| 产品描述: | Pardoprunox (SLV-308) hydrochloride is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC50s of 8, 9.2, and 6.3, respectively |
| 靶点: |
5-HT1A Receptor:6.3 (pEC50);D2 Receptor:8 (pEC50);D3 Receptor:9.2 (pEC50);DopamineReceptor;5-HTReceptor;AdrenergicReceptor |
| 体外研究: |
Pardoprunox (SLV-308) hydrochloride acts as a potent but partial D2 receptor agonist (pEC50= 8.0 and pA2=8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D3 receptors, Pardoprunox hydrochloride acts as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC50=9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA2=9.0). Pardoprunox hydrochloride acts as a full 5-HT1A receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT1A receptors but with low potency (pEC50=6.3). |
| 参考文献: |
1. Glennon JC, et al. In vitro characterization of SLV308 (7-[4-methyl-1-piperazinyl]-2(3H)-benzoxazolone, monohydrochloride): a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist. Synapse. 2006 Dec 15;60(8):599-608. 2. Jones CA, et al. An in vivo pharmacological evaluation of pardoprunox (SLV308)--a novel combined dopamine D(2)/D(3) receptor partial agonist and 5-HT(1A) receptor agonist with efficacy in experimental models of Parkinson's disease. Eur Neuropsychopharmacol. 2010 Aug;20(8):582-93. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.707 ml |
18.537 ml |
37.074 ml |
| 5 mM |
0.741 ml |
3.707 ml |
7.415 ml |
| 10 mM |
0.371 ml |
1.854 ml |
3.707 ml |
| 50 mM |
0.074 ml |
0.371 ml |
0.741 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。 |