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

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 (α1-adrenergic, α2-adrenergic, β-adrenergic, muscarinic, D2-dopaminergic, H1-histaminergic, 5HT1-serotonergic, 5HT2-serotoner...

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Veröffentlicht in:Japanese journal of pharmacology 1983, Vol.33(4), pp.749-755
Hauptverfasser: TERAI, Michio, USUDA, Shinji, KUROIWA, Izumi, NOSHIRO, Osamu, MAENO, Hiroo
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container_issue 4
container_start_page 749
container_title Japanese journal of pharmacology
container_volume 33
creator TERAI, Michio
USUDA, Shinji
KUROIWA, Izumi
NOSHIRO, Osamu
MAENO, Hiroo
description 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.
doi_str_mv 10.1254/jjp.33.749
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title SELECTIVE BINDING OF YM-09151-2, A NEW POTENT NEUROLEPTIC, TO D2-DOPAMINERGIC RECEPTORS
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