anti-angina activity and is an adrenergic receptor antagonist.
  • $388
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5-HT1A modulator 1
T10168142477-34-7In house
5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).
  • $263
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Delequamine
T68051119905-05-4In house
Delequamine (RS 15385-197) is a selective and potent TNIK inhibitor (IC50: 8 nM).TINK-IN-1 inhibits colorectal cancer cell viability and can be used to study mental retardation.
  • $258
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Oxyfedrine L-form HCl
T2457916777-42-7In house
Oxyfedrine L-form HCl (Ildamen) is a partial agonist at beta-adrenergic receptors and acts as a coronary vasodilator and cardiotonic agent.
  • $98
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(4E)-SUN9221
T12596222318-55-0
(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist, exhibiting antihypertensive and antiplatelet aggregation activities in hypertensive rats.
  • $700
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LY377604
T15819204592-94-9In house
LY377604 is a human β3-adrenergic receptor agonist (EC50: 2.4 nM) and β1/2-adrenergic receptor antagonist for the study of obesity.
  • $127
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TargetMol
PF-610355
T16509862541-45-5In house
PF-610355 is a long-acting and potent β2-adrenergic receptor agonist (EC50: 0.26 nM).PF-610355 can be used to study asthma and COPD.
  • $633
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Aplindore Fumarate
T30098189681-71-8In house
Aplindore Fumarate (DAB-452) is a small molecule dopamine D2 receptor partial agonist.Aplindore Fumarate exhibits high affinity for dopamine D2 and D3 receptors, and low affinity for dopamine D4, 5-hydroxytryptophan (5-HT2), and α1-adrenergic receptors.Aplindore Fumarate is used in the study of Parkinson's disease and schizophrenia. Fumarate can be used to study Parkinson's and schizophrenia.
  • $293
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Bedoradrine sulfate
T26760194785-31-4In house
Bedoradrine sulfate (MN-221 sulfate) is a novel, highly selective β2-adrenoceptor agonist for the treatment of asthma and chronic obstructive pulmonary disease.
  • $762
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Bedoradrine
T70047194785-19-8In house
Bedoradrine (MN-221) free base is a novel, highly selective β2-adrenoceptor agonist for the treatment of asthma and chronic obstructive pulmonary disease.
  • $762
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Reboxetine mesylate
T696398769-84-7
Reboxetine mesylate (FCE20124 mesylate) is a norepinephrine reuptake inhibitor with a Ki of 8.2 nM.
  • $35
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PF-4348235 HCl
T72226L In house
PF-4348235 HCl (β2AR M-receptor agonist-2 HCl) is a muscarinic M3 receptor antagonist (Ki: 0.73 nM) and β2 adrenergic receptor agonist (MABA, EC50: 3.7 nM). PF-4348235 HCl is also a bronchial BM213 acetate is a bronchodilator used to study cardiovascular and respiratory diseases such as chronic obstructive pulmonary disease (COPD).
  • $195
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BODIPY FL prazosin
T63980175799-93-6In house
BODIPY FL prazosin is a fluorescent α1-adrenergic antagonist with binding affinities of Ki: 14.5 nM for α1a-AR and Ki: 43.3 nM for α1b-AR, used to study subcellular localization differences in α1-adrenoceptor subtypes.
  • $293 TargetMol
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Faxeladol
T31750433265-65-7In house
Faxeladol, a potent adrenergic absorption inhibitor and serotonin reuptake inhibitor, is a small-molecule Opioid receptor agonist that can be used to study neurological disorders.
  • $628
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Fipamezole
T24064150586-58-6In house
Fipamezole is a potent alpha2 adrenergic receptor antagonist that may be useful for studying autonomic dysfunction in Parkinson's disease.
  • $628
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(S)-(+)-Niguldipine hydrochloride
T23301113145-69-0In house
(S)-(+)-Niguldipine hydrochloride is a selective α1A-AR antagonist used in the study of depression and epilepsy.
  • $75 TargetMol
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Trifluoperazine
T8389117-89-5
Trifluoperazine (trifluoroperazine) is a Dopamine D2 receptor inhibitor(IC50 : 1.2 nM), and Treatment of schizophrenia.
  • $41
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TargetMol | Citations Cited
Dexmedetomidine hydrochloride
T6466145108-58-3
Dexmedetomidine hydrochloride (Precedex) is a potent, selective, orally active α2-adrenoceptor agonist with a Ki value of 1.08 nM. It shows 1620-fold selectivity over α1-adrenoceptors. Dexmedetomidine hydrochloride (Precedex) can protect against sepsis-induced acute lung injury through anti-inflammatory, anti-oxidative, and anti-apoptotic effects.
  • $35
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Escitalopram
T0185128196-01-0
Escitalopram (Seroplex) is a furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.
  • $40
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TargetMol | Citations Cited
ZK-90055 hydrochloride
T1340384638-81-3In house
ZK-90055 hydrochloride, a β2 adrenergic receptor agonist, is employed in the study of asthma.
  • $350
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Salmeterol
T1282989365-50-4
Salmeterol (GR33343X) is a long-acting agonist of beta2-adrenergic receptor (beta 2AR) used for treatment ofasthma.
  • $50
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Isoprenaline hydrochloride
T105651-30-9
Isoprenaline hydrochloride (NCI-c55630) is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.
  • $33
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TargetMol | Citations Cited
Bucumolol
T30606L58409-59-9
Bucumolol (Bucumarol) is a β-adrenergic blocking agent and a local anesthetic with antihypertensive activity and can be used to study myocardial infarction.
  • $195
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AVN-101
T266901061354-48-0
AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.
