关于两种竞争性拮抗剂的同时作用。
On the simultaneous action of two competitive antagonists.
作者信息
Gingsborg B L, Stephenson R P
出版信息
Br J Pharmacol. 1974 Jun;51(2):287-300. doi: 10.1111/j.1476-5381.1974.tb09659.x.
Abstract
1 A hypothesis is outlined predicting the conditions in which the addition of a second competitive antagonist will increase rather than reduce the response to an agonist.2 Experiments were performed with the guinea-pig ileum as the test tissue, hexyltrimethyl ammonium as the agonist, benzilyltropine methiodide as the ;slow' antagonist and pentyltriethyl ammonium as the ;fast' antagonist.3 The results are consistent with the hypothesis, if the affinity constant for hexyltrimethyl ammonium is between 2.7 and 3.7 x 10(4)M(-1), if the dissociation time constant for the slow antagonist is greater than 10 min and if that for the fast antagonist is less than 10 seconds.
摘要
概述了一个假说，该假说预测在何种条件下添加第二种竞争性拮抗剂会增强而非降低对激动剂的反应。
以豚鼠回肠作为测试组织进行实验，以己基三甲基铵作为激动剂，以甲磺酸苄基托品作为“慢”拮抗剂，以戊基三乙基铵作为“快”拮抗剂。
如果己基三甲基铵的亲和常数在2.7至3.7×10⁴M⁻¹之间、“慢”拮抗剂的解离时间常数大于10分钟且“快”拮抗剂的解离时间常数小于10秒，那么结果与该假说相符。
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