组胺H2拮抗剂甲硫米特对离体大鼠全胃作用的定量研究。
A quantitative study of metiamide, a histamine H2-antagonist, on the isolated whole rat stomach.
作者信息
Bunce K T, Parsons M E
出版信息
J Physiol. 1976 Jun;258(2):453-65. doi: 10.1113/jphysiol.1976.sp011430.
Abstract
- An isolated whole stomach preparation from immature rats is described. The lumen of the stomach was perfused and the hydrogen ion activity of the perfusate recorded continuously. 2. The mean basal acid secretion before stimulation was 4-19 +/- 0-31 X 10 (-8) mol min-1. Metiamide did not significantly reduce this spontaneous secretion. 3. The preparation gave dose-dependent responses to histomine (10(-5)-10(-4)M) which were readily reversed on washing. 4. The effect of metiamide on histamine-stimulated acid secretion was investigated. Metamide, at doses of 3 X 10(-6)M, and 3 X 10(-5)M, caused a parallel displacement of the histamine dose-response curve, indicating competitive antagonism. These dose-response curves were used to calculate dose ratios (DR) for metiamide. 5. A plot of log10 (DR - 1) against log 10 [antagonist] gave a pA2 value for metiamide of 5-91.
摘要
- 描述了一种从未成熟大鼠制备的离体全胃标本。对胃腔进行灌注，并连续记录灌注液中的氢离子活性。2. 刺激前的平均基础酸分泌为4 - 19±0 - 31×10（-8）摩尔/分钟。甲硫咪胺并未显著降低这种自发分泌。3. 该标本对组胺（10（-5）- 10（-4）M）呈现剂量依赖性反应，冲洗后反应易于逆转。4. 研究了甲硫咪胺对组胺刺激的酸分泌的影响。剂量为3×10（-6）M和3×10（-5）M的甲硫咪胺导致组胺剂量 - 反应曲线平行位移，表明存在竞争性拮抗作用。这些剂量 - 反应曲线用于计算甲硫咪胺的剂量比（DR）。5. 以log10（DR - 1）对log10[拮抗剂]作图，得出甲硫咪胺的pA2值为5 - 91。
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