Levalbuterol ((R)-Albuterol) hydrochloride is a short-acting β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. Levalbuterol hydrochloride is a more potent bronchodilator than Salbutamol and has the potential for the treatment of COPD[1].
ADRA1D receptor agonist 1 (compound (R)-9S) is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM[1].
Bufuralol hydrochloride (Ro 3-4787 hydrochloride) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate[1][2].
Bometolol Hydrochloride is a beta-adrenergic blocking agent, used for the research of cardiovascular disease.
Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure[1][4].
Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].
Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM. IC50 Value: 0.25-1.2 nM(Ki for adrenergic receptor); 0.03-4.0 nM(Ki for 5-HT receptor)Target: 5-HT Receptor; Adrenergic ReceptorAsenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic. Asenapine has a broad receptor affinity profile for most serotonergic, dopaminergic, and adrenergic receptors, with no appreciable affinity for muscarinic receptors. Asenapine may be a helpful treatment option for patients with schizophrenia when weight gain, dyslipidemia, and endocrine abnormalities are a concern.
Clonidine-d4 is the deuterium labeled Clonidine. Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent[1][2][3][4][5].
Mebeverine D6 Hydrochloride is the deuterium labeled Mebeverine, which is an antimuscarinic.
(Rac)-Nebivolol-d8 ((rac)-R 065824-d8) is a labelled racemic Nebivolol. Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM[1][2].
(Des-His6)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production[1].
Zilpaterol-d7 is a deuterium labeled Zilpaterol. Zilpaterol is a β-adrenergic receptor agonist that putatively, through activation of protein kinase A, increases protein synthesis in skeletal muscle fibers as well as reduces lipogenesis and increases lipolysis in adipose tissues. Formulations containing Zilpaterol have been used to increase lean body weight and improve feed efficiency in commercial beef cattle.
Corynanthine is a selective α1-adrenergic receptor antagonist. Corynanthine can significantly lower intraocular pressure in rabbits[1].
AR-08 is an agonist of α2-adrenergic receptor, used for the treatment of attention deficit hyperactivety disorder (ADHD).
BRL-44408 maleate is an α2A-adrenoceptor antagonist (Ki: 8.5 nM). BRL-44408 maleate has antidepressant and analgesic activity. BRL-44408 also improves cecal ligation puncture (CLP)-induced acute lung injury[1][2].
Mabuterol-D9 is a deuterium labeled Mabuterol. Mabuterol is an agonist of the β2-adrenergic receptor[1].
5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, with weak α1 adrenoceptor blocking activity.
Carvedilol(BM14190) is a non-selective beta blocker/alpha-1 blocker with an IC50 of 3.8 μM for inhibition of LDL oxidation.IC50 Value: 3.8 μM ( inhibition of LDL oxidation)Target: beta Adrenergic ReceptorCarvedilol is a nonselective-blocking agent and is used in the treatment of hypertension and angina pectoris. As a third-generation β-adrenergic blocker (β-blocker), Carvedilol is able to reverse cardiac structural remodeling. Recentresults demonstrated that the effect caused by Carvedilol on cardiac remodeling is largely dependent on endogenous NO.
Sotalol Hydrochloride is an adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.Target: Adrenergic ReceptorSotalol is a non-selective competitive β-adrenergic receptor blocker that also exhibits Class III antiarrhythmic properties by its inhibition of potassium channels. Sotalol is a competitive beta adrenoceptor antagonist devoid of membrane-stabilizing activity and intrinsic sympathomimetic activity that has no preferential actions on beta 1 or beta 2 responses. Sotalol causes concentration-dependent increases in the contractility of isolated ventricular tissue that is not blocked by previous beta or alpha blockade or catecholamine depletion. Sotalol consistently reduces the heart rate to a greater degree than propranolol and causes significantly less cardiac suppression than propranolol at a given heart rate [1]. Sotalol is not only a beta blocker but a class III antiarrhythmic drug. Its possible antifibrillatory activity was therefore investigated in both the ventricles and atria of dog heart in situ, since vulnerability to fibrillation is not the same in both these parts of the myocardium [2].
