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Studies on the relationship of binding affinity to psychoactive and anticholinergic potency of a group of psychotomimetic glycolates

Authors
Journal
Brain Research
0006-8993
Publisher
Elsevier
Publication Date
Volume
124
Issue
2
Identifiers
DOI: 10.1016/0006-8993(77)90889-7
Disciplines
  • Biology
  • Pharmacology

Abstract

Abstract A study was undertaken of the possible relationship of the binding affinity of a series of anticholinergic psychotomimetic drugs to their psychopharmacological and anticholinergic effects. Binding was measured to brain homogenates and nerve endings using [ 3H]quinuclidinyl benzilate (QB), a highly potent psychotomimetic agent presumably affecting muscarinic sites in the brain. The two stereoisomers of QB were compared; and although the l-isomer had 15 times the binding affinity of d-isomer, the l-isomer had over 200 times the psychopharmacological potency of the d-form. When the relative binding affinity of a homologous series of glycolate esters was compared with their relative psychoactive potency, the correlation was excellent; however, when compounds with heterocyclic amino ring (e.g., tropanol) other than quinuclidine and piperidine were considered, the correlation was poor. The correlation between binding affinity and antagonism to acetylcholine-induced contraction of ileum was more consistent. A study was undertaken on the effect of added lipids on QB binding to nerve endings, and it was found that phosphatidyl serine had a significant enhancing effect while gangliosides were inhibitory.

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