  • $30
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Deriglidole
T10998122830-14-2In house
Deriglidole (SL 86-0715) is a peripheral adrenergic receptor antagonist that is a selective inhibitor of alpha2 receptors. Deriglidole inhibits colistin and Idazoxan but does not show activity against prazosin and rat cortical and human platelet α2-adrenergic receptors.
  • $460
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Cyclazosin HCl
T70585146929-33-1In house
Cyclazosin HCl is a subtype-selective α-adrenergic receptor antagonist that competitively antagonizes norepinephrine-induced α(1B)-adrenergic receptor contraction and can be used to study non-arteritic ischemic optic neuropathy and other neurological diseases.
  • $293
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Taprizosin
T28922210538-44-6In house
Taprizosin(UK-338003) is a selective and orally active α1-adrenoceptor antagonist for vasodilatation in the treatment of benign prostatic hyperplasia.
  • $373
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Risperidone
T0351106266-06-2
Risperidone (R 64 766) is a selective blocker of dopamine D2 receptors and serotonin 5-HT2 receptors that act as an atypical antipsychotic agent.
  • $43
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TargetMol | Citations Cited
Labetalol
T2057036894-69-6
Labetalol (Apo-Labetalol) is a mixed alpha beta-adrenergic antagonist.It is used to treat high blood pressure. It can be given by mouth for long term hypertension management or intravenously in severe hypertensive situations. The pharmacokinetics of labetalol is affected by the common CYP2C19 polymorphisms.
  • $35
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Penbutolol sulfate
T1240238363-32-5In house
Penbutolol sulfate ((-)-Terbuclomine) binds to both β2-adrenergic and β1-adrenergic receptors, making it a non-selective β-blocker.
  • $35
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Mapenterol hydrochloride
T4062254238-51-6
Mapenterol hydrochloride is an agonist of β2-adrenergic receptor.
  • $44
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Falintolol
T6840290581-63-8In house
Falintolol is a novel beta-adrenergic antagonist with antihypertensive effects and can be used to study glaucoma.
  • $293
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Bisaramil hydrochloride
T2682296480-44-3In house
Bisaramil hydrochloride (Bisaramil) is a novel diazabicyclononane antiarrhythmic compound that inhibits the generation of free radicals.Bisaramil hydrochloride blocks sodium currents and inhibits the slow Ca(2+) action potential induced by isoproterenol in K(+)-depolarized muscle.
  • $293 TargetMol
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SM-2470
T6289399899-45-3In house
SM-2470 is an α1-adrenoceptor antagonist with antihypertensive activity that decreases anterior ganglionic adrenal nerve activity and aortic descending nerve activity.SM-2470 has hypocholesterolemic activity and inhibits cholesterol absorption.
  • $462 TargetMol
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Monatepil maleate
T25828103379-03-9In house
Monatepil maleate (AJ-2615 maleate) is an orally active Ca2+-channel and α1-adrenoceptor antagonist and non-competitive heparanoyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with antihypertensive activity.Monatepil maleate is used in studies of hyperlipidemia and atherosclerosis. Monatepil maleate is used to study hyperlipidemia and atherosclerosis.
  • $293
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Brexpiprazole
T2306913611-97-9
Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors.
  • $45
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Napitane
T26363L148152-63-0In house
napitane (A 75200) is a novel catecholamine uptake inhibitor with inhibitory effects on α-adrenergic receptors and potential antidepressant activity for the study of depression.
  • $329
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OPC-28326
T13804167626-17-7In house
OPC-28326 is a specific an α2-adrenergic receptor antagonist and acts as a peripheral vasodilator. OPC-28326 inhibits α2A-, α2B- and α2C-adrenoceptors with Ki of 2040, 285, and 55 nM, respectively.
  • $197
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Taxifolin
T1738480-18-2
Taxifolin (Dihydroquercetin) is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.
  • $30
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TargetMol | Citations Cited
CGP 20712 A
T10778105737-62-0In house
CGP 20712 A (CGP 20712 mesylate) is a selective and potent β1-adrenergic receptor antagonist (IC50: 0.7 nM) with antihypertensive activity, capable of reversing RKT-induced gastric relaxation.
  • $98
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Xamoterol hemifumarate
T2353673210-73-8
Xamoterol hemifumarate is a potent and selective β1-adrenoceptor agonist.Xamoterol hemifumarate is a potential compound for the study of the relationship between cardiac arrhythmias and β1-adrenergic stimulation with IKr.
  • $42
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Esprolol
T27286L396654-09-4In house
Esprolol (ACC-9369 free base) is a novel β-adrenergic receptor antagonist for the study of exertional angina.
  • $129 TargetMol
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Pipoxazole
T2841991595-86-7In house
Pipoxazole (COR-32-24) is an adrenergic receptor agonist that can be used to study depression.
  • $293 TargetMol
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T-0509
T2889596843-99-1In house
T-0509 is a selective beta 1 receptor agonist that increases inotropy in canine ventricular muscle and selectively down-regulates rat cardiac beta 1-adrenoceptors.
  • $350
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(±)-Prenalterol
T2598457526-81-5In house
(±)-Prenalterol (H 80 62) is a new cardioselective positive inotropic compound that is an agonist of beta-2- and beta-1-adrenergic receptors and can be used to study chronic congestive heart failure.
  • $228 TargetMol
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Pimozide
T25462062-78-4
Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors.
  • $31
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TargetMol | Citations Cited
(S)-(-)-Propranolol hydrochloride
T233024199-10-4
(S)-(-)-Propranolol hydrochloride, an adrenergic receptor antagonist, exhibits potential anticancer activity and may enhance the prognosis of burn patients.
  • $33
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