| Literature DB >> 15203132 |
Harshad K Rami1, 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.
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.Entities:
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Year: 2004 PMID： 15203132 DOI： 10.1016/j.bmcl.2004.05.028
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823