In vivo modulation of benzodiazepine receptor function after inhibition of endogenous gamma-aminobutyric acid synthesis

被引：6

作者：

Bottlaender, M ^{[1
]}

Schmid, L ^{[1
]}

Fuseau, C ^{[1
]}

Fournier, D ^{[1
]}

Brouillet, E ^{[1
]}

Maziere, M ^{[1
]}

机构：

[1] SERV HOSP FREDERIC JOLIOT,DSV,DRM,CEA,F-91400 ORSAY,FRANCE

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1997年 / 321卷 / 01期

关键词：

GABA (gamma-aminobutyric acid); benzodiazepine receptor; in vivo; efficacy; intrinsic; (non-human primate); DL-allylglycine; brain;

D O I：

10.1016/S0014-2999(97)00004-6

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The influence of decreased endogenous gamma-aminobutyric acid (GABA) concentration on benzodiazepine receptor function was studied in the brain of living baboons. Positron emission tomography and the radiotracer [C-11]flumazenil combined with electroencephalography were used to determine the pharmacological properties of two benzodiazepine receptors agonists, diazepam and bretazenil, in baboons pre-treated or not with DL-allylglycine (an inhibitor of GABA synthesis). Our results show that, in vivo, DL-allylglycine reduces the affinity of benzodiazepine receptors for their agonists without altering the intrinsic capability of agonists to allosterically modulate GABAergic transmission. (C) 1997 Elsevier Science B.V.

引用

页码：13 / 17

页数：5

共 18 条

[1] BOTTLAENDER M, 1994, J NEUROCHEM, V62, P1102
[2] INVIVO BIDIRECTIONAL MODULATORY EFFECT OF BENZODIAZEPINE RECEPTOR LIGANDS ON GABAERGIC TRANSMISSION EVALUATED BY POSITRON EMISSION TOMOGRAPHY IN NONHUMAN-PRIMATES
BROUILLET, E
CHAVOIX, C
BOTTLAENDER, M
KHALILIVARASTEH, M
HANTRAYE, P
FOURNIER, D
DODD, RH
MAZIERE, M
[J]. BRAIN RESEARCH, 1991, 557 (1-2) : 167 - 176
[3] RELATIONSHIPS BETWEEN BENZODIAZEPINE RECEPTORS, IMPAIRMENT OF GABAERGIC TRANSMISSION AND CONVULSANT ACTIVITY OF BETA-CCM - A PET STUDY IN THE BABOON PAPIO-PAPIO
CHAVOIX, C
BROUILLET, E
KUNIMOTO, M
DELASAYETTE, V
KHALILIVARASTEH, M
HANTRAYE, P
DODD, RH
GUIBERT, B
PRENANT, C
NAQUET, R
MAZIERE, M
[J]. EPILEPSY RESEARCH, 1991, 8 (01) : 1 - 10
[4] MODELING ANALYSIS OF [C-11] FLUMAZENIL KINETICS STUDIED BY PET - APPLICATION TO A CRITICAL-STUDY OF THE EQUILIBRIUM APPROACHES
DELFORGE, J
SYROTA, A
BOTTLAENDER, M
VARASTET, M
LOCH, C
BENDRIEM, B
CROUZEL, C
BROUILLET, E
MAZIERE, M
[J]. JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM, 1993, 13 (03) : 454 - 468
[5] Haefely W., 1986, Benzodiazepine/GABA receptors and chloride channels: structural and functional properties, P97
[6] Haefely W., 1985, ADV DRUG RES, V14, P165
[7] PENTYLENETETRAZOL-INDUCED SEIZURE IS NOT MEDIATED BY BENZODIAZEPINE RECEPTORS INVIVO
HANTRAYE, P
BROUILLET, E
GUIBERT, B
CHAVOIX, C
FUKUDA, H
PRENANT, C
CROUZEL, M
NAQUET, R
MAZIERE, M
[J]. NEUROPHARMACOLOGY, 1987, 26 (10) : 1509 - 1512
[8] REGIONAL CHANGES IN CEREBRAL GABA CONCENTRATION AND CONVULSIONS PRODUCED BY D-ALLYLGLYCINE AND BY L-ALLYLGLYCINE
HORTON, RW
CHAPMAN, AG
MELDRUM, BS
[J]. JOURNAL OF NEUROCHEMISTRY, 1978, 30 (06) : 1501 - 1504
[9] SYNTHESIS OF ETHYL 8-FLUORO-5,6-DIHYDRO-5-[C-11]METHYL-6-OXO-4H-IMIDAZO[1,5-A][1,4]BENZODIAZEPINE-3-CARBOXYLATE (RO 15.1788-11C) - A SPECIFIC RADIOLIGAND FOR THE INVIVO STUDY OF CENTRAL BENZODIAZEPINE RECEPTORS BY POSITRON EMISSION TOMOGRAPHY
MAZIERE, M
HANTRAYE, P
PRENANT, C
SASTRE, J
COMAR, D
[J]. INTERNATIONAL JOURNAL OF APPLIED RADIATION AND ISOTOPES, 1984, 35 (10): : 973 - 976
[10] GABA SHIFT INVIVO - ENHANCEMENT OF BENZODIAZEPINE BINDING INVIVO BY MODULATION OF ENDOGENOUS GABA
MILLER, LG
GREENBLATT, DJ
BARNHILL, JG
SUMMER, WR
SHADER, RI
[J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1988, 148 (01) : 123 - 130

← 1 2 →