Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.
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Culshaw, Andrew, Bevan, Stuart, Christiansen, Martin, Copp, Prafula, Davis, Andrew, Davis, Clare, Dyson, Alex, Dziadulewicz, Ed, Edwards, Lee, Eggelte, Hendrikus, Fox, Alyson, Gentry, Clive, Groarke, Alex, Hallett, Allan, Hart, Terry, Hughes, Glyn, Knights, Sally, Kotsonis, Peter, Lee, Wai, Lyothier, Isabelle, Mcbryde, Andrew, Mcintyre, Peter, Paloumbis, George, Panesar, Moh, Patel, Sadhana, Seiler, Max Peter, Yaqoob, Mo and Zimmermann, Kaspar (2006) Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain. Journal of Medicinal Chemistry, 49 (2). pp. 471-474. ISSN 0022-2623
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.
| Item Type: | Article |
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| Date Deposited: | 14 Dec 2009 13:59 |
| Last Modified: | 31 Jan 2013 01:17 |
| URI: | https://oak.novartis.com/id/eprint/443 |