ML-154

ML-154 is an antagonist of the neuropeptide S receptor (NPSR; IC₅₀ = 3.5 nM).¹ It is selective for NPSR over arginine vasopressin (AVP) receptor V_1B, as well as a panel of 55 receptors, channels, and transporters at 10 µM.^2,1 ML-154 reduces NPS-induced calcium mobilization, cAMP formation, and ERK activation with IC₅₀ values of 0.96, 45, and 1.3 nM, respectively, in CHO cells expressing NPSR.¹ It reduces alcohol self-administration and the progressive ratio breakpoint, but not cue- or stress-induced reinstatement of alcohol-seeking behavior, in rats when administered intraperitoneally at a dose of 1 mg/kg.² ML-154 (10 µg, i.c.v.) inhibits decreases in food intake induced by intracerebroventricular administration of NPS in rats.¹

WARNING This product is not for human or veterinary use.

1. Patnaik, S., Marugan, J.J., Liu, K., et al. Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide S receptor. J. Med. Chem. 56(22), 9045-9056 (2013).

2. Thorsell, A., Tapocik, J.D., Liu, K., et al. 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. J. Neurosci. 33(24), 10132-10142 (2013).