N-2 METHYLATED QUATERNARY DERIVATIVES OF BETA-CARBOLINE-3-CARBOXYLATES INHIBIT ACETYLCHOLINESTERASE IN-VITRO

被引：2

作者：

DEKHANE, M

DUBOIS, L

BLANCHET, G

GARRIGUE, H

SENTENACROUMANOU, H

POTIER, P

DODD, RH

机构：

[1] CNRS,INST CHIM SUBSTANCES NAT,F-91198 GIF SUR YVETTE,FRANCE

[2] CTR RECH,SERV SANTE ARMEES,F-38702 LA TRONCHE,FRANCE

[3] CTR ETUD BOUCHET,F-91710 VERT LE PETIT,FRANCE

[4] DIRECT RECH ETUD & TECH,F-75996 PARIS,FRANCE

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)80774-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Alkyl beta-carboline-3-carboxylate derivatives (e.g. beta-CCM and beta-CCB), known to interact with the central benzodiazepine receptor, were quaternized at the N-2 position using methyl iodide. The products strongly inhibited acetylcholinesterase in vitro and displayed affinities for muscarinic receptors in the micromolar range.

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页码：2831 / 2836

页数：6

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共 38 条

[1] ROLE OF N-METHYLTRANSFERASES IN THE NEUROTOXICITY ASSOCIATED WITH THE METABOLITES OF 1-METHYL-4-PHENYL-1,2,3,6-TETRAHYDROPYRIDINE (MPTP) AND OTHER 4-SUBSTITUTED PYRIDINES PRESENT IN THE ENVIRONMENT [J].

ANSHER, SS ;

CADET, JL ;

JAKOBY, WB ;

BAKER, JK .

BIOCHEMICAL PHARMACOLOGY, 1986, 35 (19) :3359-3363

[2] USE OF A 96-WELL MICROPLATE READER FOR MEASURING ROUTINE ENZYME-ACTIVITIES [J].

ASHOUR, MBA ;

GEE, SJ ;

HAMMOCK, BD .

ANALYTICAL BIOCHEMISTRY, 1987, 166 (02) :353-360

[3] PHYSOSTIGMINE AND RECENT MEMORY - EFFECTS IN YOUNG AND AGED NONHUMAN-PRIMATES [J].

BARTUS, RT .

SCIENCE, 1979, 206 (4422) :1087-1089

[4] ANXIOGENIC EFFECTS OF METHYL-BETA-CARBOLINE-3-CARBOXYLATE IN A LIGHT DARK CHOICE SITUATION [J].

BELZUNG, C ;

MISSLIN, R ;

VOGEL, E ;

DODD, RH ;

CHAPOUTHIER, G .

PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 1987, 28 (01) :29-33

[5] URINARY AND BRAIN BETA-CARBOLINE-3-CARBOXYLATES AS POTENT INHIBITORS OF BRAIN BENZODIAZEPINE RECEPTORS [J].

BRAESTRUP, C ;

NIELSEN, M ;

OLSEN, CE .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES, 1980, 77 (04) :2288-2292

[6] BETA-CARBOLINES - SYNTHESIS AND NEUROCHEMICAL AND PHARMACOLOGICAL ACTIONS ON BRAIN BENZODIAZEPINE RECEPTORS [J].

CAIN, M ;

WEBER, RW ;

GUZMAN, F ;

COOK, JM ;

BARKER, SA ;

RICE, KC ;

CRAWLEY, JN ;

PAUL, SM ;

SKOLNICK, P .

JOURNAL OF MEDICINAL CHEMISTRY, 1982, 25 (09) :1081-1091

[7] CHANGES IN CORTICAL ACETYLCHOLINE OUTPUT INDUCED BY MODULATION OF THE NUCLEUS BASALIS [J].

CASAMENTI, F ;

DEFFENU, G ;

ABBAMONDI, AL ;

PEPEU, G .

BRAIN RESEARCH BULLETIN, 1986, 16 (05) :689-695

[8] TRANQUILIZING MEMORIES - A REVIEW OF THE EFFECTS OF BENZODIAZEPINES ON HUMAN-MEMORY [J].

CURRAN, HV .

BIOLOGICAL PSYCHOLOGY, 1986, 23 (02) :179-213

[9] ANXIOGENIC AND NON-ANXIOGENIC BENZODIAZEPINE ANTAGONISTS [J].

DECARVALHO, LP ;

GRECKSCH, G ;

CHAPOUTHIER, G ;

ROSSIER, J .

NATURE, 1983, 301 (5895) :64-66

[10] CHARACTERIZATION OF CONVULSIONS INDUCED BY METHYL BETA-CARBOLINE-3-CARBOXYLATE IN MICE [J].

DECARVALHO, LP ;

GRECKSCH, G ;

CAVALHEIRO, EA ;

DODD, RH ;

CHAPOUTHIER, G ;

ROSSIER, J .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1984, 103 (3-4) :287-293

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