产品
编 号:F366955
分子式:C15H17ClN4O
分子量:304.77
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CAS No: 479683-64-2
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生物活性:
CP-809101 is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A 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.
体内研究:
CP-809101 (0.1-56 mg/kg; s.c.; single) inhibits the conditioned avoidance response of rats in a dose-dependent manner.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).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.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.Animal Model:Male CF rats (conditioned avoidance responding (CAR) model).
Dosage:0.1-56 mg/kg
Administration:Subcutaneous injection; single.
Result:Resulted in a dose-dependent inhibition of the conditioned avoidance response with an ID50 value of 4.8 mg/kg.
Animal Model:Male CD rats (PCP or d-amphetamine-induced hyperactivity model).
Dosage:0.56, 1.78, 5.6, 17.8 mg/kg
Administration:Subcutaneous injection; single.
Result:Antagonized PCP-induced hyperactivity, with an ED50 value of 2.4 mg/kg.Antagonized d-amphetamine-induced hyperactivity, with an ED50 value of 2.7 mg/kg, and in a dose-dependent manner.
Animal Model:Male CD rats (spontaneous locomotor model).
Dosage:0.56, 1.78, 5.6, 17.8 mg/kg
Administration:Subcutaneous injection; single.
Result:Inhibited spontaneous locomotor activity in a dose-dependent manner (ED50=2.7 mg/kg).
Animal Model:Adult male Sprague-Dawley rats (280-400 g).
Dosage:0.3, 1, 3 mg/kg
Administration:Subcutaneous injection; single.
Result:Produced a dose-related decrease in responding for food and nicotine self-administration in rats.