| Literature DB >> 16420034 |
Andrew J Culshaw1, Stuart Bevan, Martin Christiansen, Prafula Copp, Andrew Davis, Clare Davis, Alex Dyson, Edward K Dziadulewicz, Lee Edwards, Hendrikus Eggelte, Alyson Fox, Clive Gentry, Alex Groarke, Allan Hallett, Terance W Hart, Glyn A Hughes, Sally Knights, Peter Kotsonis, Wai Lee, Isabelle Lyothier, Andrew McBryde, Peter McIntyre, George Paloumbis, Moh Panesar, Sadhana Patel, Max-Peter Seiler, Mohammed Yaqoob, Kaspar Zimmermann.
Abstract
Vanilloid receptor 1 (VR1, TRPV1) is a cation-selective ion channel that is expressed on primary afferent neurons and is upregulated following inflammation and nerve damage. Blockers of this channel may have utility in the treatment of chronic nociceptive and neuropathic pain. Here, we describe the optimization from a high throughput screening hit, of a series of 6-aryl-7-isopropylquinazolinones that are TRPV1 antagonists in vitro. We also demonstrate that one compound is active in vivo against capsaicin-induced hyperalgesia and in models of neuropathic and nociceptive pain in the rat.Entities:
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Year: 2006 PMID： 16420034 DOI： 10.1021/jm051058x
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446