Neuropharmacology Poster Session
Alper, R. (Department of Pharmacology, University of Kansas Medical Center, USA)
Levant, B. (Department of Pharmacology, University of Kansas Medical Center, USA)
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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|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|
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