Witte K, Olbrich H G, Langer L, Lemmer B
Center of Pharmacology, J.W. Goethe-University, Frankfurt, Germany.
Eur J Pharmacol. 1993 Oct 15;247(2):215-8. doi: 10.1016/0922-4106(93)90080-s.
The beta-adrenoceptor-adenylyl cyclase system was studied in heart ventricles from Wistar rats, cardiomyopathic (BIO 8262) and nonfailing control hamsters (CLAC) using the beta 1-adrenoceptor antagonist CGP 20712A. In radioligand binding studies, the majority of beta-adrenoceptors in ventricles from rats as well as from CLAC hamsters was of the beta 1-subtype (72.2% and 76.6%, respectively). In BIO ventricles a significant (CLAC vs. BIO, P < 0.05) reduction in the beta 1-subtype (62.9%) was found. In Wistar rats the subtype-mediated stimulation of adenylyl cyclase reflected the beta 1:beta 2 ratio as determined by binding studies. In hamster ventricles the effect of isoprenaline was mediated predominantly (CLAC) or exclusively (BIO) via the beta 2-subtype, indicating that cardiac beta 1-adrenoceptors were partly (CLAC) or completely (BIO) uncoupled from the adenylyl cyclase.
使用β1肾上腺素能受体拮抗剂CGP 20712A,对Wistar大鼠、心肌病(BIO 8262)和非衰竭对照仓鼠(CLAC)的心室中的β肾上腺素能受体-腺苷酸环化酶系统进行了研究。在放射性配体结合研究中,大鼠心室以及CLAC仓鼠心室中的大多数β肾上腺素能受体为β1亚型(分别为72.2%和76.6%)。在BIO心室中,发现β1亚型显著减少(CLAC与BIO相比,P < 0.05)(62.9%)。在Wistar大鼠中,亚型介导的腺苷酸环化酶刺激反映了结合研究确定的β1:β2比值。在仓鼠心室中,异丙肾上腺素的作用主要通过β2亚型介导(CLAC)或仅通过β2亚型介导(BIO),表明心脏β1肾上腺素能受体部分(CLAC)或完全(BIO)与腺苷酸环化酶解偶联。