Heterotropic activation of the midazolam hydroxylase activity of CYP3A by a positive allosteric modulator of mGlu5: In vitro to in vivo translation and potential impact on clinically relevant drug-drug interactions

Drug Metabolism and Disposition

Volumn 41, Issue 12, 2013, Pages 2066-2075

  Blobaum, Anna L ^a   Bridges, Thomas M ^a   Byers, Frank W ^a   Turlington, Mark L ^a   Mattmann, Margrith E ^a   Morrison, Ryan D ^a   Mackie, Claire ^b   Lavreysen, Hilde ^b   Bartolomé, José M ^c   MacDonald, Gregor J ^b   Steckler, Thomas ^b   Jones, Carrie K ^a   Niswender, Colleen M ^a   Conn, P Jeffrey ^a   Lindsley, Craig W ^a   Stauffer, Shaun R ^a   Daniels, J Scott ^a  

^a VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^c NONE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

2 (PHENOXYMETHYL) N (PYRIDIN 3 YLMETHYL 4,5,6,7 TETRAHYDROPYRAZOLO [1,5A]PYRIDIN 4 AMINE); 5 (4 FLUOROBENZYL) 2 (3 FLUOROPHENOXY METHYL) 4,5,6,7 TETRAHYDROPYRAZOLO [1,5A]PYRAZINE; CYTOCHROME P450 3A; CYTOCHROME P450 3A4; G PROTEIN COUPLED RECEPTOR; KETOCONAZOLE; METABOTROPIC RECEPTOR 5; MIDAZOLAM; OXYGENASE; UNCLASSIFIED DRUG; VU 0448187; VU 0464797;

ALLOSTERISM; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONCENTRATION (PARAMETERS); DRUG METABOLISM; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME KINETICS; ENZYME SPECIFICITY; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LIVER CELL; LIVER MICROSOME; MALE; NONHUMAN; POSITIVE ALLOSTERIC MODULATOR; PRIORITY JOURNAL; RAT; SCHIZOPHRENIA;

RATTUS; RODENTIA;

ALLOSTERIC REGULATION; ANIMALS; CYTOCHROME P-450 CYP3A; DRUG INTERACTIONS; HEPATOCYTES; HUMANS; INTESTINES; KETOCONAZOLE; KINETICS; LIVER; MALE; MICE; MICROSOMES; MICROSOMES, LIVER; MIDAZOLAM; MIXED FUNCTION OXYGENASES; RATS; RATS, SPRAGUE-DAWLEY;

EID: 84888591764     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.113.052662     Document Type: Article

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