Open AccessSelective binding of YM-09151-2, a new potent neuroleptic, to D2-dopaminergic receptors.
Author(s) -
Michio Terai,
Shinji Usuda,
Izumi Kuroiwa,
Osamu Noshiro,
Hiroo Maeno
Publication year - 1983
Publication title -
japanese journal of pharmacology/japanese journal of pharmacology
Language(s) - English
Resource type - Journals
eISSN - 1347-3506
pISSN - 0021-5198
DOI - 10.1254/jjp.33.749
Subject(s) - spiperone , dopaminergic , chemistry , dopamine receptor , endocrinology , sulpiride , 5 ht2 receptor , medicine , pharmacology , dopamine receptor d2 , receptor , chlorpromazine , dopamine , serotonin , 5 ht receptor
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.