The first selective antagonist for a GABA(C) receptor

被引:68
作者
Murata, Y
Woodward, RM
Miledi, R
Overman, LE
机构
[1] UNIV CALIF IRVINE,DEPT CHEM,IRVINE,CA 92697
[2] UNIV CALIF IRVINE,DEPT PSYCHOBIOL,IRVINE,CA 92697
关键词
D O I
10.1016/0960-894X(96)00364-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
(1,2,5,6-Tetrahydropyridine-4-yl)methylphosphinic acid (TPMPA, 1), which is synthesized in six steps from 3-butyn-1-ol, is the first gamma-aminobutyric acid (GABA) receptor antagonist that shows strong selectivity for mammalian GABA(C) receptors. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:2073 / 2076
页数:4
相关论文
共 27 条
[1]  
ARNOLD H, 1991, ORG SYNTH, V70, P111
[2]   GABA(B) RECEPTOR ANTAGONISTS - FROM SYNTHESIS TO THERAPEUTIC APPLICATIONS [J].
BITTIGER, H ;
FROESTL, W ;
MICKEL, SJ ;
OLPE, HR .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1993, 14 (11) :391-394
[3]   GABA(C) RECEPTORS [J].
BORMANN, J ;
FEIGENSPAN, A .
TRENDS IN NEUROSCIENCES, 1995, 18 (12) :515-519
[4]   CATIONIC MODULATION OF RHO(1)-TYPE GAMMA-AMINOBUTYRATE RECEPTORS EXPRESSED IN XENOPUS OOCYTES [J].
CALVO, DJ ;
VAZQUEZ, AE ;
MILEDI, R .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1994, 91 (26) :12725-12729
[5]   THE MILD AND SELECTIVE N-DEBENZYLATION OF TERTIARY ALKYLAMINES USING BETA-TRIMETHYLSILYLETHYL CHLOROFORMATE [J].
CAMPBELL, AL ;
PILIPAUSKAS, DR ;
KHANNA, IK ;
RHODES, RA .
TETRAHEDRON LETTERS, 1987, 28 (21) :2331-2334
[6]   CLONING OF THE GAMMA-AMINOBUTYRIC-ACID (GABA) RHO-1 CDNA - A GABA RECEPTOR SUBUNIT HIGHLY EXPRESSED IN THE RETINA [J].
CUTTING, GR ;
LU, L ;
OHARA, BF ;
KASCH, LM ;
MONTROSERAFIZADEH, C ;
DONOVAN, DM ;
SHIMADA, S ;
ANTONARAKIS, SE ;
GUGGINO, WB ;
UHL, GR ;
KAZAZIAN, HH .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1991, 88 (07) :2673-2677
[7]   A THIN SLICE PREPARATION FOR PATCH CLAMP RECORDINGS FROM NEURONS OF THE MAMMALIAN CENTRAL NERVOUS-SYSTEM [J].
EDWARDS, FA ;
KONNERTH, A ;
SAKMANN, B ;
TAKAHASHI, T .
PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY, 1989, 414 (05) :600-612
[8]  
GAMMILL RB, 1993, ANNU REP MED CHEM, V28, P19
[9]   BACLOFEN-H-3 AND H-3-GABA BIND TO BICUCULLINE-INSENSITIVE GABA-B SITES IN RAT-BRAIN [J].
HILL, DR ;
BOWERY, NG .
NATURE, 1981, 290 (5802) :149-152
[10]   STEREOSELECTIVE SYNTHESIS OF VINYLPHOSPHONATE [J].
HIRAO, T ;
MASUNAGA, T ;
OHSHIRO, Y ;
AGAWA, T .
TETRAHEDRON LETTERS, 1980, 21 (37) :3595-3598