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

被引：9

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

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1995年 / 36卷 / 02期

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

页码：129 / 135

页数：7

共 6 条

[1]

BITTIGER H, 1988, EUROP J NEUROSCI S

[2]

DINGWALL JG, 1987, PHOSPHORUS SULFUR, V30, P571

[3]

DINGWALL JG, 1989, J CHEM SOC P1, P3787

[4] CGP 35348 - A CENTRALLY ACTIVE BLOCKER OF GABA-B RECEPTORS [J].

OLPE, HR ;

KARLSSON, G ;

POZZA, MF ;

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STEINMANN, M ;

VANRIEZEN, H ;

FAGG, G ;

HALL, RG ;

FROESTL, W ;

BITTIGER, H .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1990, 187 (01) :27-38

[5]

PRISHCHENKO AA, 1990, ZH OBSHCH KHIM+, V60, P1420

[6]

WARDLEWORTH PS, Patent No. 307362

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