NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo. IC50 value: 2.6 nM Target: NK-1 receptor In vitro, the binding of NKP608 to bovine retina was characterized by an IC50 of 2.6+/-0.4 nM, whereas the compounds affinity to other receptor binding sites, including NK-2 and NK-3, was much lower. Species differences in IC(50) values with NKP608 were less pronounced than with previously described NK-1 receptor antagonists, being 13+/-2 and 27+/-2 nM in gerbil midbrain and rat striatum, respectively. In vivo, using the hind foot thumping model in gerbils, NKP608 exhibited a potent NK-1 antagonistic activity following oral administration (ID(50)=0.23 mg/kg, 2 h pretreatment), supporting a central activity of NKP608. NKP608 may prove a useful anxiolytic compound.
Molekulargewicht:
619.98
Reinheit:
99.88
CAS Nummer:
[177707-12-9]
Formel:
C31H24ClF6N3O2
Target-Kategorie:
Neurokinin Receptor
Anwendungsbeschreibung:
MCE Product type: Reference compound
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