The Classification of Dopamine Receptors: Relationship to Radioligand Binding

The Classification of Dopamine Receptors: Relationship to Radioligand Binding The past 25 years has seen our appreciation of the function of dopamine (DA) in the brain elevated from that of a precursor for norepinephrine to a neurotransmitter in its own right. The association of disturbances of dopaminergic neurotransmission with neurological and psychiatric disor­ ders has further emphasized the crucial role of this neurotransmitter in normal brain function.Dopaminergic agonists have a firmly established role in the treatment of Parkinson's disease and may be of value in the therapy of tardive dyskinesia.Dopaminergic antagonists have a longer history in the treatment of schizophrenia, Huntington's disease, and Gilles de la Touret­ te's syndrome. Since 1975, the elegantly simple radioligand binding technique has al­ lowed direct examination of the interactions of agonists and antagonists with putative dopamine receptors (DARs), and these studies form the major focus of this review. Such studies have complemented investigations ofDA regulation of adenylate cyclase activity and hormone release in various tissues. Although problems remain, the correspondence between such radi­ oligand binding sites and functional DARs is steadily being established. These experiments have clearly dividedDARs into distinct subtypes, much as was done earlier for the alpha and beta adrenergic receptors. These findings will have a profound effect on http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Annual Review of Neuroscience Annual Reviews

The Classification of Dopamine Receptors: Relationship to Radioligand Binding

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Publisher
Annual Reviews
Copyright
Copyright 1983 Annual Reviews. All rights reserved
Subject
Review Articles
ISSN
0147-006X
eISSN
1545-4126
D.O.I.
10.1146/annurev.ne.06.030183.000355
Publisher site
See Article on Publisher Site

Abstract

The past 25 years has seen our appreciation of the function of dopamine (DA) in the brain elevated from that of a precursor for norepinephrine to a neurotransmitter in its own right. The association of disturbances of dopaminergic neurotransmission with neurological and psychiatric disor­ ders has further emphasized the crucial role of this neurotransmitter in normal brain function.Dopaminergic agonists have a firmly established role in the treatment of Parkinson's disease and may be of value in the therapy of tardive dyskinesia.Dopaminergic antagonists have a longer history in the treatment of schizophrenia, Huntington's disease, and Gilles de la Touret­ te's syndrome. Since 1975, the elegantly simple radioligand binding technique has al­ lowed direct examination of the interactions of agonists and antagonists with putative dopamine receptors (DARs), and these studies form the major focus of this review. Such studies have complemented investigations ofDA regulation of adenylate cyclase activity and hormone release in various tissues. Although problems remain, the correspondence between such radi­ oligand binding sites and functional DARs is steadily being established. These experiments have clearly dividedDARs into distinct subtypes, much as was done earlier for the alpha and beta adrenergic receptors. These findings will have a profound effect on

Journal

Annual Review of NeuroscienceAnnual Reviews

Published: Mar 1, 1983

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