Nipecotic and iso -nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists
作者:Changyou Zhou、Liangqin Guo、Greg Morriello、Alex Pasternak、Yanping Pan、Susan P Rohrer、Elizebeth T Birzin、Su-Er Wu Huskey、Tom Jacks、Klaus D Schleim、Kang Cheng、James M Schaeffer、Arthur A Patchett、Lihu Yang
DOI:10.1016/s0960-894x(00)00687-9
日期:2001.2
N-Substituted nipecotic and iso-nipecotic amides of beta -methylTrpLys tert-butyl ester were found to be novel, selective and potent agonists of the somatostatin subtype-2 receptor in vitro. For example iso-nipecotic amide 8a showed high hsst2 binding affinity (K-i = 0.5 nM) and good selectivity (h(5)/h(2) = 832). (C) 2001 Elsevier Science Ltd. All rights reserved.