1358772-20-9Relevant academic research and scientific papers
Discovery of a novel class of bicyclo[3.1.0]hexanylpiperazines as noncompetitive neuropeptide y Y1 antagonists
Hu, Shuanghua,Huang, Yazhong,Deshpande, Milind,Luo, Guanglin,Bruce, Marc A.,Chen, Ling,Mattson, Gail,Iben, Lawrence G.,Zhang, Jie,Russell, John W.,Clarke, Wendy J.,Hogan, John B.,Ortiz, Astrid,Flint, Oliver,Henwood, Andrew,Gao, Qi,Antal-Zimanyi, Ildiko,Poindexter, Graham S.
scheme or table, p. 222 - 226 (2012/05/04)
A novel class of bicyclo[3.1.0]hexanylpiperazine neuropeptide Y (NPY) Y1 antagonists has been designed and synthesized. Scatchard binding analysis showed these compounds to be noncompetitive with [125I]PYY binding to the Y1 receptor. The most potent member, 1-((1α,3α,5α,6β)-6- (3-ethoxyphenyl)-3-methylbicyclo[3.1.0]hexan-6-yl)-4-phenylpiperazine (2) had an IC50 = 62 nM and displayed excellent oral bioavailability in rat (% F po = 80), as well as good brain penetration (B/P ratio = 0.61). In a spontaneous nocturnal feeding study with male Sprague-Dawley rats, 2 significantly reduced food intake during a 12 h period.
