A. Crider, P. H. Andersen, S. Cruse
Jun 1, 1992
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Influential Citations
8
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Journal
European Journal of Medicinal Chemistry
Abstract
A variety of 3-phenylpyrrolidines were synthesized and evaluated for their dopamine binding affinity in rat striatal tissue in vitro using [3H] SCH 23390 and [3H] spiperone as the D1 and D2 selective radioligands, respectively. Maximal D1 and D2 receptor binding affinity occurs with a n-pentyl group on the pyrrolidine ring nitrogen. Introduction of a trans methyl group at the 4-position of the ring decreases both D1 and D2 binding affinity. However, a cis 4-methyl group increases D1 receptor selectivity when the pyrrolidine ring is substituted with a n-propyl group. 3-Phenylpyrrolidines having a catechol nucleus exhibit greater affinity at both D1 and D2 receptors than meta-hydroxyphenyl derivatives