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BTS-54-505 is an active metabolite of sibutramine.1 It inhibits norepinephrine, serotonin (5-HT), and dopamine uptake in rat cortical synaptosomes (IC50s = 0.066, 5.1, and 0.61 µM, respectively). In vivo, BTS-54-505 prevents reserpine-induced ptosis in rats (ED50 = 3.7 mg/kg) and decreases immobility in the Porsolt learned helplessness test in mice when administered at a dose of 10 mg/kg. BTS-54-505 (10 mg/kg) increases colonic temperature, a marker of thermogenesis, and decreases food intake in rats.2
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1. The contribution of metabolites to the rapid and potent down-
2. Mechanism of the thermogenic effect of Metabolite 2 (BTS 54 505), a major pharmacologically active metabolite of the novel anti-