Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: Identification of potent, soluble, and orally active TRPV1 antagonists.

Authors: Paul Ratcliffe, John Maclean, Lynn Abernethy, Tom Clarkson, Maureen Dempster, Anna-Marie Easson, Darren Edwards, Katy Everett, Helen Feilden, Peter Littlewood, Duncan McArthur, Deborah McGregor, Hazel McLuskey, Olaf Nimz, Lesley-Anne Nisbet, Ronnie Palin, Heather Tracey, Glenn Walker

Journal, date & volume: Bioorg. Med. Chem. Lett., 2011 Apr 15 , 21, 2559-63

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/21435873

Abstract
Optimization of a water soluble, moderately potent lead series of isoxazole-3-carboxamides was conducted, affording a compound with the requisite balance of potency, solubility and physicochemical properties for in vivo use. Compound 8e was demonstrated to be efficacious in a rat model of inflammatory pain, following oral administration.