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Document Type

Research

Keywords

dopaminergic pharmacophore; ergot alkaloids; structure-activity relationships; drug design

Abstract

The problem of defining structural similarities between apomorphine and certain ergot alkaloid derivatives, two chemically dissimilar types of drugs having similar pharmacological effects, is addressed by considering the three-dimensional geometry of the molecules. Conformational analytical concepts can be used to design new chemical entities and to assess structure-activity relationship hypotheses, and indeed this strategy has led to synthesis of new categories of potentially clinically valuable agents. Some conclusions are presented with respect to the combinations of atoms within the molecules in various chemical categories of dopaminergic agonists, which are responsible for the observed pharmacological effects. On the basis of these conclusions, some general properties of in vivo dopamine receptors are inferred, and proposals are advanced for structural analysis of the molecule of dopamine itself, which may be applicable to the design of new, superior therapeutic agents for those pathological conditions which are referable to the dopaminergic nervous system.

Publication Date

December 1986

Journal Title

Proceedings of the Iowa Academy of Science

Volume

93

Issue

4

First Page

167

Last Page

174

Copyright

© Copyright 1986 by the Iowa Academy of Science, Inc.

Language

EN

File Format

application/pdf

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