使用亚型选择性毒蕈碱受体拮抗剂的功能和直接结合研究。
Functional and direct binding studies using subtype selective muscarinic receptor antagonists.
作者信息
Kunysz E L, Michel A D, Whiting R L
机构信息
Department of Pharmacology, Palo Alto, CA 94304.
出版信息
Br J Pharmacol. 1988 Mar;93(3):491-500. doi: 10.1111/j.1476-5381.1988.tb10303.x.
Abstract
- Muscarinic receptor antagonists were examined in direct binding studies on guinea-pig cardiac and cortical muscarinic receptors. Pirenzepine, dicyclomine and hexahydroadiphenine were shown to be selective ligands for the putative M1-muscarinic receptor. 2. Functional affinity estimates of the muscarinic ligands studied was determined from their ability to inhibit carbachol-stimulated inositol phosphate (IP) accumulation in guinea-pig cortical slices. 3. The affinity estimates for the inhibition of muscarinic agonist-stimulated IP accumulation were better correlated with affinity estimates obtained from binding studies on the M1 than the M2 muscarinic receptor. 4. These data provide additional evidence, both from direct binding and functional studies, for the presence of M1 and M2 muscarinic receptor subtypes.
摘要
- 在豚鼠心脏和皮层毒蕈碱受体的直接结合研究中对毒蕈碱受体拮抗剂进行了检测。哌仑西平、双环维林和六氢阿地芬宁被证明是假定的M1毒蕈碱受体的选择性配体。2. 所研究的毒蕈碱配体的功能亲和力估计值是根据它们抑制豚鼠皮层切片中卡巴胆碱刺激的肌醇磷酸（IP）积累的能力来确定的。3. 抑制毒蕈碱激动剂刺激的IP积累的亲和力估计值与从M1而非M2毒蕈碱受体结合研究中获得的亲和力估计值相关性更好。4. 这些数据从直接结合和功能研究两方面为M1和M2毒蕈碱受体亚型的存在提供了额外证据。
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