CGP 20712 A

CGP 20712 A (CGP 20712 mesylate) is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 A exhibits ~10,000-fold selectivity over β2-adrenoceptors[1].

In myocytes, the activation of adenylate cyclase causes by β2-adrenoceptors is not detected in the presence of 10 nM, 100 nM or 1000 nM CGP 20712 A (CGP 20712 mesylate), which selectively antagonized beta1-adrenoceptors[2].

Pretreatment of 8-day-old rats with 5 mg/kg CGP 20712 A do not change the plasma ACTH response to insulin injection[3].

[1]. Dooley DJ, et al. CGP 20712 A: a useful tool for quantitating beta 1- and beta 2-adrenoceptors. Eur J Pharmacol. 1986 Oct 14;130(1-2):137-9. [2]. Kitagawa Y, et al. Determination of beta-adrenoceptor subtype on rat isolated ventricular myocytes by use of highly selective beta-antagonists. Br J Pharmacol. 1995 Sep;116(1):1635-43. [3]. Grino M, et al. Ontogeny of insulin-induced hypoglycemia stimulation of adrenocorticotropin secretion in the rat: role of catecholamines. Endocrinology. 1992 Dec;131(6):2763-8.