adrenergic

Prazosin hydrochloride (Vasoflex) reduces peripheral resistance and relaxes vascular smooth muscles as a selective adrenergic alpha-1 antagonist by a mechanism not completely known. Prazosin hydrochloride is a synthetic piperazine derivative with hypotensive antiadrenergic properties, It is used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud's syndrome, prostatic hypertrophy, and urinary retention.

Phentolamine mesylate (Phentolamine methanesulfonate) is a nonselective alpha-adrenergic antagonist used to treat hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of [RAYNAUD DISEASE] and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.

Dibenamine hydrochloride is a competitive and irreversible blocker of the β-adrenergic receptor.

Metaraminol tartrate (Metaradrine tartrate) is a sympathomimetic agent that acts predominantly at alpha-1 adrenergic receptors. It has been used primarily as a vasoconstrictor in the treatment of HYPOTENSION.

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

Iobenguane sulfate (MIBG sulfate) is a high-affinity substrate for cholera toxin that disrupts cellular mono(ADP-ribosylation). Radioiodinated Iobenguane sulfate is used clinically as a tumor-targeted radiopharmaceutical for diagnosing and treating adrenergic tumors.

β-Adrenergic-receptor kinase (EC 2.7.11.15) requires activation by G proteins, categorizing it within the G protein-dependent receptor kinase (GRK) family. It specifically acts upon receptors in their agonist-bound state and can phosphorylate rhodopsin, albeit at a slower rate. It does not phosphorylate casein or histones.

5-HT1A modulator 1 is a small molecule modulator, a high-affinity multi-target ligand with potent inhibitory activity against 5-HT1A receptor (IC50=2 nM), α1-adrenergic receptor (IC50=10 nM), and dopamine D2 receptor (IC50=40 nM). This compound is primarily used for research on neuropsychiatric disorders such as anxiety, depression, or schizophrenia.

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 is a small molecule inhibitor, a β-adrenergic receptor antagonist that exerts its pharmacological effect by blocking catecholamine-induced agonism of this receptor, with anti-anginal properties, used for cardiovascular disease research.

Tamsulosin hydrochloride (Flomax hydrochloride) is the hydrochloride salt of tamsulosin, a sulfonamide derivative with α1 adrenergic antagonist activity.

AR-08 is a potent α2-adrenergic receptor agonist for the study of ADHD and attention deficit.

QF0301B is a potent α1-adrenergic receptor antagonist with inhibitory effects on α2-adrenergic receptors, 5-HT2A and histamine H1 receptors.

Arbutamine (GP 21213) is a novel potent non-selective beta-adrenoceptor agonist with alpha-1-sympathomimetic activity.Arbutamine promotes cardiac stress and increases heart rate, cardiac contractility.Arbutamine can be used to study cardiac stress and coronary artery disease

Bucindolol Formatel is a blocker of β1-adrenergic receptor. Bucindolol exhibits intrinsic sympathomimetic activity. Bucindolol can be used in the research of heart failure.

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.

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

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.

Midaglizole hydrochloride ((±)-DG5128) (DG5128) is a preferred α2-adrenoceptor antagonist. Midazolazole hydrochloride (DG5128) has an affinity for α2-adrenoceptor (pKi = 6.28) 7.4 times higher than that of α1-adrenoceptor.

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.

Indanidine is a highly selective and potent α-adrenergic agonist with antihypertensive activity.Indanidine is an α-adrenergic antagonist that can be used in the study of neurological disorders.

Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively.

MG 1 is a potent alpha-1 adrenergic receptor antagonist.

Benzquinamide (P2647), an antiemetic agent with anticancer activity, inhibits p-glycoprotein-mediated drug efflux and potentiates the cytotoxicity of anticancer drugs in multidrug-resistant cells.The Ki values of Benzquinamide for α2A, α2B, and α2C adrenergic receptor (α2-AR) were 1,365, 691, and 545 nM, respectively. 545 nM, respectively.