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NKP608

CAS No. : 177707-12-9

Biological Activity：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.

Research Area：Neurological Disease|Endocrinology

Targets：Neurokinin Receptor

Related Screening Libraries:Bioactive Compound Library Plus;GPCR/G Protein Compound Library;Neuronal Signaling Compound Library;Endocrinology Compound Library;Neurotransmitter Receptor Compound Library;

Related Small Molecules:(β-Ala8)-Neurokinin A (4-10);Talnetant hydrochloride;Pavinetant;MEN11467;(D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P;Vapreotide acetate;Rolapitant;Eprazinone dihydrochloride;Orvepitant maleate;Netupitant metabolite Monohydroxy Netupitant;SB-222200;Senktide;GR 87389;Hemokinin 1, human;Neurokinin A TFA;Imnopitant dihydrochloride;[Glp6] Substance P (6-11);[Lys5,MeLeu9,Nle10]-NKA(4-10) TFA;[Pro9]-Substance P;Befetupitant;Hemokinin 1 (mouse);Substance P Receptor Antagonist 1;(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B;Substance P (1-9);(D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P;Substance P-Gly-Lys-Arg

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