Pyrido[2,3-b]pyrazines, discovery of TRPV1 antagonists with reduced potential for the formation of reactive metabolites

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 15, 2010, Pages 4359-4363

  Hodgetts, Kevin J ^a   Blum, Charles A ^a   Caldwell, Timothy ^a   Bakthavatchalam, Rajagopal ^a   Zheng, Xiaozhang ^a   Capitosti, Scott ^a   Krause, James E ^a   Cortright, Daniel ^a   Crandall, Marci ^a   Murphy, Beth Ann ^b   Boyce, Susan ^b   Brian Jones, A ^b   Chenard, Bertrand L ^a  

^a NEUROGEN CORPORATION   (United States)

^b Merck Sharp & Dohme Limited   (United Kingdom)

Author keywords

1,8 Naphthyridine; Analgesia; Pyrido 2,3 b pyrazine; TRPV1 antagonist

Indexed keywords

1,8 NAPHTHYRIDINE DERIVATIVE; CAPSAICIN; CARRAGEENAN; FREUND ADJUVANT; NAPROXEN; PYRAZINE DERIVATIVE; PYRIMIDINE; PYRIMIDINE DERIVATIVE; VANILLOID RECEPTOR 1 ANTAGONIST;

ANALGESIA; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BLOOD BRAIN BARRIER; BRAIN; CHRONIC PAIN; CONTROLLED STUDY; COVALENT BOND; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG MEGADOSE; DRUG PENETRATION; HUMAN; HUMAN CELL; HYPERALGESIA; IN VITRO STUDY; IN VIVO STUDY; METABOLITE; NONHUMAN; RAT; REACTIVE INHIBITION; THERMAL HYPERALGESIA;

ADMINISTRATION, ORAL; ANIMALS; DOGS; DRUG EVALUATION, PRECLINICAL; HUMANS; HYPERALGESIA; MACACA MULATTA; MICROSOMES, LIVER; NAPHTHYRIDINES; PAIN; PYRAZINES; RATS; TRPV CATION CHANNELS;

EID: 77955426977     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.06.069     Document Type: Article

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