一种合成的B2受体拮抗剂对豚鼠缓激肽诱导的支气管收缩的抑制作用
Inhibition of bradykinin-induced bronchoconstriction in the guinea-pig by a synthetic B2 receptor antagonist.
作者信息
Jin L S, Seeds E, Page C P, Schachter M
机构信息
Department of Pharmacology, King's College, Chelsea Campus, University of London.
出版信息
Br J Pharmacol. 1989 Jun;97(2):598-602. doi: 10.1111/j.1476-5381.1989.tb11991.x.
Abstract
- Intravenous bradykinin (Bk) elicited bronchoconstriction in the anaesthetized ventilated guinea-pig which was not mimicked by the B1 receptor agonist, des-Arg9-Bk. 2. Bradykinin-induced bronchoconstriction was inhibited by the B2 receptor antagonist B4881, but not by the B1 receptor antagonist des-Arg9-Leu8-Bk. The effect of B4881 was short-lived. 3. The B2 receptor antagonist as B4881 was selective for bradykinin as B4881 did not significantly inhibit bronchoconstriction induced by i.v. bombesin, platelet activating factor, acetylcholine, histamine or vagal stimulation. 4. These results suggest that bradykinin-induced bronchoconstriction in the guinea-pig is via activation of a B2 receptor population and that B4881 is a selective B2 antagonist that may be useful for investigating the involvement of bradykinin in the lung.
摘要
- 静脉注射缓激肽（Bk）可使麻醉通气的豚鼠出现支气管收缩，而B1受体激动剂去-精氨酸9-缓激肽（des-Arg9-Bk）不会模拟这种效应。2. 缓激肽诱导的支气管收缩受到B2受体拮抗剂B4881的抑制，但不受B1受体拮抗剂去-精氨酸9-亮氨酸8-缓激肽（des-Arg9-Leu8-Bk）的抑制。B4881的作用持续时间较短。3. B4881作为B2受体拮抗剂对缓激肽具有选择性，因为B4881不会显著抑制静脉注射蛙皮素、血小板活化因子、乙酰胆碱、组胺或迷走神经刺激所诱导的支气管收缩。4. 这些结果表明，豚鼠体内缓激肽诱导的支气管收缩是通过激活一群B2受体实现的，并且B4881是一种选择性B2拮抗剂，可能有助于研究缓激肽在肺部的作用。
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