| Description | NKP608 is a selective 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 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. |
| In vivo | 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. |
| Target activity | NK1 receptor:2.6 nM |
| molecular weight | 619.98 |
| Molecular formula | C31H24ClF6N3O2 |
| CAS | 177707-12-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: Insoluble DMSO: 100 mg/mL (161.30 mM), Sonication is recommended. |
| References | 1. El-Hashim AZ, Wyss D, Lewis C. Effect of a novel NK1 receptor selective antagonist (NKP608) on citric acid induced cough and airway obstruction. Pulm Pharmacol Ther. 2004;17(1):11-8. 2. Vendruscolo LF, Takahashi RN, Brüske GR, Ramos A. Evaluation of the anxiolytic-like effect of NKP608, a NK1-receptor antagonist, in two rat strains that differ in anxiety-related behaviors. Psychopharmacology (Berl). 2003 Nov;170(3):287-93. 3. Rupniak NM, Carlson EJ, Shepheard S, et al. Comparison of the functional blockade of rat substance P (NK1) receptors by GR205171, RP67580, SR140333 and NKP-608. Neuropharmacology. 2003 Aug;45(2):231-41. 4. Gentsch C, Cutler M, Vassout A, et al. Anxiolytic effect of NKP608, a NK1-receptor antagonist, in the social investigation test in gerbils. Behav Brain Res. 2002 Jul 18;133(2):363-8. |