盐酸贝凡洛尔（NC - 1400）和拉贝洛尔对大鼠离体胸主动脉的α1 - 肾上腺素能受体阻断活性——它们能区分亚型吗？

Alpha 1-adrenoceptor blocking activities of bevantolol hydrochloride(NC-1400) and labetalol in rat isolated thoracic aorta--do they distinguish between subtypes?

Shiraishi K, Moriya M, Miyake N, Takayanagi I

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

Gen Pharmacol. 1992 Sep;23(5):843-5. doi: 10.1016/0306-3623(92)90235-c.

Abstract

alpha 1-adrenoceptor blocking activity of bevantolol(NC-1400) was tested in the rat thoracic aorta, comparing with that of labetalol. 2. In alpha 1-adrenoceptor blocking activity, bevantolol(NC-1400) was 1/20th as potent as labetalol. 3. The pA2 values of bevantolol(NC-1400) and labetalol estimated in the rat thoracic aorta were compared with those in the rabbit thoracic aorta, which were reported by Takayanagi et al. [Takayanagi I., Kizawa Y., Iwasaki S. and Nakagoshi A. (1987) Gen. Pharmac. 18, 87-89]. 4. The pA2 values of bevantolol(NC-1400) and labetalol were approximately 1 order of magnitude higher in rat aorta than in rabbit aorta, suggesting that both the drugs distinguish between subtypes of alpha 1-adrenoceptors.

摘要

在大鼠胸主动脉中测试了贝凡洛尔（NC - 1400）的α1 - 肾上腺素能受体阻断活性，并与拉贝洛尔进行了比较。2. 在α1 - 肾上腺素能受体阻断活性方面，贝凡洛尔（NC - 1400）的效力仅为拉贝洛尔的1/20。3. 将在大鼠胸主动脉中测得的贝凡洛尔（NC - 1400）和拉贝洛尔的pA2值与高柳等人[高柳一、木泽洋、岩崎史、中越昭（1987年）《普通药理学》18卷，87 - 89页]报道的兔胸主动脉中的pA2值进行了比较。4. 贝凡洛尔（NC - 1400）和拉贝洛尔在大鼠主动脉中的pA2值比在兔主动脉中大约高1个数量级，这表明这两种药物对α1 - 肾上腺素能受体亚型具有区分能力。