哌仑西平和N-甲基东莨菪碱对大鼠输精管毒蕈碱受体亚型的选择性拮抗作用。

Selective antagonism by pirenzepine and N-methyl-scopolamine on muscarinic receptor subtypes of the rat vas deferens.

Miranda H F, Silva W I, Wolstenholme W W, Cuevas N

Department of Pharmacology, School of Medicine, Central Caribbean University, Cayey, PR 00634.

Gen Pharmacol. 1988;19(3):417-20. doi: 10.1016/0306-3623(88)90039-0.

Abstract

The effects of pirenzepine and N-methyl-scopolamine on the responses to ACh in the isolated rat vas deferens were studied. 2. Pirenzepine was inactive at the M2-ACh receptor. 3. N-methyl-scopolamine was a competitive antagonist (pA2 = 8.76) at M2-ACh receptor, alone or in the presence of pirenzepine. 4. Pirenzepine and N-methyl-scopolamine were both non-competitive antagonists at M1-ACh receptor. 5. The mixture of pirenzepine and N-methyl-scopolamine did not alter the type of antagonism demonstrated by each drug at the M1-ACh receptor.

摘要

研究了哌仑西平和N-甲基东莨菪碱对离体大鼠输精管中乙酰胆碱（ACh）反应的影响。2. 哌仑西平对M2-ACh受体无活性。3. N-甲基东莨菪碱单独或在哌仑西平存在时，是M2-ACh受体的竞争性拮抗剂（pA2 = 8.76）。4. 哌仑西平和N-甲基东莨菪碱都是M1-ACh受体的非竞争性拮抗剂。5. 哌仑西平和N-甲基东莨菪碱的混合物未改变每种药物在M1-ACh受体上表现出的拮抗类型。