CAS NO: | 64208-32-8 |
规格: | 98% |
分子量: | 315.8 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
Background:
CGP 12177 hydrochloride is a partial agonist of β3-adrenoceptor and an antagonist of β1- and β2-adrenoceptors with Ki values of 0.9, 4 and 88 nM for β1-, β2- and β3-adrenoceptors, respectively.
β3-adrenoceptor is exists mainly in adipose tissue and plays an important role in the regulation of thermogenesis and lipolysis.
CGP 12177 hydrochloride is a partial agonist of β3-adrenoceptor and an antagonist of β1- and β2-adrenoceptors. In human ventricular myocytes (HVMs), CGP12177 slightly activated L-type Ca2+ current (ICa,L) [1].
In sympathectomized (SX) interscapular brown adipose tissue (BAT) isolated from rats, CGP-12177 restored normal thyroxine (T4) deiodination, which suggested that CGP-12177 activated 5’-deiodinase type II through β3-adrenoceptor [2]. In spontaneously hypertensive rats (SHR) and normotensive rats, CGP12177 induced vasorelaxant effects and decreased hindquarters
perfusion pressure in a dose-dependent way induced by 5-hydroxytryptamine (5-HT), which was inhibited by bupranolol, a β1LA-adrenoceptor antagonist. These results suggested that CGP12177 induced vasorelaxant effects through activation of β1LA-adrenoceptor [3].
参考文献:
[1]. Treinys R, Zablockait? D, Gendvilien? V, et al. β?-Adrenergic regulation of L-type Ca2? current and force of contraction in human ventricle. J Membr Biol, 2014, 247(4): 309-318.
[2]. Hofer D, Raíces M, Schauenstein K, et al. The in vivo effects of beta-3-receptor agonist CGP-12177 on thyroxine deiodination in cold-exposed, sympathectomized rat brown fat. Eur J Endocrinol, 2000, 143(2): 273-277.
[3]. Holopherne D, Mallem MY, Le Strat E, et al. CGP12177-induced haemodynamic and vascular effects in normotensive and hypertensive rats. Eur J Pharmacol, 2008, 591(1-3): 196-202.