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Identification of potent, soluble, and orally active TRPV1 antagonists |
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| Authors: | Ratcliffe Paul Maclean John Abernethy Lynn Clarkson Tom Dempster Maureen Easson Anna-Marie Edwards Darren Everett Katy Feilden Helen Littlewood Peter McArthur Duncan McGregor Deborah McLuskey Hazel Nimz Olaf Nisbet Lesley-Anne Palin Ronnie Tracey Heather Walker Glenn |
| Affiliation: | a Department of Chemistry, MSD, Newhouse, Lanarkshire ML1 5SH, UK b Department of Pharmacology, MSD, Newhouse, Lanarkshire ML1 5SH, UK c Department of Molecular Pharmacology, MSD, Newhouse, Lanarkshire ML1 5SH, UK |
| 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. |
| Keywords: | TRPV1 antagonist Antihyperalgesia Isoxazoles |
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