| 产品描述: | SNAP-94847 is a selective and competitive MCH1 receptor (MCH1-R) antagonist (Ki: 2.2 nM). It has anxiolytic and antidepressant activity and reduces food intake in mice. |
| 靶点: |
GPR; Melanin-concentrating Hormone Receptor (MCHR);GPR; Melanin-concentratingHormoneReceptor(MCHR) |
| 体外研究: |
SNAP-94847 showed a favorable combination of MCH1 receptor affinity (Ki: 2.2 nM) and human R1A receptor (>80-fold) and D2 (>500-fold) selectivity |
| 体内研究: |
SNAP-94847 (10 mg/kg, p.o.) had no effect on basal water consumption measured over 2 h: vehicle-treated (2.0 mL); 16g-treated (2.3 mL). MCH-evoked water intake was inhibited significantly by SNAP-94847 at doses of 1.0, 2.5, and 10 mg/kg. BALB/c mice treated for 21 days with fluoxetine or SNAP 94847 (20 mg/kg/day) showed marked increases in quinpirole-induced locomotor activity, with the onset of hyper-locomotion appearing earlier in the time course after SNAP 94847 compared to fluoxetine. Administration of either compound for 7 days was also sufficient to augment the quinpirole response in BALB/c mice. The intra-locus coeruleus and intracerebroventricular injections of melanin-concentrating hormone and chronic injections of corticosterone increased immobility time in the forced swim test and decreased sucrose preference in the sucrose preference test. All these depressive-like behaviors were reversed by an intra-locus coeruleus microinjection of SNAP-94847 |
| 参考文献: |
1. Ye H, et al. Melanin-Concentrating Hormone (MCH) and MCH-R1 in the Locus Coeruleus May Be Involved in the Regulation of Depressive-Like Behavior. Int J Neuropsychopharmacol. 2018 Dec 1;21(12):1128-1137. 2. Marsteller DA, et al. The MCH1 receptor antagonist SNAP 94847 induces sensitivity to dopamine D2/D3 receptor agonists in rats and mice. Eur J Pharmacol. 2009 Jan 5;602(1):66-72. 3. Chen CA, et al. Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits. J Med Chem. 2007 Aug 9;50(16):3883-90. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
2-8°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.09 ml |
10.448 ml |
20.896 ml |
| 5 mM |
0.418 ml |
2.09 ml |
4.179 ml |
| 10 mM |
0.209 ml |
1.045 ml |
2.09 ml |
| 50 mM |
0.042 ml |
0.209 ml |
0.418 ml |
|
| 注意: |
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