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大鼠输精管中节前和节后毒蕈碱受体亚型

Pre- and postjunctional muscarinic receptor subtypes in the vas deferens of rat.

作者信息

Miranda H F, Duran E, Bustamante D, Paeile C, Pinardi G

机构信息

Department of Pharmacology, Faculty of Medicine, Universidad de Chile, Santiago.

出版信息

Gen Pharmacol. 1994 Dec;25(8):1643-7. doi: 10.1016/0306-3623(94)90366-2.

Abstract
  1. A pharmacological study of the pre- and postjunctional muscarinic receptors of the isolated rat vas deferens was carried out using more selective agonists and antagonists. 2. The prejunctional receptor was characterized on electrically stimulated preparations, while the postjunctional receptor was studied on vasa deferentia without stimulation. 3. The results indicate that atropine exhibited a similar affinity for the two populations of muscarinic receptor subtypes of this tissue. 4. 4-DAMP was able to differentiate with high affinity a subtype located at postjunctional level which had pharmacological similarities with the M3-ACh subtype and with low affinity a subtype located at prejunctional level. 5. The selective M1-ACh agonist McN-A-343 was not able to activate the postjunctional receptor, but showed a similar affinity to ACh for the prejunctional one. 6. At present, the prejunctional receptor can be considered as an atypical M1-ACh subtype based on the results obtained with the selective drugs available.
摘要
  1. 使用更具选择性的激动剂和拮抗剂,对离体大鼠输精管的节前和节后毒蕈碱受体进行了药理学研究。2. 在电刺激的标本上对节前受体进行表征,而在未受刺激的输精管上研究节后受体。3. 结果表明,阿托品对该组织的两种毒蕈碱受体亚型群体表现出相似的亲和力。4. 4-二甲基氨基吡啶(4-DAMP)能够以高亲和力区分位于节后水平的一种亚型,该亚型与M3-乙酰胆碱(ACh)亚型具有药理学相似性,并以低亲和力区分位于节前水平的一种亚型。5. 选择性M1-ACh激动剂 McN-A-343 不能激活节后受体,但对节前受体显示出与ACh相似的亲和力。6. 目前,根据现有选择性药物获得的结果,节前受体可被视为非典型的M1-ACh亚型。

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