NPY 5RA972 is a potent and selective NPY5-R (neuropeptide Y) antagonist (IC50 values are 3.1, >10000, >10000 and >10000 nM for NPY5-R, NPY1-R, NPY2-R and NPY4-R respectively). This compound does not block NPY-induced feeding in vivo. NPY 5RA972 has also been shown to be a brain penetrant.
Block et al (2002) Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity. J.Med.Chem. 45 3509. Turnbull et al (2002) Selective antagonism of the NPY Y5 receptor does not have a major effect on feeding i