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Beschreibung

A selective, brain-penetrant 5-HT2C receptor antagonist (pKi 8.2-9.0 ), with some effects on the 5-HT2B receptor (pKi 6.8-7.0) and 5-HT2A receptor (pKi 6.1-6.8). SB 242084 has been shown to increase the effectiveness of the selective serotonin reuptake inhibitor (SSRI) class of antidepressants, and may also reduce their side effects. In animal studies, SB-242,084 produced stimulant-type activity and reinforcing effects, somewhat similar to but much weaker than cocaine or amphetamines. In vivo (ocular) IC50 values reported at 2.08 µ,M.