PHOSPHINIC ACID ANALOGS OF GAMMA-AMINOBUTYRIC-ACID (GABA) - SYNTHESIS OF A NEW RADIOLIGAND

被引:8
|
作者
HALL, RG
KANE, PD
BITTIGER, H
FROESTL, W
机构
[1] CIBA GEIGY PLC,CENT RES LABS,MACCLESFIELD SK10 2NX,CHESHIRE,ENGLAND
[2] CIBA GEIGY PHARMACEUT CORP,HORSHAM RH12 4AB,W SUSSEX,ENGLAND
[3] CIBA GEIGY AG,DIV PHARMACEUT,CH-4002 BASEL,SWITZERLAND
关键词
TRITIUM; GAMMA-AMINOPHOSPHINIC ACIDS; GABA-B; SYNTHESIS;
D O I
10.1002/jlcr.2580360205
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The synthesis of a new radioligand, which binds with high selectivity and affinity (K-D=7.4 nM) to the GABA-B receptor, is described. A Wittig-Horner approach was employed to prepare an unsaturated protected intermediate (($) under bar 6), suitable for tritiation and deprotection.
引用
收藏
页码:129 / 135
页数:7
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