对平滑肌毒蕈碱受体具有高选择性的己环铵衍生物。
Hexocyclium derivatives with a high selectivity for smooth muscle muscarinic receptors.
作者信息
Micheletti R, Schiavone A, Cereda E, Donetti A
机构信息
Department of Pharmacology, Istituto De Angeli, Milano, Italy.
出版信息
Br J Pharmacol. 1990 May;100(1):150-2. doi: 10.1111/j.1476-5381.1990.tb12067.x.
Abstract
- The affinity of a number of derivatives of the muscarinic antagonist, hexocyclium, containing an amidine cationic head, for guinea-pig cardiac and ileal receptors was investigated. 2. All the compounds studied displayed a greater affinity for muscular than for cardiac muscarinic receptors. 3. The 5 fold ileal selectivity of hexocyclium was increased by a number of chemical substitutions. The largest discrimination between receptors (about 200 fold) was found for the formamidine derivative. 4. The selectivity displayed by the hexocyclium derivatives stemmed from a greater decrease in affinity towards cardiac as compared to ileal receptors.
摘要
- 研究了一系列含有脒阳离子头的毒蕈碱拮抗剂己环铵的衍生物对豚鼠心脏和回肠受体的亲和力。2. 所有研究的化合物对肌肉型毒蕈碱受体的亲和力均大于对心脏型毒蕈碱受体的亲和力。3. 己环铵5倍的回肠选择性通过一些化学取代得以提高。甲脒衍生物的受体间最大区分度（约200倍）被发现。4. 己环铵衍生物表现出的选择性源于其对心脏受体的亲和力相较于回肠受体有更大程度的降低。
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