Highlights of D1 dopamine receptor antagonist research.
SCH 39166 is now undergoing clinical trials in schizophrenics as a selective D1 dopamine receptor antagonist. It differs from SCH 23390, the prototype D1 receptor antagonist, by having reduced affinity for serotonin receptors and a longer duration of action in primates, as measured in the squirrel monkey conditioned avoidance paradigm. Further studies on this difference in primates indicates that it may be attributable to reduced affinity of SCH 39166 compared to SCH 23390 for the hepatic glucuronosyltransferase system. Their affinities are similar in rats, a species in which both have similar duration of action. These and other studies presented are consistent with the novel profile of SCH 39166.
Barnett
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Schering-Plough Research, Bloomfield, NJ 07003.
McQuade
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Tedford
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D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects; D001552:Benzazepines / Q000378:metabolism* / Q000494:pharmacology; D001667:Binding, Competitive; D014453:Glucuronosyltransferase / Q000378:metabolism; D008099:Liver / Q000201:enzymology; D008861:Microsomes / Q000201:enzymology; D051381:Rats; D017447:Receptors, Dopamine D1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D012106:Research; D012453:Saimiri
D001552:Benzazepines; D017447:Receptors, Dopamine D1; D011985:Receptors, Serotonin; C058081:ecopipam; D014453:Glucuronosyltransferase