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• W1967603237 abstract "YM992, (S)-2-[[(7-fluoro-4-indanyl)oxy]methyl]morpholine monohydrochloride, exhibited the biochemical profile of a selective serotonin (5-HT) reuptake inhibitor (SSRI) with 5-HT2A receptor antagonistic activity. YM992 showed the same high affinity as fluoxetine against the 5-HT reuptake site (Ki=21 nM) and a similar affinity to that of trazodone against the 5-HT2A receptor (Ki=86 nM). In other receptor binding studies, an affinity for the adrenergic cell α1 receptor (Ki=200 nM) and 5-HT2C receptor (Ki=680 nM) was observed. In a monoamine uptake study, YM992 showed a selective 5-HT uptake inhibition (IC50=0.15 μM), but only very weakly inhibited both noradrenaline (NA) and dopamine (DA) uptake (IC50=3.1 μM (NA), >10 μM (DA)). YM992 was also found to potently inhibit the aggregation of human platelets (IC50=1.9 μM), revealing antagonistic activity for the 5-HT2A receptor in vitro. Enhanced serotonergic neurotransmission, in particular that mediated by the 5-HT1A receptor, has recently been reported to be important in the long-term treatment of depressive disorders with antidepressants. In addition, some 5-HT1A receptor-mediated responses are known to be potentiated by co-administration of 5-HT2A receptor antagonists. Thus, YM992, having both selective 5-HT reuptake inhibition and 5-HT2A antagonistic activity, might show potent therapeutic activity as a novel antidepressant in comparison with conventional SSRIs." @default.
• W1967603237 created "2016-06-24" @default.
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• W1967603237 date "1996-01-01" @default.
• W1967603237 modified "2023-10-03" @default.
• W1967603237 title "Biochemical profile of YM992, a novel selective serotonin reuptake inhibitor with 5-HT2A receptor antagonistic activity" @default.
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• W1967603237 doi "https://doi.org/10.1016/s0028-3908(96)00079-2" @default.
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