CP-809101 hydrochloride 是选择性 5-HT2C 受体激动剂,对于人类 5-HT2C/5-HT2B/5-HT2A 受体。
产品描述
CP-809101 hydrochloride is a potent and selective 5-HT2C receptor agonist (pEC50: 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors).
体外活性
CP-809101 is a potent, functionally selective 5-HT2C agonist that displays approximately 100% efficacy in vitro[4].
体内活性
Similar to currently available antipsychotic drugs, CP-809101 dose-dependently inhibited conditioned avoidance responding (CAR, ED50 = 4.8 mg/kg, sc). CP-809101 antagonized both PCP- and d-amphetamine-induced hyperactivity with ED50 values of 2.4 and 2.9 mg/kg (sc), respectively, and also reversed an apomorphine induced-deficit in prepulse inhibition. At doses up to 56 mg/kg, CP-809101 did not produce catalepsy. CP-809101 was inactive in two animal models of antidepressant-like activity, the forced swim test, and learned helplessness[4].
Cas No.
1215721-40-6
分子式
C15H18Cl2N4O
分子量
341.24
别名
CP-809101 hydrochloride
储存和溶解度
H2O:20 mg/mL (58.61 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years