Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5- methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABAA α5 inverse agonist for cognitive dysfunction

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 4, 2006, Pages 872-875

  Jones, Philip ^a   Atack, John R ^a   Braun, Matthew P ^b   Cato, Brian P ^b   Chambers, Mark S ^a   O'Connor, Desmond ^a   Cook, Susan M ^a   Hobbs, Sarah C ^a   Maxey, Robert ^a   Szekeres, Helen J ^a   Szeto, Nicola ^a   Wafford, Keith A ^a   MacLeod, Angus M ^a  

^a NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Aldehyde oxidase; Cognition; GABA; GABAA 5; Inverse agonist; Metabolism; Radiolabel

Indexed keywords

(3 TERT BUTYL 7 (5 METHYLISOXAZOL 3 YL) 3 (1 METHYL 1H 1,2,4 TRIAZOL 5 YLMETHOXY)PYRAZOLO[1,5 D][1,2,4]TRIAZINE; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; ALDEHYDE OXIDASE; DRUG METABOLITE; TRIAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; COGNITION; COGNITIVE DEFECT; CONTROLLED STUDY; DOG; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG SYNTHESIS; NONHUMAN; RAT; RHESUS MONKEY;

ANIMALS; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; GABA AGONISTS; HYDROLYSIS; ISOXAZOLES; MACACA MULATTA; MICE; MOLECULAR CONFORMATION; PROTEIN SUBUNITS; RATS; RECEPTORS, GABA-A; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TISSUE DISTRIBUTION; TRIAZINES;

ANIMALIA; CANIS FAMILIARIS; MACACA MULATTA;

EID: 30344453647     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.11.012     Document Type: Article

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