The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
SELECTIVE BINDING OF YM-09151-2, A NEW POTENT NEUROLEPTIC, TO D2-DOPAMINERGIC RECEPTORS
Michio TERAIShinji USUDAIzumi KUROIWAOsamu NOSHIROHiroo MAENO
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1983 Volume 33 Issue 4 Pages 749-755

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Abstract
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 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 nueroleptics tested.
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