Potent neuropeptide S receptor (NPSR) antagonist (pA2
= 9.98). Inhibits neuropeptide S-induced ERK phosphorylation over cAMP responses and calcium responses (IC50
values are 9.3, 22.1 and 36.5 nM, respectively). Appears to modulate addictive behavior in vivo
. Displays no activity against vasopressin V1B
receptors. Brain penetrant.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.
Patnaik et al.
J Med Chem., 2013;56:9045
A novel brain penetrant NPS receptor antagonist, NCGC00185684, blocks alcohol-induced ERK-phosphorylation in the central amygdala and decreases operant alcohol self-administration in rats.
Thorsell et al.