Metipranolol is a nonselective and orally active β-adrenergic receptor antagonist. Metipranolol can be used for hypertension and glaucoma research[1][2].
Carmoterol hydrochloride is a highly potent, selective and long-acting β2-adrenoceptor agonist with the pEC50 of 10.19. Carmoterol has 53 times higher affinity for the β2-adrenoceptors than for the β1-adrenoceptors. Carmoterol hydrochloride can be used for the research of asthma and chronic obstructive pulmonary disease (COPD)[1][2].
Medetomidine(Domtor) is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively). IC50 value:Target: α2-adrenoceptorMedetomidine displays greater selectivity over α1-adrenoceptors than clonidine and UK 14,304 (1620-, 220- and 300-fold respectively). Medetomidine inhibits twitch response in electrically stimulated mouse vas deferens (pD2 = 9.0). Active in vivo; displays hypotensive, bradycardic, sedative, anxiolytic, hypothermic and analgesic effects.
Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition[1][2][3].
Naphazoline HCl is an ocular vasoconstrictor and imidazoline derivative sympathomimetic amine.Target: Adrenergic Receptorphazoline hydrochloride is the common name for 2-(1-naphthylmethyl)-2-imidazoline hydrochloride. It is a sympathomimetic agent with marked alpha adrenergic activity. It is a vasoconstrictor with a rapid action in reducing swelling when applied to mucous membrane. It acts on alpha-receptors in the arterioles of the conjunctiva to produce constriction, resulting in decreased congestion. It is an active ingredient in several over-the-counter formulations including Clear Eyes and Naphcon eye drops. From Wikipedia.
Romifidine is an α2 adrenergic receptor agonist. Romifidine shows sedation effects in vivo[1][2].
Indanidine is an alpha-adrenergic agonist.
Pronethalol is a non-selective beta-adrenergic blocking agent, protect against and to reverse Digitalis-induced ventricular arrhythmias. Target: beta-adrenergic receptor
Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.Target: β1- adrenergic receptorNebivolol reduces cell proliferation of human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) in a concentration- and time-dependent maner. Nebivolol treatment for 7 days causes significant reduction in cell growth of haCSMCs with IC50 of 6.1 μM, and inhibits accelerated haCSMC proliferation stimulated by growth factors PDGF-BB, bFGF, and TGFβ with IC50 values of 6.8 μM, 6.4 μM and 7.7 μM, repectively. Nebivolol treatment (10-5 M) of haCSMCs for 48 hours induces a moderate apoptosis of 23% and a decrease from 16% to 5% in the number of cells in S-phase. During Nebivolol incubation, NO formation of HaCEs increases, while endothelin-1 transcription and secretion are suppressed.Administratiion of Nebivolol (initially by iv within 10 minutes of reperfusion and then orally) to rats with myocardial infarction (MI) reduces myocardial apoptosis, which is mediated by regulation of NO . Nebivolol, significantly, prevents left ventricular (LV) pressure changes, reduces total and regional apoptotic cardiomyocytes. Nebivolol treatment lowers mean blood pressure (MBP) in rats with MI slightly, but not significantly.
(S)-Alprenolol is a potent and nonselective β-adrenoceptor antagonist[1].
Anisodamine hydrochloride is an anticholinergic and α1 adrenergic receptor antagonist. Anisodamine hydrochloride can be used for improving blood flow in circulatory disorders such as septic shock, Anisodamine hydrochloride displays a spectrum of pharmacological effects similar to Atropine (HY-B1205) and Sopolamine (HY-B2065) including inhibition of salivation, gastrointestinal and sweat secretion, gastrointestinal motility, respiratory secretion and urinary bladder contraction in vivo[1].