NDLI: Identification, characterization, and localization of the dopamine D3 receptor in rat brain using 7-[3H]hydroxy-N,N-di-n-propyl-2-aminotetralin.

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Identification, characterization, and localization of the dopamine D3 receptor in rat brain using 7-[3H]hydroxy-N,N-di-n-propyl-2-aminotetralin.

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Identification, characterization, and localization of the dopamine D3 receptor in rat brain using 7-[3H]hydroxy-N,N-di-n-propyl-2-aminotetralin.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Diaz, J. Sokoloff, P. Lévesque, D. Souil, E. Schwartz, J. C. Schott, D. Pilon, C. Giros, B. Martres, M. P. Morgat, J. L.
Description	Author Affiliation: Lévesque D ( Unité de Neurobiologie et Pharmacologie (U. 109) de l'Institut National de la Santé et de la Recherche Médicale, Paris, France.);
Abstract	We have identified 7-[3H]hydroxy-N,N-di-n-propyl-2-aminotetralin ([3H]7-OH-DPAT) as a selective probe for the recently cloned dopamine D3 receptor and used it to assess the presence of this receptor and establish its distribution and properties in brain. In transfected Chinese hamster ovary (CHO) cells, it binds to D3 receptors with subnanomolar affinity, whereas its affinity is approximately 100-, 1000-, and 10,000-fold lower at D2, D4, and D1 receptors, respectively. Specific [3H]7-OH-DPAT binding sites, with a Kd of 0.8 nM and a pharmacology similar to those at reference D3 receptors of CHO cells, were identified in rat brain. D3 receptors differ from D2 receptors in brain by their lower abundance (2 orders of magnitude) and distribution, restricted to a few mainly phylogenetically ancient areas--e.g., paleostriatum and archicerebellum--as evidenced by membrane binding are autoradiography studies. Native D3 receptors in brain are characterized by an unusually high nanomolar affinity for dopamine and a low modulatory influence of guanyl nucleotides on agonist binding. These various features suggest that D3 receptors are involved in a peculiar mode of neurotransmission in a restricted subpopulation of dopamine neurons.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	17
Volume Number	89
Language	English
Publisher	National Academy of Sciences
Publisher Date	1992-10-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Brain Metabolism Receptors, Dopamine Tetrahydronaphthalenes Pharmacology Animals Brain Mapping Cell Membrane Cells, Cultured Drug Design Gene Expression In Vitro Techniques Nucleic Acid Hybridization RNA, Messenger Genetics Rats, Inbred Strains Sulpiride Analogs & Derivatives Research Support, Non-U.S. Gov't Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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