Sulpiride isomers exhibit reversed stereospecificity for D-1 and D-2 dopamine receptors in the CNS.
We have investigated the stereospecificity of the interaction of (-) and (+)sulpiride with [3H]cis-flupentixol and [3H]spiperone binding to D-1 and D-2 dopamine receptors respectively in rat striatum. Both isomers of sulpiride compete more potently at D-2 vs. D-1 dopamine receptors. (-)Sulpiride is 50-fold more potent than (+)sulpiride in blocking D-2 receptors, while (+)sulpiride is 3-fold more potent than (-)sulpiride at D-1 receptors. This reversed stereospecificity of sulpiride interactions with CNS D-1 and D-2 dopamine receptors is similar to the stereospecificity of sulpiride interactions at DA1 and DA2 dopamine receptors in peripheral vascular beds.
D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects*; D003342:Corpus Striatum / Q000378:metabolism; D005475:Flupenthixol / Q000494:pharmacology; D066298:In Vitro Techniques; D051381:Rats; D011954:Receptors, Dopamine / Q000187:drug effects*; D013134:Spiperone / Q000494:pharmacology; D013237:Stereoisomerism; D013469:Sulpiride / Q000494:pharmacology*
D011954:Receptors, Dopamine; D013134:Spiperone; D013469:Sulpiride; D005475:Flupenthixol