Selective binding of YM-09151-2, a new potent neuroleptic, to D2-dopaminergic receptors.
Effects of YM-09151-2 and five other neuroleptics (haloperidol, spiperone, chlorpromazine, sulpiride and clozapine) on the binding of [3H]-ligands to nine different receptors (alpha 1-adrenergic, alpha 2-adrenergic, beta-adrenergic, muscarinic, D2-dopaminergic, H1-histaminergic, 5HT1-serotonergic, 5HT2-serotonergic and opiate receptors) and on dopamine-sensitive adenylate cyclase were determined using brain membranes in the rat, guinea-pig and dog. The affinity of YM-09151-2 for D2-receptors with a Ki value of 0.1 nM was more than 1000-times higher than that for the other receptors and dopamine-sensitive adenylate cyclase, and it was the greatest among the neuroleptics tested.
D000262:Adenylyl Cyclases / Q000378:metabolism; D000818:Animals; D014150:Antipsychotic Agents / Q000378:metabolism*; D001549:Benzamides / Q000378:metabolism*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D008566:Membranes / Q000378:metabolism; D011506:Proteins / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000378:metabolism*; D013134:Spiperone / Q000378:metabolism
D014150:Antipsychotic Agents; D001549:Benzamides; D011506:Proteins; D011954:Receptors, Dopamine; D013134:Spiperone; D000262:Adenylyl Cyclases; C030265:nemonapride