Pharmacological and pharmacokinetic characterization of 2-piperazine-α-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists

Bioorganic and Medicinal Chemistry

Volumn 16, Issue 10, 2008, Pages 5606-5618

  Chen, Chen ^a   Tucci, Fabio C ^a   Jiang, Wanlong ^a   Tran, Joe A ^a   Fleck, Beth A ^a   Hoare, Sam R ^a   Wen, Jenny ^a   Chen, Takung ^a   Johns, Michael ^a   Markison, Stacy ^a   Foster, Alan C ^a   Marinkovic, Dragan ^a   Chen, Caroline W ^a   Arellano, Melissa ^a   Harman, John ^a   Saunders, John ^a   Bozigian, Haig ^b   Marks, Daniel ^b  

^a NEUROCRINE BIOSCIENCES INC   (United States)

^b OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

Antagonist; Cachexia; Melanocortin 4 receptor; Pharmacokinetics; SAR

Indexed keywords

1 [2 [2 [1 (DIMETHYLAMINOPROPIONYL)AMINO] 2 METHYLPROPYL] 6 FLUOROPHENYL] 4 [METHYL 3 (4 CHLOROPHENYL)PROPIONYL]PIPERAZINE; 2 PIPERAZINE ALPHA ISOPROPYLBENZYLAMINE DERIVATIVE; BENZYLAMINE DERIVATIVE; HORMONE RECEPTOR BLOCKING AGENT; MELANOCORTIN 4 RECEPTOR; MELANOCORTIN 4 RECEPTOR ANTAGONIST; N,N DIMETHYLAMINOPROPIONAMIDE; PIPERAZINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; C57BL 6 MOUSE; CACHEXIA; CANCER MODEL; CELL STRAIN CACO 2; CELL STRAIN HEK293; CONTROLLED STUDY; CRYSTAL STRUCTURE; CULTURE MEDIUM; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFECT; DRUG EFFICACY; DRUG HALF LIFE; DRUG PENETRATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; DUAL ENERGY X RAY ABSORPTIOMETRY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN TISSUE; LIPOPHILICITY; LIVER MICROSOME; MALE; MOLECULAR WEIGHT; MONOLAYER CULTURE; MOUSE; NONHUMAN; PROTON NUCLEAR MAGNETIC RESONANCE; REACTION ANALYSIS; RECEPTOR AFFINITY; STRUCTURE ANALYSIS;

ANIMALS; BENZYLAMINES; CACHEXIA; CACO-2 CELLS; CARCINOMA, LEWIS LUNG; CRYSTALLOGRAPHY, X-RAY; DISEASE MODELS, ANIMAL; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; HAPLORHINI; HUMANS; MALE; MICE; MICE, INBRED C57BL; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PIPERAZINES; RATS; RECEPTOR, MELANOCORTIN, TYPE 4; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TIME FACTORS; TISSUE DISTRIBUTION; XENOGRAFT MODEL ANTITUMOR ASSAYS;

ANIMALIA; MURINAE; MUS;

EID: 43749088040     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2008.03.072     Document Type: Article

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