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CP-809101
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CP-809101图片
CAS NO:479683-64-2
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
CP-809101 是一种有效且高度选择性的 5-HT2C 受体激动剂，对人 5HT2C、5HT2B 和 5HT2A 受体的 pEC50 分别为 9.96、7.19 和 6.81 M。
Cas No.479683-64-2
别名6'-(3-氯苄基氧基)-3,4,5,6-四氢-2H-[1,2']联吡嗪,CP809101;CP 809101
化学名2-((3-chlorobenzyl)oxy)-6-(piperazin-1-yl)pyrazine
Canonical SMILESClC1=CC=CC(COC2=NC(N3CCNCC3)=CN=C2)=C1
分子式C15H17ClN4O
分子量304.77
溶解度DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 2 mg/ml,PBS (pH 7.2): 0.1 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CP-809101 is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively. IC50 Value: 9.96(pEC50 for 5-HT2C); 7.19(pEC50 for 5-HT2B); 6.81(pEC50 for 5-HT2A)Target: 5-HT2C ReceptorCP-809101 is a potent, functionally selective 5-HT2C agonist that displays approximately 100% efficacy in vitro. The aim of the present studies was to assess the efficacy of a selective 5-HT2C agonist in animal models predictive of antipsychotic-like efficacy and side-effect liability. 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. Thus, the present results demonstrate that the 5-HT2C agonist, CP-809101, has a pharmacological profile similar to that of the atypical antipsychotics with low extrapyramidal symptom liability. CP-809101 was inactive in two animal models of antidepressant-like activity, the forced swim test and learned helplessness.

References:
[1]. Higgins GA, Silenieks LB, Lau W, et al. Evaluation of chemically diverse 5-HT2C receptor agonists on behaviours motivated by food and nicotine and on side effect profiles. Psychopharmacology (Berl). 2013 Apr;226(3):475-90.
[2]. Strong PV, Christianson JP, Loughridge AB, et al. 5-hydroxytryptamine 2C receptors in the dorsal striatum mediate stress-induced interference with negatively reinforced instrumental escape behavior. Neuroscience. 2011 Dec 1;197:132-44. doi: 10.1016/j.neur
[3]. Fletcher PJ, Tampakeras M, Sinyard J et al. Characterizing the effects of 5-HT(2C) receptor ligands on motor activity and feeding behaviour in 5-HT(2C) receptor knockout mice. Neuropharmacology. 2009 Sep;57(3):259-67. doi: 10.1016/j.neuropharm.2009.05.011
[4]. Siuciak JA, Chapin DS, McCarthy SA, et al. CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity. Neuropharmacology. 2007 Feb;52(2):279-90.