| Description | Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD). |
| In vitro | 帕罗西汀(4 mg/kg；i.p.)与NK1受体拮抗剂 Vofopitant/GR205171(30 mg/kg；i.p.)或L733060(40 mg/kg；i.p.)联合给药，增强了帕罗西汀对野生型小鼠皮层[5-HT]ext的影响，而 Vofopitant/GR205171(30 mg/kg；i.p.)对NK1受体敲除小鼠帕罗西汀诱导的皮层[5-HT]ext增加没有影响。当 Vofopitant/GR205171(300 micro mol/L)通过“逆向微透析”灌注到背侧丘脑核时，增强了帕罗西汀对皮层[5-HT]ext的影响，并抑制了帕罗西汀诱导的背侧丘脑核[5-HT]ext增加[2]。 |
| In vivo | 在T型迷宫中，Vofopitant(GR205171，30 mg/kg，s.c.)增加了对25秒延迟奖励的选择次数[3]。Vofopitant(GR205171，30 mg/kg，i.p.)增加了帕罗西汀处理的野生型小鼠额叶皮层中的细胞外5-HT水平，而不是在野生型小鼠和帕罗西汀处理的NK1受体敲除小鼠中增加[2]。 |
| Target activity | NK1 receptor (rat):9.5 (pKi), NK1 receptor (human):10.6 (pKi), NK1 receptor (ferret):9.8(pKi) |
| Synonyms | GR 205171 |
| molecular weight | 432.44 |
| Molecular formula | C21H23F3N6O |
| CAS | 168266-90-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 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. 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. 3. 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. |