Direct effect of a nomifensine derivative on dopamine receptors.
A study was made of the effects of nomifensine, 4'-hydroxynomifensine and 3',4'-dihydroxynomifensine on dopamine receptors in rat striatum and nucleus accumbens, using the dopamine-sensitive adenylate cyclase assay. Nomifensine and its 4'-hydroxy metabolite were both inactive as dopaminergic agonists. 3',4'-dihydroxynomifensine was, however, a potent agonist, being approximately 2 to 4 times less active than dopamine. The effects of dopamine and of 3',4'-dihydroxynomifensine were blocked by fluphenazine. It is concluded that the dopaminergic activity of 3',4'-dihydroxynomifensine is dependent upon the presence of the two hydroxyl groups.
D000262:Adenylyl Cyclases / Q000378:metabolism; D000818:Animals; D001921:Brain / Q000201:enzymology; D003342:Corpus Striatum / Q000378:metabolism; D000242:Cyclic AMP / Q000378:metabolism; D005260:Female; D005476:Fluphenazine / Q000494:pharmacology; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000494:pharmacology*; D009627:Nomifensine / Q000031:analogs & derivatives / Q000494:pharmacology*; D009714:Nucleus Accumbens / Q000378:metabolism; D051381:Rats; D011954:Receptors, Dopamine / Q000187:drug effects*
D007546:Isoquinolines; D011954:Receptors, Dopamine; D009627:Nomifensine; D000242:Cyclic AMP; D000262:Adenylyl Cyclases; D005476:Fluphenazine