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哌仑西平和阿托品对豚鼠胃底及胃平滑肌的pA2值比较研究。

Comparative study of pA2 values of pirenzepine and atropine for guinea-pig gastric fundus and gastric smooth muscle.

作者信息

Del Tacca M, Soldani G, Bernardini C, Martinotti E

出版信息

Pharmacology. 1984;29(6):329-35. doi: 10.1159/000138032.

Abstract

Concentration-response curves of bethanechol were obtained from isolated guinea pig gastric fundus and gastric circular smooth muscle strips before and after exposure to pirenzepine or atropine. In the presence of pirenzepine and atropine these curves were shifted parallel to the right with no change in maximum response. Against bethanechol, mean pA2 values were 7.06 for pirenzepine and 8.16 for atropine on gastric fundus, with slopes of Schild plots close to unity for both antagonists, whereas in the case of gastric smooth muscle pA2 values were 6.52 for pirenzepine and 8.52 for atropine, with the slope of the Schild plot significantly less than -1 in the case of pirenzepine. The values of the Schild slope seem to indicate that pirenzepine interacts with a single, apparently homogeneous population of muscarinic receptors on gastric mucosa, at variance with the behaviour of pirenzepine on receptors of gastric smooth muscle.

摘要

在暴露于哌仑西平或阿托品之前和之后,从离体豚鼠胃底和胃环行平滑肌条获得了氨甲酰甲胆碱的浓度-反应曲线。在存在哌仑西平和阿托品的情况下,这些曲线平行右移,最大反应无变化。在胃底,针对氨甲酰甲胆碱,哌仑西平的平均pA2值为7.06,阿托品为8.16,两种拮抗剂的Schild图斜率均接近1,而在胃平滑肌中,哌仑西平的pA2值为6.52,阿托品为8.52,哌仑西平的Schild图斜率明显小于-1。Schild斜率值似乎表明,哌仑西平与胃黏膜上单一的、明显同质的毒蕈碱受体群体相互作用,这与哌仑西平在胃平滑肌受体上的行为不同。

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