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Molecular connectivity study of muscarinic receptor affinity of acetylcholine antagonists

✍ Scribed by Lemont B. Kier; Lowell H. Hall

Publisher
John Wiley and Sons
Year
1978
Tongue
English
Weight
539 KB
Volume
67
Category
Article
ISSN
0022-3549

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✦ Synopsis

A correlation between three molecular connectivity indexes and the muscarinic receptor affinity of 104 acetylcholine antagonists was found. Analysis of structure from these indexes reveals not only the importance of the onium and the bulky portions of the molecule but also their virtual independence of each other on the affinity. Analysis of the onium group portion of the molecules indicates that its contribution to the experimental affinity is virtually constant through a variety of structural variations. The influence of the bulky side chains, in contrast, is quite structure dependent. The equation relating connectivity indexes to muscarinic affinity of antagonists is capable of predicting the affinity of other antagonists as well as a number of agonist molecules.

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Molecular properties of local anesthetic
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## Abstract In spinal anesthesia, the effects of local anesthetics (LAs) are not completely explained by sodium channel inhibition. Other targets include neuronal nicotinic acetylcholine receptors (nAChRs). LA affinities for the __Torpedo californica__ nAChR were measured by inhibition of [^3^H]TCP