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
Mini-Reviews in Medicinal Chemistry
Title: Recent Advances in the Development of Dopamine D3 Receptor Agonists and Antagonists
Volume: 1 Issue: 1
Author(s): A. Michael Crider and Mark A. Scheideler
Affiliation:
Keywords: polymorphic forms, transmembrane segments, protonated amine group, substantia nigra, tricyclic analogs, pyrrolidinylmethylbenzamide, locomotor activity
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.
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Cite this article as:
Crider Michael A. and Scheideler A. Mark, Recent Advances in the Development of Dopamine D3 Receptor Agonists and Antagonists, Mini-Reviews in Medicinal Chemistry 2001; 1 (1) . https://dx.doi.org/10.2174/1389557013407287
DOI https://dx.doi.org/10.2174/1389557013407287 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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