豚鼠盲肠带中的β3-肾上腺素能受体机制

Beta3-adrenoceptor mechanisms in guinea-pig taenia caecum.

作者信息

Koike K, Takayanagi I

机构信息

Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Funabashi, Chiba, Japan.

出版信息

Life Sci. 1998;62(17-18):1503-7. doi: 10.1016/s0024-3205(98)00097-6.

DOI:10.1016/s0024-3205(98)00097-6

PMID:9585126

Abstract

Beta-adrenoceptor-mediated relaxation of guinea-pig taenia caecum was investigated by studying the effects of BRL37344, CGP12177 and norepinephrine. These drugs caused graded relaxation of the guinea-pig taenia caecum. The concentration-response curves for these drugs were unaffected by propranolol, atenolol, butoxamine, prazosin, yohimbine and phentolamine. Bupranolol produced shifts of the concentration-response curves for these drugs. Schild regression analyses carried out for bupranolol against BRL37344, CGP12177 and norepinephrine gave pA2 values of 5.79, 5.61 and 5.53, respectively. CGP12177 and norepinephrine significantly increased cyclic AMP levels in this preparation. Bupranolol significantly decreased cyclic AMP levels elicited by CGP12177 and norepinephrine, whereas propranolol produced no effect. These results suggest that the relaxant responses to BRL37344, CGP12177 and norepinephrine in the guinea-pig taenia caecum are mediated by beta3-adrenoceptors.

摘要

通过研究BRL37344、CGP12177和去甲肾上腺素的作用，对豚鼠盲肠带β-肾上腺素能受体介导的舒张作用进行了研究。这些药物引起豚鼠盲肠带的分级舒张。这些药物的浓度-反应曲线不受普萘洛尔、阿替洛尔、丁氧胺、哌唑嗪、育亨宾和酚妥拉明的影响。布普萘洛尔使这些药物的浓度-反应曲线发生位移。对布普萘洛尔针对BRL37344、CGP12177和去甲肾上腺素进行的Schild回归分析分别得出pA2值为5.79、5.61和5.53。CGP12177和去甲肾上腺素显著提高了该制剂中的环磷酸腺苷水平。布普萘洛尔显著降低了CGP12177和去甲肾上腺素引起的环磷酸腺苷水平，而普萘洛尔则没有作用。这些结果表明，豚鼠盲肠带对BRL37344、CGP12177和去甲肾上腺素的舒张反应是由β3-肾上腺素能受体介导的。