THE GLYCINE-SITE NMDA RECEPTOR ANTAGONIST, R-(+)-CIS-BETA-METHYL-3-AMINO-1-HYDROXYPYRROLID-2-ONE, L-687,414 IS ANTICONVULSANT IN BABOONS

被引：37

作者：

SMITH, SE ^{[1
]}

MELDRUM, BS ^{[1
]}

机构：

[1] INST PSYCHIAT,DEPT NEUROL,DE CRESPIGNY PK,DENMARK HILL,LONDON SE5 8AF,ENGLAND

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1992年 / 211卷 / 01期

关键词：

GLYCINE; L-687,414; NMDA (N-METHYL-D-ASPARTATE); BEHAVIOR; EXCITATORY AMINO ACIDS; EPILEPSY;

D O I：

10.1016/0014-2999(92)90270-E

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The glycine-site NMDA receptor antagonist, R-(+)cis-beta-methyl-3-amino-1-hydroxypyrrolid-2-one (L-687,414) administered i.t. to photosensitive baboons. The anticonvulsant action of L-687,414 (5-45 mg kg-1) was dose-dependent and peaked between 15 min and 2 h after administration. Gross behavioural effects were not observed at the doses tested. L-687,414 is a potent systemically acting anticonvulsant apparently devoid of serious side effects.

引用

页码：109 / 111

页数：3

共 9 条

[1] FOSTER AC, 1991, BR J PHARM S, V102, pP64
[2] KEMP JA, 1991, BR J PHARM S, V102, pP65
[3] NONCOMPETITIVE EXCITATORY AMINO-ACID RECEPTOR ANTAGONISTS
LODGE, D
JOHNSON, KM
[J]. TRENDS IN PHARMACOLOGICAL SCIENCES, 1990, 11 (02) : 81 - 86
[4] MELDRUM BS, 1978, EEG S, V34, P317
[5] PALFREYMAN MG, 1991, EXCITATORY AMINO ACI, P101
[6] SAYWELL K, 1990, BRIT J PHARMACOL, V102, pP66
[7] A POTENT ANTAGONIST OF THE STRYCHNINE INSENSITIVE GLYCINE RECEPTOR HAS ANTICONVULSANT PROPERTIES
SHEARDOWN, MJ
DREJER, J
JENSEN, LH
STIDSEN, CE
HONORE, T
[J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1989, 174 (2-3) : 197 - 204
[8] ENANTIOMERS OF HA-966 (3-AMINO-1-HYDROXYPYRROLID-2-ONE) EXHIBIT DISTINCT CENTRAL NERVOUS-SYSTEM EFFECTS - (+)-HA-966 IS A SELECTIVE GLYCINE N-METHYL-D-ASPARTATE RECEPTOR ANTAGONIST, BUT (-)-HA-966 IS A POTENT GAMMA-BUTYROLACTONE-LIKE SEDATIVE
SINGH, L
DONALD, AE
FOSTER, AC
HUTSON, PH
IVERSEN, LL
IVERSEN, SD
KEMP, JA
LEESON, PD
MARSHALL, GR
OLES, RJ
PRIESTLEY, T
THORN, L
TRICKLEBANK, MD
VASS, CA
WILLIAMS, BJ
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1990, 87 (01) : 347 - 351
[9] BLOCKADE OF N-METHYL-D-ASPARTATE INDUCED CONVULSIONS BY 1-AMINOCYCLOPROPANECARBOXYLATES
SKOLNICK, P
MARVIZON, JCG
JACKSON, BW
MONN, JA
RICE, KC
LEWIN, AH
[J]. LIFE SCIENCES, 1989, 45 (18) : 1647 - 1655

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