摘要：This study assessed the specificity of displacement potencies of MCI-9042 ((±)-1-[o-[2-(m-methoxyphenyl)ethyl]phenoxy]-3-(dimethylamino)-2-propyl hydrogen succinate hydrochloride), a new antiplatelet agent, in [3H]4-bromo-2, 5-dimethoxyphenylisopropylamine ([3H]DOB) and [3H] ketanserin binding to 5HT2-serotonergic receptors in the rat brain using the radioligand binding method. The assessment of the displacement potencies of MCI-9042 and its derivative, M-1 (((±)-1-[2-(3-methoxyphenyl) ethyl] phenoxy]-3-(dimethylamino)-2-propanol)hydrochloride), on α1-, α2-, β-adrenergic, 5HT1-, 5HT2- and muscarinic receptors were also studied. MCI-9042 and M-1 showed strong displacement effects to 5HT2-receptors using [3H] DOB binding and [3H] ketanserin binding sites, and weak displacement effects for [3H] serotonin, [3H] prazosin, [3H] p-aminoclonidine, [3H] CGP12177 and [3H] QNB binding to 5HT1-, α1-, α2-, β-adrenergic receptors and muscarinic receptors. Thus, the present study suggests that MCI-9042 is specific for 5HT2-receptor.
