Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N′-[3-(tetrazol-5-ylamino)phenyl]ureas

Journal of Medicinal Chemistry

Volumn 39, Issue 4, 1996, Pages 842-849

  Castro, José L ^a   Ball, Richard G ^b   Broughton, Howard B ^a   Russell, Michael G N ^a   Rathbone, Denise ^a   Watt, Alan P ^a   Baker, Raymond ^a   Chapman, Kerry L ^a   Fletcher, Alan E ^a   Patel, Smita ^a   Smith, Alison J ^a   Marshall, George R ^a   Ryecroft, Wayne ^a   Matassa, Victor G ^a  

^a NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 (2,3 DIHYDRO 1 METHYL 2 OXO 5 PHENYL 1H 1,4 BENZODIAZEPIN 3 YL) 3 (3 METHYLPHENYL)UREA; 1 (5 CYCLOHEXYL 2,3 DIHYDRO 1 METHYL 2 OXO 1H 1,4 BENZODIAZEPIN 3 YL) 3 [3 [N METHYL N (5 TETRAZOLYL)AMINO]PHENYL]UREA; BENZODIAZEPINE DERIVATIVE; CHOLECYSTOKININ B RECEPTOR ANTAGONIST; CHOLECYSTOKININ OCTAPEPTIDE; DEVAZEPIDE; L 736380; L 738425; PENTAGASTRIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ANXIETY; ARTICLE; DEPRESSION; DRUG CONFORMATION; DRUG DESIGN; DRUG SYNTHESIS; INTRAPERITONEAL DRUG ADMINISTRATION; NOCICEPTION; NONHUMAN; PANIC; PKA; RAT; RECEPTOR AFFINITY; SATIETY;

ANIMALS; BENZODIAZEPINONES; BRAIN; CELL MEMBRANE; CRYSTALLOGRAPHY, X-RAY; INDICATORS AND REAGENTS; IODINE RADIOISOTOPES; KINETICS; MICE; MICE, INBRED STRAINS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PHENYLUREA COMPOUNDS; RADIOLIGAND ASSAY; RECEPTOR, CHOLECYSTOKININ B; RECEPTORS, CHOLECYSTOKININ; SINCALIDE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0030043963     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm9506736     Document Type: Article

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59. 38
60. Comparisons of the above brain penetration data have to be taking cautiously, however, because in this model the extent of binding to central CCK-B receptors is measured after 30 min of dosing, and different pharmacokinetic behavior of the compounds might influence the end result.