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神经节与回肠毒蕈碱受体之间的拮抗剂鉴别

Antagonist discrimination between ganglionic and ileal muscarinic receptors.

作者信息

Brown D A, Forward A, Marsh S

出版信息

Br J Pharmacol. 1980;71(2):362-4. doi: 10.1111/j.1476-5381.1980.tb10948.x.

Abstract

The effects of four antagonists on the depolarization of isolated superior cervical ganglia and the contraction of isolated ileal segments of the rat were compared. pA2 values estimated from Schild plots indicated significantly higher affinities of stercuronium (x100) and pirenzepine (x23) and a significantly lower affinity of 4-diphenylacetoxy-N-methylpiperidine methiodide (x0.39) for the ganglion than for the ileum. The affinities of N-methylscopolamine for the two tissues were not significantly different. It is concluded that the two types of muscarinic receptor are not identical.

摘要

比较了四种拮抗剂对大鼠离体颈上神经节去极化和离体回肠段收缩的影响。从Schild图估算的pA2值表明,与回肠相比,司替碘铵(x100)和哌仑西平(x23)对神经节的亲和力显著更高,而4-二苯基乙酰氧基-N-甲基哌啶甲碘化物(x0.39)对神经节的亲和力显著更低。N-甲基东莨菪碱对这两种组织的亲和力无显著差异。结论是两种毒蕈碱受体类型不相同。

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