使用体外胃酸分泌试验估算组胺H2受体拮抗剂的pKB值。
Estimation of pKB values for histamine H2-receptor antagonists using an in vitro acid secretion assay.
作者信息
Angus J A, Black J W, Stone M
出版信息
Br J Pharmacol. 1980 Mar;68(3):413-23. doi: 10.1111/j.1476-5381.1980.tb14555.x.
Abstract
1 Histamine H2-receptor antagonism by burimamide, metiamide and cimetidine was analysed under apparent equilibrium conditions in the lumen-perfused isolated stomach preparation of the mouse. 2 The behaviour of these compounds was not incompatible with simple competitive antagonism but the estimated pKB values (-log KB) were all significantly lower, by about 1 log unit, than reference values reported for guinea-pig atrium or rat uterus. 3 There seems no need to propose that the parietal cell receptors are somehow different from the others; metiamide continually appears in the gastric juice so that a steady-state but not equilibrium can presumably be reached with respect to the bath concentration and this could keep the antagonist concentration artificially low in the region of the receptors.
摘要
- 在小鼠胃腔灌注离体胃制备物的表观平衡条件下，分析了布立马胺、甲硫米特和西咪替丁对组胺H2受体的拮抗作用。2. 这些化合物的行为与简单竞争性拮抗作用并不矛盾，但估计的pKB值（-log KB）均显著低于豚鼠心房或大鼠子宫报道的参考值，约低1个对数单位。3. 似乎没有必要提出壁细胞受体与其他受体有所不同；甲硫米特持续出现在胃液中，因此相对于浴液浓度，大概可以达到稳态而非平衡状态，这可能会使受体区域的拮抗剂浓度人为降低。
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