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豚鼠食管黏膜肌层和气管毒蕈碱受体的体外比较

Comparison of the muscarinic receptors of the guinea-pig oesophageal muscularis mucosae and trachea in vitro.

作者信息

Eglen R M, Whiting R L

机构信息

Syntex Research Institute of Pharmacology, Palo Alto, CA 94304.

出版信息

J Auton Pharmacol. 1988 Sep;8(3):181-9. doi: 10.1111/j.1474-8673.1988.tb00181.x.

Abstract
  1. The muscarinic receptor profile of the guinea-pig oesophageal muscularis mucosae has been compared to that of the trachea in vitro. There was no significant difference in the potency of the following muscarinic agonists at muscarinic receptors in the two tissues: carbachol, RS-86, ethoxyethyltrimethyl-ammonium, bethanechol and pilocarpine. RS-86 was 6-fold more potent at receptors in the muscularis mucosae in comparison to the trachea. There was no difference in the affinity of either carbachol or RS 86 at receptors in the two tissues. 2. The affinities (pA2) of the majority of antagonists (atropine, 4 diphenylacetoxy-N-methylpiperidine methiodide, AF-DX 116, silabenzhexol, methoctramine and gallamine) were similar at receptors in the muscularis mucosae and trachea. In contrast, the affinity of pirenzepine was approximately 5-fold greater at receptors in the muscularis mucosae (pA2 = 7.4) in comparison to receptors in the trachea (pA2 = 6.8). 3. It is concluded that the muscarinic receptor profile of the oesophageal muscularis and trachea are similar and only differ slightly with respect to the affinity of pirenzepine. Consequently, it is difficult to justify receptor heterogeneity in these two tissues.
摘要
  1. 已在体外比较了豚鼠食管黏膜肌层与气管的毒蕈碱受体特征。以下毒蕈碱激动剂对两种组织中毒蕈碱受体的效力无显著差异:卡巴胆碱、RS - 86、乙氧基乙基三甲基铵、氨甲酰甲胆碱和毛果芸香碱。与气管相比,RS - 86对黏膜肌层受体的效力高6倍。卡巴胆碱或RS 86对两种组织中受体的亲和力无差异。2. 大多数拮抗剂(阿托品、4 - 二苯基乙酰氧基 - N - 甲基哌啶甲碘化物、AF - DX 116、西拉苄醇、甲奥克胺和加拉明)对黏膜肌层和气管中受体的亲和力(pA2)相似。相比之下,哌仑西平对黏膜肌层中受体的亲和力(pA2 = 7.4)比气管中受体的亲和力(pA2 = 6.8)大约高5倍。3. 得出的结论是,食管肌层和气管的毒蕈碱受体特征相似,仅在哌仑西平的亲和力方面略有不同。因此,很难证明这两种组织中存在受体异质性。

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