CP-809,101 is a potent and high-affinity 5-hydroxytryptamine receptor 2C (5-HT2C) full agonist with only weaker partial agonist activity toward 5-HT2A & 5-HT2B (cellular Ca2+ mobilization EC50 in nM/efficiency = 0.11/93% and 0.06/97% with human and rat 5-HT2C, respectively; 153/67%/human 5HT2A, 65.3/57%/human 5HT2B, 119/79%/rat 5HT2A) and much reduced or little affinity toward other receptors, ion channels and uptake sites tested. CP-809,101 exhibits antipsychotic efficacy in reducing conditioned avoidance response/CAR (ED50 = 4.8 mg/kg s.c.) and locomotor activity (ED50 in mg/kg via s.c. = 2/rats, 1/mice; no effect up to 10 mg/kg in 5-HT2C-knockout mice), while oral administration is reported to suppress spontaneous and nocturnal food intake as well as fasting-induced refeeding in rats (∼8% and ∼24% reduction of cumulative food intake and body weight in 4 days, respectively; 30 mg/kg/day p.o.).
Drug metabolism and disposition: the biological fate of chemicals, 35(6), 848-858 (2007-03-09)
2-(3-Chlorobenzyloxy)-6-(piperazin-1-yl)pyrazine (3) is a potent and selective 5-HT(2C) agonist that exhibits dose-dependent inhibition of food intake and reduction in body weight in rats, making it an attractive candidate for treatment of obesity. However, examination of the genotoxicity potential of 3
CP-809,101 is a potent, functionally selective 5-HT(2C) agonist that displays approximately 100% efficacy in vitro. The aim of the present studies was to assess the efficacy of a selective 5-HT(2C) agonist in animal models predictive of antipsychotic-like efficacy and side-effect
5-HT(2C) receptor agonists have considerable therapeutic potential, however there is little in vivo data to compare the potency and selectivity of 5-HT(2C) receptor agonists. Since 5-HT(2C) receptor agonists reduce locomotor activity and food intake, changes in these drug-induced behaviours in
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