Utility of the carboxylesterase inhibitor bis-para-nitrophenylphosphate (BNPP) in the plasma unbound fraction determination for a hydrolytically unstable amide derivative and agonist of the TGR5 receptor

Xenobiotica

Volumn 40, Issue 6, 2010, Pages 369-380

  Eng, H ^a   Niosi, M ^a   McDonald, T S ^a   Wolford, A ^a   Chen, Y ^a   Simila, S T M ^b   Bauman, J N ^a   Warmus, J ^b   Kalgutkar, A S ^a  

^a Dynamics and Metabolism   (United States)

^b PFIZER INC   (United States)

Author keywords

Amide; Carboxylesterase; Cytochrome P450; Inhibition; Metabolite; Plasma; Takeda G protein coupled receptor 5 (TGR5) agonist; Unbound fraction

Indexed keywords

1 (6 FLUORO 2 METHYL 3,4 DIHYDROQUINOLIN 1(2H) YL) 2 (ISOQUINOLIN 5 YLOXY)ETHANONE; ADENOSINE DERIVATIVE; AMIDE; BETA NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE; BIS(4 NITROPHENYL) PHOSPHATE; CARBOXYLESTERASE; G PROTEIN COUPLED RECEPTOR; NICOTINAMIDE; REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE; TAKEDA G PROTEIN COUPLED RECEPTOR 5; UNCLASSIFIED DRUG;

AEROBIC METABOLISM; ARTICLE; BINDING SITE; CHEMICAL BOND; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG HALF LIFE; DRUG PROTEIN BINDING; DRUG RESEARCH; DRUG STABILITY; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HYDROLYSIS; IN VIVO STUDY; LIVER MICROSOME; MOLECULAR PROBE; MOUSE; NONHUMAN; PHARMACODYNAMICS; PROTEIN DEGRADATION; RAT;

ANIMALS; CARBOXYLESTERASE; DOGS; DRUG STABILITY; FEMALE; HUMANS; HYDROLYSIS; ISOQUINOLINES; MALE; MICE; MICROSOMES, LIVER; NADP; NITROPHENOLS; ORGANOPHOSPHORUS COMPOUNDS; OXIDATION-REDUCTION; QUINOLINES; RATS; RATS, WISTAR; RECEPTORS, G-PROTEIN-COUPLED; TRIAZOLES;

CANIS FAMILIARIS; RATTUS; RODENTIA;

EID: 77952258130     PISSN: 00498254     EISSN: 13665928     Source Type: Journal    
DOI: 10.3109/00498251003706598     Document Type: Article

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