Design, synthesis and binding affinities of novel non-peptide mimics of somatostatin/sandostatin(R)

被引:33
|
作者
Damour, D
Barreau, M
Blanchard, JC
Burgevin, MC
Doble, A
Herman, F
Pantel, G
JamesSurcouf, E
Vuilhorgne, M
Mignani, S
Poitout, L
LeMerrer, Y
Depezay, JC
机构
[1] RHONE POULENC RORER SA,CTR RECH VITRY ALFORTVILLE,F-94403 VITRY SUR SEINE,FRANCE
[2] UNIV PARIS 05,CHIM & BIOCHIM PHARMACOL & TOXICOL LAB,CNRS,F-75270 PARIS 06,FRANCE
关键词
D O I
10.1016/0960-894X(96)00289-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Based on molecular modelling studies of Sandostatin(R), sugar-based derivatives I-VI were prepared as potential non-peptide mimics of somatostatin/Sandostatin(R). These compounds displaced 3-[I-125]-Tyr(11)-SRIF-14 from the somatostatin receptor on membranes of rat cerebral cortex with IC50 values between 10 and 15 mu M. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:1667 / 1672
页数:6
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