Talibegron hydrochloride (ZD2079 hydrochloride) is a potent β3-adrenoceptor agonist with a pD2 of 3.72 on phenylephrine-preconstricted rat mesenteric artery. Talibegron hydrochloride has potent vasorelaxant effect[1].
Dicentrine is a natural product isolated from the plant Lindera megaphylla with antihypertensive effect. Dicentrine is an α1-adrenoceptor antagonist which has effective against human hyperplastic prostates[1].
BRL 37344 sodium (BRL 37344A) is a specific β3-adrenergic receptor agonist. BRL 37344 sodium treatment significantly lowers the body weight of obese mice[1].
Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities[1][2][3][4][5].
Terazosin hydrochloride is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment[1][2][3].
Bunitrolol is a beta-adrenergic antagonist. Bunitrolol has intrinsic sympathomimetic activity. Bunitrolol can be used for the research of ischemic myocardium[1].
Dobutamine tartrate is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine tartrate is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine tartrate can increase cardiac output and correct hypoperfusion[1][2][3][4].
Scopine Hcl salt is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.
β2AR agonist /M-receptor antagonist-1 is a potent dual muscarinic antagonist/beta 2 agonist (MABA). β2AR agonist /M-receptor antagonist-1 potently relaxes either Carbachol (HY-B1208)-induced contraction, in the absence (MABA) or presence of Propranolol (M3; HY-B1208), or Histamine (HY-B1204)-induced contraction (β2)[1][2].
Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol. IC50 Value:Target: β2-adrenergic receptorLevosalbutamol and salbutamol produced significantly better bronchodilator responses than placebo. Both the drugs showed equivalent time-dependent bronchodilator responses as measured by area under curve for percent change in FEV(1) and FVC over 6h. The time to onset of action, mean maximum bronchodilator response and duration of bronchodilator response were similar between levosalbutamol and salbutamol [1].
Zenidolol (ICI-118551) is a selective β2 adrenergic receptor antagonist. Zenidolol inhibits β2-, β1- and β3-adrenergic receptor with Ki values of 0.7, 49.5 and 611 nM, respectively. Zenidolol can be used as an ocular hypotensive agent used for ophthalmic disease research[1].
Zinterol hydrochloride (MJ 9184 hydrochloride) is a potent and selective β2-adrenoceptor agonist[1]. Zinterol hydrochloride increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM[2]. Zinterol hydrochloride induces ventricular arrhythmias in conscious heart failure rabbits[3].
Metoprolol fumarate (CGP 2175C) is an orally active, selective β1-adrenoceptor antagonist. Metoprolol fumarate shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3].
Methyldopate hydrochloride is an ethyl ester hydrochloride prodrug of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate hydrochloride has the potential for severe hypertension research[1].
Mabuterol is a selective and orally active beta-2 adrenergic receptor (ADRB2) agonist. Mabuterol inhibits the proliferation and suppresses the increase of intracellular Ca2+ induced by PDGF-BB. Mabuterol suppresses the protein expressions of Drp-1, cyclinD1 and PCNA and enhanced the expression of Mfn-2 induced by PDGF-BB[1][2].
Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor[1][2][3].
Synephrine (Oxedrine) hemitartrate, an alkaloid, is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium. Synephrine hemitartrate is a sympathomimetic compound and can be used for weight loss[1][2].
Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
Epiberberine chloride, a natural alkaloid, is a BACE1 inhibitor, which also exhibits inhibition activity on CYP2D6 and aldose reductase, alpha-adrenoceptors, acetylcholinesterase (AChE), butyrylcholinesterase, and b-site amyloid precursor protein cleaving enzyme 1.
Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy[1][2][3].
Fenmetozole Tosylate is an antagonist of the actions of ethanol, also antagonizes α2-adrenergic receptor, and acts as an antidepressant drug.
(±)-Befunolol is a β-adrenoceptor blocking agent.
Lidamidine hydrochloride (WHR-1142A) is an α2-adrenergic receptor agonist and antidiarrheal agent[1].
Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
Bamosiran is a small interfering RNA targeting β-adrenergic receptor 2, and is used to lower intraocular pressure
(S)-Alprenolol is a potent and nonselective β-blocker[1].
Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate is a prodrug of pindolol and can be used for essential and renovascular hypertension research[1][2].
Trimazosin is an orally active, quinazoline derivative which is structurally related to prazosin. Trimazosin shows hypotensive effect by selectively block α1-adrenoceptors[1][2].
2-MPMDQ is a potent and selective α1-adrenoceptor (Ki=0.37 nM) antagonist over α2-adrenoceptor (Ki=1740 nM). 2-MPMDQ is potent anti-hypertensive agent and has the potential for hypertension research[1].
Dopexamine hydrochloride is a β2 adrenergic receptor agonist.