米芬替丁对组胺刺激的人离体心房的作用：与雷尼替丁和西咪替丁的比较

Effect of mifentidine on histamine-stimulated human atrium "in vitro": comparison with ranitidine and cimetidine.

作者信息

Poli E, Medici D, Contini G A, Bertaccini G

出版信息

Arch Int Pharmacodyn Ther. 1985 Feb;273(2):221-5.

Abstract

The new H2-antagonist mifentidine was tested on human atrium, in comparison with cimetidine and ranitidine, for its activity against histamine-induced inotropic effect. Mifentidine was found to be 10 times more potent than ranitidine and 100 times more potent than cimetidine. The kinetics of the three compounds are typical of a competitive antagonism and the pA2 value was of 8.60, 6.35, 5.94 for mifentidine, ranitidine and cimetidine, respectively. Our data confirm previous findings in another isolated heart preparation, namely the guinea-pig papillary muscle.

摘要

将新型H2拮抗剂米芬替丁与西咪替丁和雷尼替丁进行比较，在人体心房上测试了其对组胺诱导的变力作用的活性。结果发现，米芬替丁的效力比雷尼替丁强10倍，比西咪替丁强100倍。这三种化合物的动力学表现为典型的竞争性拮抗作用，米芬替丁、雷尼替丁和西咪替丁的pA2值分别为8.60、6.35和5.94。我们的数据证实了先前在另一种离体心脏标本即豚鼠乳头肌中的研究结果。

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引用本文的文献

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Pharmacokinetics of mifentidine after single and multiple oral administration to healthy volunteers.单次及多次口服给予健康志愿者米芬替丁后的药代动力学

Br J Clin Pharmacol. 1988 Oct;26(4):407-13. doi: 10.1111/j.1365-2125.1988.tb03399.x.

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Pharmacokinetic and pharmacodynamic properties of histamine H2-receptor antagonists. Relationship between intrinsic potency and effective plasma concentrations.组胺H2受体拮抗剂的药代动力学和药效学特性。内在活性与有效血药浓度之间的关系。

Clin Pharmacokinet. 1991 Mar;20(3):218-36. doi: 10.2165/00003088-199120030-00004.

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