SNAP 94847

SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (K_i= 2.2 nM, K_d=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]. IC50 & Target: Ki: 2.2 nM (MCHR1); Kd: 530 pM (MCHR1)^[1] In Vivo: 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].