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Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.

Culshaw, Andrew and Bevan, Stuart and Christiansen, Martin and Copp, Prafula and Davis, Andrew and Davis, Clare and Dyson, Alex and Dziadulewicz, Ed and Edwards, Lee and Eggelte, Hendrikus and Fox, Alyson and Gentry, Clive and Groarke, Alex and Hallett, Allan and Hart, Terry and Hughes, Glyn and Knights, Sally and Kotsonis, Peter and Lee, Wai and Lyothier, Isabelle and Mcbryde, Andrew and Mcintyre, Peter and Paloumbis, George and Panesar, Moh and Patel, Sadhana and Seiler, Max Peter and 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

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