现货大促销,价格低至8折起,量大更优惠,详细咨询客服
全部分类
全部分类
  • CP-809101
CP-809101的可视化放大

CP-809101

A potent 5-HT2C receptor agonist

原价
¥1037-4025
价格
830-3220
CP-809101的二维码

所有产品仅用于科学研究,我们不为任何个人用途提供产品和服务

询价有惊喜,量大更优惠 点击这里给我发消息

  • 库存: 现货
可选包装 >>>
首页
  • 货号: ajci18608
  • CAS: 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
  • 分子式: C15H17ClN4O
  • 分子量: 304.77
  • 纯度: >98%
  • 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: Store at -20°C
  • 库存: 现货

Background

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.


参考文献:
[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.

动态评分

0.0

没有评分数据
没有评价数据
一键回到顶部
展开 收缩
安捷凯在线客服