布普洛尔对豚鼠盲肠带中CGP 12177诱导的舒张和环磷酸腺苷（cAMP）积累的影响。

Effect of bupranolol on CGP 12177-induced relaxation and cAMP accumulation in the guinea pig taenia caecum.

Koike K, Horinouchi T, Takayanagi I

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

Gen Pharmacol. 1995 Dec;26(8):1791-4. doi: 10.1016/0306-3623(95)00115-8.

Abstract

The effect of bupranolol on CGP 12177-induced relaxation and cAMP accumulation in the guinea pig taenia caecum was examined. 2. The relaxant response to CGP 12177 was unaffected by propranolol (approximately 10(-6) M), whereas that to CGP 12177 was antagonized in a concentration-dependent manner by bupranolol; Schild plot of the data revealed the pA2 value of 5.61. 3. CGP 12177 significantly increased cyclic AMP level in this preparation. Bupranolol (10(-4) M) significantly decreased the cyclic AMP level that was elicited by CGP 12177, whereas propranolol (10(-5) M) produced no effect. 4. These results suggest that bupranolol appears to be an efficient beta3-antagonist in the guinea pig taenia caecum and confirm that the response to CGP 12177 is mediated by beta3-adrenoceptors.

摘要

研究了布普洛尔对豚鼠盲肠带中CGP 12177诱导的舒张和环磷酸腺苷（cAMP）积累的影响。2. 普萘洛尔（约10⁻⁶ M）对CGP 12177的舒张反应无影响，而布普洛尔以浓度依赖性方式拮抗对CGP 12177的舒张反应；数据的Schild图显示pA2值为5.61。3. CGP 12177显著增加了该制剂中的环磷酸腺苷水平。布普洛尔（10⁻⁴ M）显著降低了CGP 12177引起的环磷酸腺苷水平，而普萘洛尔（10⁻⁵ M）则无作用。4. 这些结果表明，布普洛尔在豚鼠盲肠带中似乎是一种有效的β3拮抗剂，并证实对CGP 12177的反应是由β3肾上腺素能受体介导的。