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 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.
| Molecular Weight | 619.98 |
| CAS Number | 177707-12-9 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Neurokinin Receptor Products |
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| Spantide II
Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. |
| Substance P (7-11)
Substance P (7-11) is a C-terminal fragment of Substance P which can cause an increase in the intracellular calcium concentration. |
| [Sar9, Met(O2)11]-Substance P TFA
[Sar9,Met(O2)11]-Substance P TFA is a tachykinin NK1 receptor selective agonist. |
| [bAla8]-Neurokinin A(4-10)
[bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor agonist. |
| [Sar9, Met(O2)11]-Substance P
[Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist. |
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