NKP608
Cat. No. :YN321172
CAS No. :177707-12-9
86-020-82000279
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order@ubiochem.com| Product Name: | NKP608 |
| CAS NO.: | 177707-12-9 |
| Chemical Name: | |
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| Molecular Weight: | 619.98 |
| Molecular Formula: | C₃₁H₂₄ClF₆N₃O₂ |
| SMILES: | O=C(C1=CC=NC2=CC=CC=C12)N[C@@H]3C[C@@H](CC4=CC=C(Cl)C=C4)N(C(C5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)=O)CC3 |
| Storage: | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Transportation: | Room temperature in continental US; may vary elsewhere. |
| 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=2.6nM) and in vivo. In vitro, the binding of NKP608 to bovine retina was characterized by an IC50 of 2.6+/-0.4nM, 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+/-2nM 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. |
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