Journal article

PSYCHOTOMIMETIC OPIATE RECEPTORS LABELED AND VISUALIZED WITH ( )-[H-3]3-(3-HYDROXYPHENYL)-N-(1-PROPYL)PIPERIDINE

BL LARGENT, AL GUNDLACH, SH SNYDER

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES | NATL ACAD SCIENCES | Published : 1984

Abstract

3-(3-Hydroxyphenyl)-N-(1-propyl)piperidine (3-PPP) has been proposed as a selective dopamine autoreceptor agonist in the central nervous system. This report describes the pharmacology and localization of specific high-affinity binding sites for (+)-[3H]3-PPP in brain. The drug specificity of (+)-[3H]3-PPP binding is identical to that of sigma receptors, which may mediate psychotomimetic effects of some opiates. Haloperidol and the opioid derivatives, pentazocine, cyclazocine, and SKF 10,047 are potent inhibitors of (+)-[3H]3-PPP binding. Stereoselectivity is exhibited for the (+) isomers of cyclazocine and SKF 10,047 at the sigma site, opposite to the stereoselectivity seen at mu, delta, and..

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