IDENTIFICATION AND CHARACTERIZATION OF THE ISOMERS OF CYCLOTHIAZIDE RESPONSIBLE FOR POTENTIATING AMPA CURRENT

被引：13

作者：

CORDI, AA

SERKIZ, B

HENNIG, P

MAHIEU, JP

BOBICHON, C

DENANTEUIL, G

LEPAGNOL, JM

机构：

[1] Institut de Recherches Servier, 92150 Suresnes, 11, rue des Moulineaux

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(01)80542-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The four diastereoisomers of cyclothiazide have been separated by chromatography. The most potent fraction was split further into two enantiomers by chiral HPLC. The most active isomer is five times more potent than cyclothiazide in potentiating AMPA transmission in rat cortex mRNA injected Xenopus oocytes.

引用

收藏

页码：1957 / 1960

页数：4

相关论文

共 8 条

[1] NOOTROPIC DRUGS POSITIVELY MODULATE ALPHA-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID-SENSITIVE GLUTAMATE RECEPTORS IN NEURONAL CULTURES [J].

COPANI, A ;

GENAZZANI, AA ;

ALEPPO, G ;

CASABONA, G ;

CANONICO, PL ;

SCAPAGNINI, U ;

NICOLETTI, F .

JOURNAL OF NEUROCHEMISTRY, 1992, 58 (04) :1199-1204

[2] GYKI 52466, A 2,3-BENZODIAZEPINE, IS A HIGHLY SELECTIVE, NONCOMPETITIVE ANTAGONIST OF AMPA/KAINATE RECEPTOR RESPONSES [J].

DONEVAN, SD ;

ROGAWSKI, MA .

NEURON, 1993, 10 (01) :51-59

[3] ANIRACETAM REDUCES GLUTAMATE RECEPTOR DESENSITIZATION AND SLOWS THE DECAY OF FAST EXCITATORY SYNAPTIC CURRENTS IN THE HIPPOCAMPUS [J].

ISAACSON, JS ;

NICOLL, RA .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1991, 88 (23) :10936-10940

[4] CYCLOTHIAZIDE REVERSES AMPA RECEPTOR ANTAGONISM OF THE 2,3-BENZODIAZEPINE, GYKI-53655 [J].

PALMER, AJ ;

LODGE, D .

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1993, 244 (02) :193-194

[5] ALLOSTERIC POTENTIATION BY DIAZOXIDE OF AMPA RECEPTOR CURRENTS AND SYNAPTIC POTENTIALS [J].

RANDLE, JCR ;

BITON, C ;

LEPAGNOL, JM .

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1993, 247 (03) :257-265

[6] STRUCTURE-ACTIVITY-RELATIONSHIPS OF 2,3-BENZODIAZEPINE COMPOUNDS WITH GLUTAMATE ANTAGONISTIC ACTION [J].

TARNAWA, I ;

BERZSENYI, P ;

ANDRASI, F ;

BOTKA, P ;

HAMORI, T ;

LING, I ;

KOROSI, J .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (01) :99-104

[7]

WEINER IM, 1985, PHARMACOL BASIS THER, P892

[8] DIAZOXIDE BLOCKS GLUTAMATE DESENSITIZATION AND PROLONGS EXCITATORY POSTSYNAPTIC CURRENTS IN RAT HIPPOCAMPAL-NEURONS [J].

YAMADA, KA ;

ROTHMAN, SM .

JOURNAL OF PHYSIOLOGY-LONDON, 1992, 458 :409-423