title: N-pyridin-3-yl- and N-quinolin-3-yl-benzamides: modulators of human vanilloid receptor 1 (TRPV1).
abstract: High throughput screening of our compound library revealed a series of N-pyridyl-3-benzamides as low micromolar agonists of the human TRPV1 receptor. Synthesis of analogs in this series led to the discovery of a series of N-quinolin-3-yl-benzamides as low nanomolar antagonists of human TRPV1.
authors: Johnson & Johnson Pharmaceutical Research and Development, Research and Early Development, Welsh and McKean Roads, Spring House, PA 19477, USA. michele137@comcast.net
authors: Michele C
authors: MC
authors: Jetter
authors: James J
authors: JJ
authors: McNally
authors: Mark A
authors: MA
authors: Youngman
authors: Mark E
authors: ME
authors: McDonnell
authors: Adrienne E
authors: AE
authors: Dubin
authors: Nadia
authors: N
authors: Nasser
authors: Sui-Po
authors: SP
authors: Zhang
authors: Ellen E
authors: EE
authors: Codd
authors: Ray W
authors: RW
authors: Colburn
authors: Dennis R
authors: DR
authors: Stone
authors: Michael R
authors: MR
authors: Brandt
authors: Christopher M
authors: CM
authors: Flores
authors: Scott L
authors: SL
authors: Dax
mesh_terms: D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D003432:Cross-Linking Reagents / Q000737:chemistry; D006801:Humans; D006930:Hyperalgesia / Q000188:drug therapy; D007546:Isoquinolines / Q000737:chemistry*; D015394:Molecular Structure; D011725:Pyridines / Q000737:chemistry*; D051381:Rats; D013329:Structure-Activity Relationship; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: D001549:Benzamides; D003432:Cross-Linking Reagents; D007546:Isoquinolines; D011725:Pyridines; D050916:TRPV Cation Channels; C494484:TRPV1 receptor; C023666:pyridine