title: Heteroaryl beta-tetralin ureas as novel antagonists of human TRPV1.
abstract: We report on a series of alpha-substituted-beta-tetralin-derived and related phenethyl-based isoquinolinyl and hydroxynaphthyl ureas as potent antagonists of the human TRPV1 receptor. The synthesis and Structure-activity relationships (SAR) of the series are described.
authors: Johnson & Johnson Pharmaceutical Research and Development, Welsh and McKean Roads, Spring House, PA 19477, USA. mjetter@prdus.jnj.com
authors: Michele C
authors: MC
authors: Jetter
authors: Mark A
authors: MA
authors: Youngman
authors: James J
authors: JJ
authors: McNally
authors: Mark E
authors: ME
authors: McDonnell
authors: Sui-Po
authors: SP
authors: Zhang
authors: Adrienne E
authors: AE
authors: Dubin
authors: Nadia
authors: N
authors: Nasser
authors: Ellen E
authors: EE
authors: Codd
authors: Christopher M
authors: CM
authors: Flores
authors: Scott L
authors: SL
authors: Dax
mesh_terms: D001667:Binding, Competitive / Q000187:drug effects; D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*; D013764:Tetrahydronaphthalenes / Q000737:chemistry / Q000494:pharmacology*; D014508:Urea / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D050916:TRPV Cation Channels; C494482:TRPV1 protein, human; D013764:Tetrahydronaphthalenes; D014508:Urea