MCH1 antagonist
CAS：487051-12-7
分子式：C29H32F2N2O2.HCl
分子量：515.03
纯度：98%
存储：Store at -20°C

Background:

SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over?MCHα1A?and MCHD2?receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters[1][3].

SNAP 94847 (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[2].SNAP 94847 (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[2].SNAP 94847 (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[3].

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.