在一系列五元环毒蕈碱激动剂中，亲和力和效能与化学结构的相关性比效价更强。
Affinity and efficacy correlate with chemical structure more than potency does in a series of pentatomic cyclic muscarinic agonists.
作者信息
Angeli P, Brasili L, Giannella M, Gualtieri F, Pigini M
出版信息
Br J Pharmacol. 1985 Aug;85(4):783-6. doi: 10.1111/j.1476-5381.1985.tb11076.x.
Abstract
The efficacy and affinity of nine pentatomic cyclic muscarinic agonists were determined on the guinea-pig ileum, according to the method of Furchgott & Bursztyn (1967). The efficacy and affinity of these agonists are affected differently by structural modifications. Our results suggest that a strong dipole oriented in the same direction as that of the hydroxy group of muscarine, or the presence of a polarizable atom in the same position, are important for efficacy.
摘要
根据Furchgott和Bursztyn（1967年）的方法，测定了九种五元环毒蕈碱激动剂对豚鼠回肠的效力和亲和力。这些激动剂的效力和亲和力受结构修饰的影响不同。我们的结果表明，与毒蕈碱羟基方向相同的强偶极，或在相同位置存在可极化原子，对效力很重要。
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