Uses
CGP-20712A methanesulfonate salt has been used as a β1-adrenergic receptor antagonist in adult rat ventricular myocytes (ARVM) and rat cardiac fibroblasts. It may also be used as an antagonist for the β1-adrenergic receptor in rat bladder smooth muscles.
Biological Activity
Highly selective and potent β 1 -adrenoceptor antagonist (IC 50 = 0.7 nM). Displays 10,000-fold selectivity over β 2 -adrenoceptors. Also available as part of the β -Adrenoceptor Antagonist Tocriset™ .
Biochem/physiol Actions
CGP-20712A methanesulfonate salt is a selective β1-adrenoceptor antagonist.
in vitro
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.
in vivo
Pretreatment of 8-day-old rats with 5 mg/kg CGP 20712 A do not change the plasma ACTH response to insulin injection.
IC 50
β adrenergic receptor
