CP-809101

CP-809101 is a potent and highly selective 5-HT_2C receptor agonist, with pEC₅₀s of 9.96, 7.19 and 6.81 M for human 5HT_2C, 5HT_2B and 5HT_2A receptor. CP-809101 inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence^[1][2]. In Vivo: CP-809101 (0.1-56 mg/kg; s.c.; single) inhibits the conditioned avoidance response of rats in a dose-dependent manner^[1].
CP-809101 (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) antagonizes PCP (phencyclidine hydrochloride)-induced and d-amphetamine-induced hyperactivity (the latter in a dose-dependent manner)^[1].
CP-809101 (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) dose-dependently decreases spontaneous locomotor activity with an ED₅₀ value of 2.2 mg/kg^[1].
CP-809101 (0.3, 1, 3 mg/kg; s.c.; single) reduces responding for both nicotine and food and blocked the discriminative stimulus properties of nicotine^[2].