β3-AR agonist 2 is a potent and selective β3-adrenergic receptor (β3-AR) agonist with an EC50 of 8 nM.
Alfuzosin-d7 is the deuterium labeled Alfuzosin[1]. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH)[2][3].
Zinterol (MJ 9184) is a potent and selective β2-adrenoceptor agonist[1]. Zinterol increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM[2].
Metipranolol is a non-selective β adrenergic receptor blocking agent.
ZK-90055 hydrochloride is a β2 adrenergic receptor agonist.
Cimaterol-D7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
(R,R)-Reboxetine mesylate is an antidepressant agent with great bioavailability. (R,R)-Reboxetine is the enantiomer of Reboxetine, which is a selective noradrenaline reuptake inhibitor. Reboxetine consists of (R,R) and (S,S) enantiomer, has low affinity for alpha-adrenergic and muscarinic receptors and low toxicity in animals[1][2].
Naphazoline (Naphthazoline) is a potent α-adrenergic receptor agonist. Naphazoline reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline can be used for non-bacterial conjunctivitis research[1][2].
Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research[1][2][3].
Indacaterol-d3 is deuterium labeled Indacaterol.
Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias, and limits the cerebral arteriovenous malformation (AVMs)[1][2].
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells [1][2][3].
Pamatolol is a cardioselective beta-adrenoceptor antagonist without sympathomimetic activity.
JP1302 dihydrochloride is a selective, high affinity antagonist of the alpha2C-adrenoceptor (α2C-adrenoceptor), with a Kb value (antagonist activity) of 16 nM and a Ki (binding affinity) value of 28 nM[1][2].
(±)-WB 4101 is a potent antagonist of noradrenaline. (±)-WB 4101 interacts with protein in smooth muscle. (±)-WB 4101 makes drug and receptor bind tightly[1].
Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH).Target: Alpha-1 Adrenergic ReceptorTerazosin is selective for alpha 1A-adrenoceptors which appear to dominate in the human prostate; the therapeutic relevance of this selectivity remains to be assessed in clinical studies [1]. Administration of terazosin 1 mg orally for 28 d. Terazosin initially shifted the dose-response curve of phenylephrine to the right, with a significant increase in ED50 for phenylephrine from a control value of 102 to 759 ng/min on day 1 of terazosin (P < 0.001). The mean Kd of terazosin was estimated as 11 +/- 15 nM in the first few days of treatment. This study demonstrates that pharmacological tolerance to the alpha 1-adrenoceptor blocking action of terazosin occurs in man and may be responsible for loss in efficacy with chronic therapy [2].
Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension[1][2].
Guanoxabenz is an α2 adrenergic receptor agonist.
Metoprolol is a cardioselective β1-adrenergic blocking agent.Target: β1- adrenergic ReceptorPatients took 50 mg metoprolol twice daily with weekly titration to response or 200 mg twice daily. beta(1)-adrenergic receptor polymorphisms are important determinants of antihypertensive response to metoprolol. In the future, codon 49 and 389 genotypes or beta(1)-adrenergic receptor haplotypes might be used to predict the diastolic blood pressure response to metoprolol in patients with hypertension [1]. Patients were studied at baseline and after each dose titration of metoprolol succinate (at 25, 50, 100, and 200 mg once/day) and immediate-release carvedilol (at 3.125, 6.25, 12.5, and 25 mg twice/day). As assessed by glucose AUC, there was no significant difference in the degree of beta(2)-blockade between metoprolol 200 mg and carvedilol 25 mg. In contrast to these data, the degree of beta(2)-blockade as assessed by potassium AUC was greater for carvedilol compared with metoprolol across all doses [2].
Mapenterol-d6 hydrochloride is the deuterium labeled Mapenterol hydrochloride. Mapenterol hydrochloride is a type of β2-adrenoceptor agonist[1][2].
Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist.
BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research[1][2].
Brombuterol hydrochloride (Bromobuterol hydrochloride) is a β-adrenergic receptor agonist[1].
Tropodifene (Tropaphen) is an α-Adrenergic receptor inhibitor.
DL 071IT is a potent non-selective beta-adrenergic receptor blocker. DL 071IT exhibits intrinsic sympathomimetic activity and weak membrane stabilizing activity. DL 071IT reduces exercise heart rate and systolic blood pressure, and even significantly lowers resting heart rate[1].
Nadolol D9 is the deuterium labeled Nadolol(SQ-11725), which is a non-selective beta blocker.
Phenylethanolamine A acts as a β-adrenergic agonist. Phenylethanolamine A is a byproduct during the Ractopamine synthesis process[1].
Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect[1][2][3][4].
Butofilolol is a potent β-blocking agent used in the research of hypertension[1].
CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD)[1].