| 产品描述： | Pimavanserin (ACP-103) hemitartrate is a potent 5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively. |
| 靶点： |
5-HT2A Receptor:8.73 (pIC50);5-HT2A Receptor:9.3 (pKi) |
| 体内研究： |
Pimavanserin hemitartrate attenuates head-twitch behavior (3 mg/kg p.o.), and prepulse inhibition deficits (1-10 mg/kg s.c.) induced by the 5-HT2A receptor agonist in rats and reduces the hyperactivity induced in mice by the N-methyl-D-aspartate receptor noncompetitive antagonist, consistent with a 5-HT 2A receptor mechanism of action in vivo and antipsychotic-like efficacy. Pimavanserin hemitartrate demonstrates 42.6% oral bioavailability in rats |
| 参考文献： |
1. Vanover KE, et al. Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP- 103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist. J Pharmacol Exp Ther. 2006 May;317(2):910-8. |
| 溶解性： |
DMSO : ≥ 75 mg/mL (149.23 mM) H2O : 50 mg/mL (99.48 mM; Need ultrasonic) |
| 保存条件： |
RT |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
0.995 ml |
4.974 ml |
9.948 ml |
| 5 mM |
0.199 ml |
0.995 ml |
1.99 ml |
| 10 mM |
0.099 ml |
0.497 ml |
0.995 ml |
| 50 mM |
0.02 ml |
0.099 ml |
0.199 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京