| 产品描述: | PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 4-8 nM and an IC50 of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility |
| 靶点: |
5-HT6 Receptor:4-8 nM (Ki);5-HT6 Receptor:19 nM (IC50);5-HT1A Receptor:420 nM (Ki);5-HT1B Receptor:260 nM (Ki);5-HT1D Receptor:2.8 μM (Ki);5-HT2A Receptor:2.5 μM (IC50);5-HT2B Receptor:2.5 μM (IC50);5-HT2C Receptor:3.7 μM (IC50);Dopamine D3 Receptor:71 nM (Ki);Histamine H2 Receptor:0.64 μM (Ki);Opioid μ Receptor:0.45 μM (Ki) |
| 体外研究: |
PRX-07034 is both a potent and highly selective 5-HT6 receptor antagonist (≥100-fold selectivity for the 5-HT6 receptor compared to 68 other GPCRs, ion channels, and transporters. PRX-07034 inhibits 5-HT1A, 5-HT1B, 5-HT1D, Dopamine D3, Histamine H2, and Opioid μ receptor with Kis of 420 nM, 260 nM, 2.8 µM, 71 nM, 0.64 µM, and 0.45 µM, respectively. PRX-07034 inhibits 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50s of 2.5 µM, 2.5 µM, and 3.7 µM, respectively. In functional assays, PRX-07034 demonstrates low antagonist activity for the dopamine D3 receptor (IC50=4.8 µM) and very low agonistic activity for the opioid μ-receptor (EC50=19 µM) . |
| 体内研究: |
PRX-07034 (0.1, 1, or 3 mg/kg; i.p.; 30 min prior to delayed spontaneous alternation testing) selectively enhances a switch to a place discrimination. Animal Model: Male Long-Evans rats weighing approximately 350 g Dosage: 0.1, 1, or 3 mg/kg Administration: Injected intraperitoneal Result: 1 and 3 mg/kg (but not 0.1 mg/kg) significantly enhanced delayed spontaneous alternation. The drug at 1 and 3 mg/kg also enhanced switching between a place and response strategy, but did not affect initial learning of either a place or response discrimination. |
| 参考文献: |
1. Eric G Mohler, et al. The effects of PRX-07034, a novel 5-HT6 antagonist, on cognitive flexibility and working memory in rats. Psychopharmacology (Berl). 2012 Apr;220(4):687-96. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.044 ml |
10.222 ml |
20.445 ml |
| 5 mM |
0.409 ml |
2.044 ml |
4.089 ml |
| 10 mM |
0.204 ml |
1.022 ml |
2.044 ml |
| 50 mM |
0.041 ml |
0.204 ml |
0.409 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。 |