Discovery of SB-705498: A potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 12, 2006, Pages 3287-3291

  Rami, Harshad K ^a   Thompson, Mervyn ^a   Stemp, Geoffrey ^a   Fell, Steve ^a   Jerman, Jeffrey C ^a   Stevens, Alexander J ^a   Smart, Darren ^a   Sargent, Becky ^a   Sanderson, Dominic ^a   Randall, Andrew D ^a   Gunthorpe, Martin J ^a   Davis, John B ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Capsaicin; Electrophysiology; FCA; Noxious heat; Pain; SB 366791; SB 452533; SB 705498; TRPV1; TRPV1 antagonist; VR1

Indexed keywords

1 (2 BROMOPHENYL) 3 [1 (5 TRIFLUOROMETHYL 2 PYRIDINYL) 3 PYRROLIDINYL]UREA; ACID; CALCIUM ION; CAPSAICIN; RECEPTOR BLOCKING AGENT; SB 452533; UNCLASSIFIED DRUG; UREA DERIVATIVE; VANILLOID RECEPTOR 1;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; ASSAY; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG SELECTIVITY; ELECTROPHYSIOLOGY; FLUORESCENT IMAGING PLATE READER ASSAY; HEAT; HUMAN; HUMAN CELL; HUMAN TISSUE; NONHUMAN; RAT;

ADMINISTRATION, ORAL; ANIMALS; CAPSAICIN; CELL LINE; DRUG DESIGN; GUINEA PIGS; HUMANS; MOLECULAR STRUCTURE; PYRROLIDINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TRPV CATION CHANNELS; UREA;

ANIMALIA;

EID: 33646677987     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.03.030     Document Type: Article

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15. + = 429, 431.