| 产品描述: | SNAP 94847 hydrochloride 是一种具有抗抑郁样活性的新型高亲和力选择性黑色素浓缩激素受体1 (MCHR1) 拮抗剂。SNAP 94847 hydrochloride 以高亲和力结合大小鼠 MCHR1,与其他 GPCR,离子通道,酶和转运蛋白具有最小的交叉反应性。SNAP 94847 hydrochloride 是 MCH 诱发的肌醇磷酸形成的高亲和力拮抗剂 (pA2=7.81)。 |
| 靶点: |
Ki: 2.2 nM (MCHR1); Kd: 530 pM (MCHR1) |
| 体内研究: |
SNAP 94847 hydrochloride (oral gavage; 20 mg/kg; 14 days) shows an exaggerated locomotor response to acute quinpirole [treatment: F(2,19)=11.31, treatment × time: F(34,323) = 4.061], the effect of SNAP 94847 on quinpirole-evoked ambulations over the entire observation period is significant compared to the untreated animals. SNAP 94847 hydrochloride (oral administration; 20 mg/kg; 21 days) in drink water, produces a significant increase in ambulation relative to untreated animals [treatment: F(3,28) = 8.971; treatment × time: F(51,476)=11.50]. shows a marked increase in locomotion is apparent after 40 min in the SNAP 94847-treated group,this effect is significant over 180 min. SNAP 94847 hydrochloride (oral administration; 10 mg/kg), has a good bioavailability (59%), low plasma and blood clearances of 4.2 L/hr/kg and 3.3 L/hr/kg, respectively, and the half-life was shown to be 5.2 h in rats in a PK study. |
| 参考文献: |
1. David DJ, et al. Efficacy of the MCHR1 antagonist N-[3-(1-{[4-(3,4-difluorophenoxy)phenyl]methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847) in mouse models of anxiety and depression following acute and chronic administration is independent of hippocampal neurogenesis. J Pharmacol Exp Ther. 2007 Apr;321(1):237-48. Epub 2007 Jan 19. 2. Nair SG, et al. Effects of the MCH1 receptor antagonist SNAP 94847 on high-fat food-reinforced operant responding and reinstatement of food seeking in rats.Psychopharmacology (Berl). 2009 Jul;205(1):129-40. 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. |
| 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 |
1.942 ml |
9.708 ml |
19.416 ml |
| 5 mM |
0.388 ml |
1.942 ml |
3.883 ml |
| 10 mM |
0.194 ml |
0.971 ml |
1.942 ml |
| 50 mM |
0.039 ml |
0.194 ml |
0.388 ml |
|
| 注意: |
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