CP-809101 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CP-809101 盐酸盐是一种有效的选择性 5-HT2C 受体激动剂（对于人 5-HT2C/5-HT2B/5-HT2A 受体，pEC50: 9.96/7.19/6.81）。

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).(In Vitro):CP-809101 is a potent, functionally selective 5-HT2C agonist that displays approximately 100% efficacy in vitro.(In Vivo):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.

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CP-809101 hydrochloride (0.1-56 mg/kg; s.c.; single) inhibits the conditioned avoidance response of rats in a dose-dependent manner.CP-809101 hydrochloride (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 hydrochloride (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 hydrochloride (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.

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Endocrinology/Hormones

5-HT Receptor

NMDA

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1215721-40-6

341.24

C15H18Cl2N4O

>98% (HPLC)

In Vitro:?H2O : 20 mg/mL (58.61 mM)

Cl.Clc1cccc(COc2cncc(n2)N2CCNCC2)c1

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(-20℃)

With Ice Pack

≥ 2 years