NKP608 is a selective and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50: 2.6 nM) and in vivo.

The binding of NKP608 to the bovine retina was characterized by an IC50 of 2.6 nM, whereas the compound's affinity to other receptor binding sites, including NK-2 and NK-3, was much lower. Species differences in IC50 values with NKP608 were less pronounced than with previously described NK-1 receptor antagonists, being 13 and 27 nM in gerbil midbrain and rat striatum, respectively.

Using the hindfoot thumping model in gerbils, NKP608 exhibited a potent NK-1 antagonistic activity following oral administration (ID50: 0.23 mg/kg, 2 h pretreatment), supporting a central activity of NKP608.

177707-12-9

C31H24ClF6N3O2

619.99

H2O:Insoluble
DMSO:100 mg/mL (161.30 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years