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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Recent Advances in the Development of Dopamine D3 Receptor Agonists and Antagonists

Author(s): A. Michael Crider and Mark A. Scheideler

Volume 1, Issue 1, 2001

Page: [89 - 99] Pages: 11

DOI: 10.2174/1389557013407287

Abstract

Advances in molecular cloning techniques have allowed the characterization of five subtypes (D1 -D5 ) of dopamine (DA) receptors. The limbic location of the D3 receptor has led to speculation about its possible role in schizophrenia and drug abuse. Since the D 3 receptor is localized in the limbic region rather than the striatum, antipsychotics with D 3 receptor selectivity could be devoid of extrapyramidal side effects commonly seen with D 2 receptor antagonists. Recent work in our laboratory revealed that the benz(e)indole cis-(±)-44b demonstrated high selectivity for the D 3 receptor. This compound exhibits a typical antipsychotic profile without the motor effects found in commonly used antipsychotic agents. This mini-review will give a brief introduction on D 3 receptors and a detailed description of selectively-acting D 3 agonists and antagonists which have recently appeared in the literature.

Keywords: polymorphic forms, transmembrane segments, protonated amine group, substantia nigra, tricyclic analogs, pyrrolidinylmethylbenzamide, locomotor activity


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