β-肾上腺素受体阻断剂与大鼠离体胃和子宫对肾上腺素及5-羟色胺的反应
Beta-adrenoceptor blocking agents and responses to adrenaline and 5-hydroxytryptamine in rat isolated stomach and uterus.
作者信息
Schechter Y, Weinstock M
出版信息
Br J Pharmacol. 1974 Oct;52(2):283-7. doi: 10.1111/j.1476-5381.1974.tb09711.x.
Abstract
1 Four beta-adrenoceptor blocking agents, (+/-)- and (+)-propranolol, practolol and oxprenolol, were found to antagonize, apparently competitively, the responses of both the rat isolated stomach and uterus to 5-hydroxytryptamine (5-HT).2 The pA(2) values for each of these agents as antagonists of the contractile action of 5-HT on the rat stomach were found to be: (+/-)-propranolol, 6.08; (+)-propranolol, 4.94; practolol, 3.43; and oxprenolol, 5.99. These values were very similar to the corresponding figures for antagonism of 5-HT-induced contractions of the uterus.3 pA(2) values for antagonism of adrenaline-induced relaxations by the four blocking agents on the rat stomach and uterus did not differ from the values for 5-HT blockade.4 To antagonize contractile responses to acetylcholine of the rat stomach it was necessary to give 100 times more (+/-)-propranolol than was needed to antagonize responses to 5-HT.
摘要
发现四种β - 肾上腺素能受体阻断剂，即（±）-和（+）-普萘洛尔、心得宁和氧烯洛尔，对大鼠离体胃和子宫对5 - 羟色胺（5 - HT）的反应具有明显的竞争性拮抗作用。
发现这些药物作为5 - HT对大鼠胃收缩作用的拮抗剂时，其pA(2)值分别为：（±）-普萘洛尔，6.08；（+）-普萘洛尔，4.94；心得宁，3.43；氧烯洛尔，5.99。这些值与拮抗5 - HT诱导的子宫收缩的相应数值非常相似。
这四种阻断剂对大鼠胃和子宫肾上腺素诱导的舒张作用的拮抗pA(2)值与5 - HT阻断的值没有差异。
要拮抗大鼠胃对乙酰胆碱的收缩反应，所需的（±）-普萘洛尔剂量是拮抗对5 - HT反应所需剂量的100倍。
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