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

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

  • J Med Chem. 2006 Jan 26;49(2):471-4. doi: 10.1021/jm051058x.
Andrew J Culshaw 1,  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
Affiliations

Affiliation

  • 1 Novartis Institutes for Biomedical Research, London WC1E 6BS, UK. andrew.culshaw@novartis.com
PMID: 16420034 DOI: 10.1021/jm051058x
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.

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