Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for κ-opioid receptors

Journal of Medicinal Chemistry

Volumn 39, Issue 4, 1996, Pages 860-872

  Cappelli, Andrea ^b   Anzini, Maurizio ^b   Vomero, Salvatore ^b   Menziani, M Cristina ^a   De Benedetti, Pier G ^a   Sbacchi, Massimo ^c   Clarke, Geoffrey D ^c   Mennuni, Laura ^d  

^a UNIVERSITY OF MODENA AND REGGIO EMILIA   (Italy)

^b UNIVERSITY OF SIENA   (Italy)

^c SmithKline Beecham SpA   (Italy)

^d Rotta Research Laboratorium   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2,3 DIHYDRO 1 METHYL 5 PHENYL 2 [2 [(2 THIENYLCARBONYL)AMINO]ETHYL] 1H 1,4 BENZODIAZEPINE; 3,4 DICHLORO N METHYL N [2 (1 PYRROLIDINYL)CYCLOHEXYL]BENZENEACETAMIDE; 4 [(3,4 DICHLOROPHENYL)ACETYL] 3 (1 PYRROLIDINYLMETHYL) 1 PIPERAZINECARBOXYLIC ACID METHYL ESTER; BENZODIAZEPINE DERIVATIVE; CHOLECYSTOKININ A RECEPTOR; CHOLECYSTOKININ B RECEPTOR; CHOLECYSTOKININ DERIVATIVE; CHOLECYSTOKININ OCTAPEPTIDE; DEVAZEPIDE; ENADOLINE; ENKEPHALIN[2 DEXTRO ALANINE 4 METHYLPHENYLALANINE 5 GLYCINE]; ENKEPHALIN[2 DEXTRO ALANINE 5 DEXTRO LEUCINE]; KAPPA OPIATE RECEPTOR; LORGLUMIDE; N METHYL N [7 (1 PYRROLIDINYL) 1 OXASPIRO[4.5]DEC 8 YL]BENZENEACETAMIDE; NALOXONE; OPIATE AGONIST; SPIRADOLINE; TIFLUADOM; UNCLASSIFIED DRUG;

ANALGESIA; ANIMAL TISSUE; ANTINOCICEPTION; ARTICLE; DIURESIS; DRUG SCREENING; DRUG SYNTHESIS; GUINEA PIG; NONHUMAN; QUANTITATIVE STRUCTURE ACTIVITY RELATION; RAT; RECEPTOR AFFINITY;

AMINO ACID SEQUENCE; ANALGESICS; ANIMALS; BENZODIAZEPINES; BINDING, COMPETITIVE; BRAIN; CEREBRAL CORTEX; COMPUTER GRAPHICS; CONSERVED SEQUENCE; ENKEPHALIN, ALA(2)-MEPHE(4)-GLY(5)-; ENKEPHALIN, LEUCINE-2-ALANINE; ENKEPHALINS; GUINEA PIGS; HUMANS; LIGANDS; MICE; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MOLECULAR STRUCTURE; PANCREAS; PROTEIN CONFORMATION; RADIOLIGAND ASSAY; RATS; RECEPTORS, CHOLECYSTOKININ; RECEPTORS, OPIOID, KAPPA; SEQUENCE HOMOLOGY, AMINO ACID; SINCALIDE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0030028469     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm950423p     Document Type: Review

References (89)

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