2. Academic Validation
  3. Discovery of small molecule antagonists of TRPV1

Discovery of small molecule antagonists of TRPV1

  • Bioorg Med Chem Lett. 2004 Jul 16;14(14):3631-4. doi: 10.1016/j.bmcl.2004.05.028.
Harshad K Rami 1,  Mervyn Thompson,  Paul Wyman,  Jeffrey C Jerman,  Julie Egerton,  Stephen Brough,  Alexander J Stevens,  Andrew D Randall,  Darren Smart,  Martin J Gunthorpe,  John B Davis
Affiliations

Affiliation

  • 1 Neurology and GI CEDD, New Frontiers Science Park, GlaxoSmithKline, Third Avenue, Harlow, Essex CM19 5AW, UK. harshad.rami@gsk.com
PMID: 15203132 DOI: 10.1016/j.bmcl.2004.05.028
Abstract

Small molecule antagonists of the vanilloid receptor 1 (TRPV1, also known as VR1) are disclosed. Ureas such as 5 (SB-452533) were used to explore the structure activity relationship with several potent analogues identified. Pharmacological studies using electrophysiological and FLIPR Ca(2+) based assays showed compound 5 was an antagonist versus capsaicin, noxious heat and acid mediated activation of TRPV1. Study of a quaternary salt of 5 supports a mode of action in which compounds from this series cause inhibition via an extracellularly accessible binding site on the TRPV1 receptor.

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