| 靶点: |
pKi: 10.6 (Human NK1 receptor), 9.5 (Rat NK1 receptor), 9.8 (Ferret NK1 receptor) |
| 体内研究: |
Vofopitant (GR205171, 30 mg/kg, s.c.) increases the number of choices of the 25-s delayed reward in a T-maze. Vofopitant (GR205171, 30 mg/kg, i.p.) increases the extracellular 5-HT levels in the frontal cortex of paroxetine-treated wild-type mice, rather than in wild-type mice and paroxetine-treated NK1 receptor knockout mice. |
| 参考文献: |
1. Gardner CJ, et al. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53. 2. Loiseau F, et al. Antidepressant-like effects of agomelatine, melatonin and the NK1 receptor antagonist GR205171 in impulsive-related behaviour in rats. Psychopharmacology (Berl). 2005 Oct;182(1):24-32. Epub 2005 Sep 29. 3. Guiard BP, et al. Blockade of substance P (neurokinin 1) receptors enhances extracellular serotonin when combined with a selective serotonin reuptake inhibitor: an in vivo microdialysis study in mice. J Neurochem. 2004 Apr;89(1):54-63. |
| 保存条件: |
RT |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.312 ml |
11.562 ml |
23.124 ml |
| 5 mM |
0.462 ml |
2.312 ml |
4.625 ml |
| 10 mM |
0.231 ml |
1.156 ml |
2.312 ml |
| 50 mM |
0.046 ml |
0.231 ml |
0.462 ml |
|
| 注意: |
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