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

…, EK Dziadulewicz, L Edwards, H Eggelte…

文献索引：Culshaw, Andrew J.; Bevan, Stuart; Christiansen, Martin; Copp, Prafula; Davis, Andrew; Davis, Clare; Dyson, Alex; Dziadulewicz, Edward K.; Edwards, Lee; Eggelte, Hendrikus; Fox, Alyson; Gentry, Clive; Groarke, Alex; Hallett, Allan; Hart, Terance W.; Hughes, Glyn A.; Knights, Sally; Kotsonis, Peter; Lee, Wai; Lyothier, Isabelle; McBryde, Andrew; McIntyre, Peter; Paloumbis, George; Panesar, Moh; Patel, Sadhana; Seiler, Max-Peter; Yaqoob, Mohammed; Zimmermann, Kaspar Journal of Medicinal Chemistry, 2006 , vol. 49, # 2 p. 471 - 474

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被引用次数: 62

摘要

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 ...