Ester to amide substitution improves selectivity, efficacy and kinetic behavior of a benzodiazepine positive modulator of GABAAreceptors containing the α5 subunit

European Journal of Pharmacology

Volumn 791, Issue , 2016, Pages 433-443

  Stamenić, Tamara Timić ^a   Poe, Michael M ^b   Rehman, Sabah ^c   Santrač, Anja ^a   Divović, Branka ^a   Scholze, Petra ^c   Ernst, Margot ^c   Cook, James M ^b   Savić, Miroslav M ^a  

^a UNIVERSITY OF BELGRADE   (Serbia)

^b UNIVERSITY OF WISCONSIN MILWAUKEE   (United States)

^c Medical University of Vienna   (Austria)

Author keywords

Amide compound; Basic behavior; Binding assay; Free brain concentration; Rat kinetics; Receptor efficacy

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR ALPHA5; 8 ETHYNYL 6 (2 FLUOROPHENYL) N,4 DIMETHYL 4H BENZO[F]IMIDAZO[1,5 A][1,4]DIAZEPINE 3 CARBOXAMIDE; AMIDE; AMPHETAMINE; BENZODIAZEPINE DERIVATIVE; ESTER; PENTETRAZOLE; UNCLASSIFIED DRUG; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; DIAZEPAM; IMIDAZOLE DERIVATIVE; SH-053-2'F-R-CH3;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG SELECTIVITY; DRUG STABILITY; DRUG SYNTHESIS; ELEVATED PLUS MAZE TEST; ELIMINATION HALF-LIFE; FEMALE; GRIP STRENGTH; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LOCOMOTION; MALE; MAXIMUM PLASMA CONCENTRATION; MUSCLE RELAXATION; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; ROTAROD TEST; TIME TO MAXIMUM PLASMA CONCENTRATION; ANALOGS AND DERIVATIVES; ANIMAL; DRUG EFFECTS; ELECTROPHYSIOLOGY; HAND STRENGTH; HEK293 CELL LINE; KINETICS; MAZE TEST; METABOLISM; WISTAR RAT; XENOPUS LAEVIS;

AMPHETAMINE; ANIMALS; DIAZEPAM; DRUG STABILITY; ELECTROPHYSIOLOGICAL PHENOMENA; GABA-A RECEPTOR AGONISTS; HAND STRENGTH; HEK293 CELLS; HUMANS; IMIDAZOLES; KINETICS; LOCOMOTION; MALE; MAZE LEARNING; RATS; RATS, WISTAR; RECEPTORS, GABA-A; XENOPUS LAEVIS;

EID: 84988476311     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2016.09.016     Document Type: Article

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