Discovery and SAR of Org 24598 - A selective glycine uptake inhibitor

被引：90

作者：

Brown, A

Carlyle, I

Clark, J

Hamilton, W

Gibson, S ^{[1
]}

McGarry, G

McEachen, S

Rae, D

Thorn, S

Walker, G

机构：

[1] Organon Res & Dev Grp, Dept Med Chem, Newhouse ML1 5SH, Lanark, Scotland

[2] Organon Res & Dev Grp, Dept Pharmacol, Newhouse ML1 5SH, Lanark, Scotland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(01)00355-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The discovery of Org 24598, one of the first potent and selective inhibitors of the glycine transporter is discussed. In vitro structure-activity relationships (SARs) data for interaction of a ligand with this system is discussed. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2007 / 2009

页数：3

共 13 条

[1] Aprison M. H., 1990, GLYCINE NEUROTRANSMI, P1
[2] Modulation of N-methyl-D-aspartate receptor function by glycine transport
Bergeron, R
Meyer, TM
Coyle, JT
Greene, RW
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1998, 95 (26) : 15730 - 15734
[3] FRONTAL CORTICAL AND LEFT TEMPORAL GLUTAMATERGIC DYSFUNCTION IN SCHIZOPHRENIA
DEAKIN, JFW
SLATER, P
SIMPSON, MDC
GILCHRIST, AC
SKAN, WJ
ROYSTON, MC
REYNOLDS, GP
CROSS, AJ
[J]. JOURNAL OF NEUROCHEMISTRY, 1989, 52 (06) : 1781 - 1786
[4] JAVITT DC, 1991, AM J PSYCHIAT, V148, P1301
[5] GLYCINE POTENTIATES THE NMDA RESPONSE IN CULTURED MOUSE-BRAIN NEURONS
JOHNSON, JW
ASCHER, P
[J]. NATURE, 1987, 325 (6104) : 529 - 531
[6] JURSKY F, 1995, J NEUROCHEM, V64, P1026
[7] THE INHIBITORY GLYCINE RECEPTOR - A LIGAND-GATED CHLORIDE CHANNEL OF THE CENTRAL-NERVOUS-SYSTEM
LANGOSCH, D
BECKER, CM
BETZ, H
[J]. EUROPEAN JOURNAL OF BIOCHEMISTRY, 1990, 194 (01): : 1 - 8
[8] LUI QR, 1993, J BIOL CHEM, V268, P22802
[9] Molecular cloning and functional expression of the human glycine transporter GlyT2 and chromosomal localisation of the gene in the human genome
Morrow, JA
Collie, IT
Dunbar, DR
Walker, GB
Shahid, M
Hill, DR
[J]. FEBS LETTERS, 1998, 439 (03) : 334 - 340
[10] NMDA ANTAGONISTS AS NEUROTHERAPEUTIC DRUGS, PSYCHOTOGENS, NEUROTOXINS, AND RESEARCH TOOLS FOR STUDYING SCHIZOPHRENIA
OLNEY, JW
FARBER, NB
[J]. NEUROPSYCHOPHARMACOLOGY, 1995, 13 (04) : 335 - 345

← 1 2 →