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一些毒蕈碱受体拮抗剂的亲和常数与其在豚鼠心房和回肠纵肌中对[3H]喹核醇基苯甲酸酯结合的取代作用的比较。

Comparison of the affinity constant of some muscarinic receptor antagonists with their displacement of [3H]quinuclidinyl benzilate binding in atrial and ileal longitudinal muscle of the guinea-pig.

作者信息

Choo L K, Mitchelson F J

出版信息

J Pharm Pharmacol. 1985 Sep;37(9):656-8. doi: 10.1111/j.2042-7158.1985.tb05106.x.

Abstract

The ability of the muscarinic receptor antagonists fenipramide, 4-diphenylacetoxy-N-methyl piperidine methiodide (4-DAMP) and secoverine to displace [3H]QNB binding was correlated with the inhibition of responses of cholinomimetics at muscarinic receptors in the atria and ileal longitudinal muscle of the guinea-pig. Fenipramide and 4-DAMP exhibited a 2-4 fold higher affinity for muscarinic receptors in ileal longitudinal muscle in both types of experiments. Secoverine exhibited no difference in affinity in the two tissues.

摘要

毒蕈碱受体拮抗剂非尼普拉明、4-二苯乙酰氧基-N-甲基哌啶甲碘化物(4-DAMP)和塞考维林取代[3H]QNB结合的能力,与它们对豚鼠心房和回肠纵肌中毒蕈碱受体处拟胆碱药反应的抑制作用相关。在这两种实验中,非尼普拉明和4-DAMP对回肠纵肌中毒蕈碱受体的亲和力高2至4倍。塞考维林在两种组织中的亲和力没有差异。

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