SELECTIVE BINDING OF YM-09151-2, A NEW POTENT NEUROLEPTIC, TO D₂-DOPAMINERGIC RECEPTORS

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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 (α₁-adrenergic, α₂-adrenergic, β-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 K_i 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 nueroleptics tested.