| 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). |
| 靶点: |
5-HT Receptor;5-HTReceptor |
| 体外研究: |
CP-809101 is a potent, functionally selective 5-HT2C agonist that displays approximately 100% efficacy in vitro |
| 体内研究: |
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 |
| 参考文献: |
1. 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. 2. 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. 3. 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.neuroscience.2011.09.041. Epub 2011 Sep 24. 4. 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. |
| 溶解性: |
Soluble in H2O |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.931 ml |
14.653 ml |
29.305 ml |
| 5 mM |
0.586 ml |
2.931 ml |
5.861 ml |
| 10 mM |
0.293 ml |
1.465 ml |
2.931 ml |
| 50 mM |
0.059 ml |
0.293 ml |
0.586 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |