INABIS '98 - Characterization of Quinpirole-Stimulated [35S] GTPgammaS Binding at D2-like Receptors in Rat Striatum.

Characterization of Quinpirole-Stimulated [35S] GTPgammaS Binding at D2-like Receptors in Rat Striatum.
Gilliland, S. (Department of Pharmacology, University of Kansas Medical Center, USA)
Alper, R. (Department of Pharmacology, University of Kansas Medical Center, USA)
Levant, B. (Department of Pharmacology, University of Kansas Medical Center, USA)

Contact Person: Sarah L. Gilliland (sgillila@kumc.edu)

Abstract

Quinpirole, (LY171555) is a selective agonist for D2-like receptors and belongs to the class of dopaminergic ergolines. Stimulation of [35S]GTPgammaS binding by quinpirole at D2-like receptors was characterized in rat striatal membranes. The optimized assay contained ~50mg protein, 300microM GDP, and 0.1nM [35S] GTPgS, incubated at 37oC for 20 minutes. Quinpirole produced a maximal stimulation of 39.8 + 0.9% above basal with an EC50 of 8505 + 700 nM. Antagonists inhibited quinpirole-stimulated [35S]GTPgammaS binding with the following rank order of potency: spiperone > haloperidol > clozapine > ketanserin > SCH 23390. This pharmacological profile concurs with that for D2-like receptors in radioligand binding studies. This indicates that quinpirole-stimulated [35S]GTPgammaS binding should be a useful tool for studying functional interactions at D2-like receptors.

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Poster Number PAgilliland0401
Keywords: quinpirole, d2 receptors, gtpgammas binding, rat striatum

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Gilliland, S.; Alper, R.; Levant, B.; (1998). Characterization of Quinpirole-Stimulated [35S] GTPgammaS Binding at D2-like Receptors in Rat Striatum.. Presented at INABIS '98 - 5th Internet World Congress on Biomedical Sciences at McMaster University, Canada, Dec 7-16th. Available at URL http://www.mcmaster.ca/inabis98/neuropharm/gilliland0401/index.html