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

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

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 1 , Issue 1 , 2001

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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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Article Details

Year: 2001
Page: [89 - 99]
Pages: 11
DOI: 10.2174/1389557013407287

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