Adrenergic Receptor

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.

Ecastolol has anti-angina activity and is an adrenergic receptor antagonist.

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).

Oxyfedrine L-form HCl (Ildamen) is a partial agonist at beta-adrenergic receptors and acts as a coronary vasodilator and cardiotonic agent.

Cicloprolol hydrochloride is a new potent and selective beta 1-adrenoceptor antagonist with partial agonist activity for the study of coronary heart disease.

(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist, exhibiting antihypertensive and antiplatelet aggregation activities in hypertensive rats.

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.

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.

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.

LY377604 is a human β3-adrenergic receptor agonist (EC50: 2.4 nM) and β1 2-adrenergic receptor antagonist for the study of obesity.

Norepinephrine (Levophed) can stimulate apoptosis in adult rat ventricular myocytes by activation of the β-adrenergic pathway. It can up-regulate the expression of vascular endothelial growth factor, matrix metalloproteinase (MMP)-2, and MMP-9 in nasopharyngeal carcinoma tumour cells.

(S)-(+)-Niguldipine hydrochloride is a selective α1A-AR antagonist used in the study of depression and epilepsy.

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).

Reboxetine mesylate (FCE20124 mesylate) is a norepinephrine reuptake inhibitor with a Ki of 8.2 nM.

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.

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.

Fipamezole is a potent alpha2 adrenergic receptor antagonist that may be useful for studying autonomic dysfunction in Parkinson's disease.

Trifluoperazine (trifluoroperazine) is a Dopamine D2 receptor inhibitor(IC50 : 1.2 nM), and Treatment of schizophrenia.

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.

Salmeterol (GR33343X) is a long-acting agonist of beta2-adrenergic receptor (beta 2AR) used for treatment ofasthma.

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.

Bucumolol (Bucumarol) is a β-adrenergic blocking agent and a local anesthetic with antihypertensive activity and can be used to study myocardial infarction.

Isoprenaline hydrochloride (NCI-c55630) is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.

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.

(3aR,9aR)-Fluparoxan is a highly selective and potent adrenergic receptor α2B antagonist for the prevention, amelioration or treatment of neurodevelopmental disorders and neurodegenerative diseases.

TD-5471 hydrochloride is a selective and potent long-acting human β2-adrenergic receptor agonist for the treatment of chronic obstructive pulmonary disease (COPD).

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.

Taprizosin(UK-338003) is a selective and orally active α1-adrenoceptor antagonist for vasodilatation in the treatment of benign prostatic hyperplasia.

Anisodamine Hydrobromide (6-Hydroxyhyoscyamine) is an anticholinergic and α1-adrenergic receptor antagonist used in the treatment of acute circulatory shock.

Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors.

ORM-10921 is an α2C-adrenoceptor antagonist that has shown antipsychotic and antidepressant activity in animal studies.

YS-49 is an activator of PI3K Akt (a downstream target of RhoA).

Penbutolol sulfate ((-)-Terbuclomine) binds to both β2-adrenergic and β1-adrenergic receptors, making it a non-selective β-blocker.

Mapenterol hydrochloride is an agonist of β2-adrenergic receptor.

Falintolol is a novel beta-adrenergic antagonist with antihypertensive effects and can be used to study glaucoma.

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.

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.

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.

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.

Taxifolin (Dihydroquercetin) is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.

ICI 118,551 hydrochloride (ICI 118551 hydrochloride) is a highly selective β2 adrenergic receptor antagonist (Kis: 0.7, 49.5, and 611 nM for β2, β1, and β3 receptors).

Esprolol (ACC-9369 free base) is a novel β-adrenergic receptor antagonist for the study of exertional angina.

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.

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.

(±)-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.

SR59230A is a potent, selective antagonist of β3-adrenergic receptor(β3, β1, and β2 receptors with IC50s of 40, 408, and 648 nM , respectively).

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.

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.