A comparison of the effects on central 5-HT functions of sibutramine hydrochloride and other weight-modifying agents

摘要

Effects on 5-HT function of sibutramine and its active metabolites, BTS 54 354 and BTS 54 505, were compared with fluoxetine, (+)-fenfluramine and (+)-amphetamine. In vitro sibutramine weakly inhibited [~3H]-5-HT uptake into brain synaptosomes. BTS 54 354, BTS 54 505 and fluoxetine were powerful [~3H]-5-HT uptake inhibitors. Whereas (+)-fenfluramine and (+)-amphetamine were very much weaker. Conversely, whilst sibutramine, its metabolites and fluoxetine did not release [~3H]-5-HT from brain slices at ≤10~-5M, (+)-fenfluramine and (+)-amphetamine concentration-dependently increase[~3H]-5-HT release.