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Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor.
Gunthorpe MJ, Hannan SL, Smart D, Jerman JC, Arpino S, Smith GD, Brough S, Wright J, Egerton J, Lappin SC, Holland VA, Winborn K, Thompson M, Rami HK, Randall A, Davis JB. Gunthorpe MJ, et al. J Pharmacol Exp Ther. 2007 Jun;321(3):1183-92. doi: 10.1124/jpet.106.116657. Epub 2007 Mar 28. J Pharmacol Exp Ther. 2007. PMID: 17392405
Cloning and functional expression of a human orthologue of rat vanilloid receptor-1.
Hayes P, Meadows HJ, Gunthorpe MJ, Harries MH, Duckworth MD, Cairns W, Harrison DC, Clarke CE, Ellington K, Prinjha RK, Barton AJL, Medhurst AD, Smith GD, Topp S, Murdock P, Sanger GJ, Terrett J, Jenkins O, Benham CD, Randall AD, Gloger IS, Davis JB. Hayes P, et al. Among authors: randall ad. Pain. 2000 Nov;88(2):205-215. doi: 10.1016/S0304-3959(00)00353-5. Pain. 2000. PMID: 11050376
Discovery of small molecule antagonists of TRPV1.
Rami HK, Thompson M, Wyman P, Jerman JC, Egerton J, Brough S, Stevens AJ, Randall AD, Smart D, Gunthorpe MJ, Davis JB. Rami HK, et al. Among authors: randall ad. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3631-4. doi: 10.1016/j.bmcl.2004.05.028. Bioorg Med Chem Lett. 2004. PMID: 15203132
Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia.
Davis JB, Gray J, Gunthorpe MJ, Hatcher JP, Davey PT, Overend P, Harries MH, Latcham J, Clapham C, Atkinson K, Hughes SA, Rance K, Grau E, Harper AJ, Pugh PL, Rogers DC, Bingham S, Randall A, Sheardown SA. Davis JB, et al. Nature. 2000 May 11;405(6783):183-7. doi: 10.1038/35012076. Nature. 2000. PMID: 10821274
Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist.
Gunthorpe MJ, Rami HK, Jerman JC, Smart D, Gill CH, Soffin EM, Luis Hannan S, Lappin SC, Egerton J, Smith GD, Worby A, Howett L, Owen D, Nasir S, Davies CH, Thompson M, Wyman PA, Randall AD, Davis JB. Gunthorpe MJ, et al. Among authors: randall ad. Neuropharmacology. 2004 Jan;46(1):133-49. doi: 10.1016/s0028-3908(03)00305-8. Neuropharmacology. 2004. PMID: 14654105
157 results