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| Cas No.: | 177707-12-9 |
| Synonyms: | NK 608;NK-608 |
| SMILES: | O=C(C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)N(CC2)[C@H](CC3=CC=C(Cl)C=C3)C[C@H]2NC(C4=C(C=CC=C5)C5=NC=C4)=O |
| Formula: | C31H24ClF6N3O2 |
| M.Wt: | 619.9846 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | 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. In vitro, the binding of NKP608 to bovine retina was characterized by an IC50 of 2.6+/-0.4 nM, whereas the compound's 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. |