Biological Activity |
SNAP 94847 hydrochloride 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 MCHalpha1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride 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)[3] In Vivo: 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 x 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 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 x 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 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[3]. |