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Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans.
Winchester WJ, Gore K, Glatt S, Petit W, Gardiner JC, Conlon K, Postlethwaite M, Saintot PP, Roberts S, Gosset JR, Matsuura T, Andrews MD, Glossop PA, Palmer MJ, Clear N, Collins S, Beaumont K, Reynolds DS. Winchester WJ, et al. J Pharmacol Exp Ther. 2014 Nov;351(2):259-69. doi: 10.1124/jpet.114.216010. Epub 2014 Aug 14. J Pharmacol Exp Ther. 2014. PMID: 25125580 Clinical Trial.
Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.
Andrews MD, Fish PV, Blagg J, Brabham TK, Brennan PE, Bridgeland A, Brown AD, Bungay PJ, Conlon KM, Edmunds NJ, af Forselles K, Gibbons CP, Green MP, Hanton G, Holbrook M, Jessiman AS, McIntosh K, McMurray G, Nichols CL, Root JA, Storer RI, Sutton MR, Ward RV, Westbrook D, Whitlock GA. Andrews MD, et al. Among authors: conlon km. Bioorg Med Chem Lett. 2011 May 1;21(9):2715-20. doi: 10.1016/j.bmcl.2010.11.120. Epub 2010 Dec 4. Bioorg Med Chem Lett. 2011. PMID: 21195614
Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors.
Storer RI, Brennan PE, Brown AD, Bungay PJ, Conlon KM, Corbett MS, DePianta RP, Fish PV, Heifetz A, Ho DK, Jessiman AS, McMurray G, de Oliveira CA, Roberts LR, Root JA, Shanmugasundaram V, Shapiro MJ, Skerten M, Westbrook D, Wheeler S, Whitlock GA, Wright J. Storer RI, et al. Among authors: conlon km. J Med Chem. 2014 Jun 26;57(12):5258-69. doi: 10.1021/jm5003292. Epub 2014 Jun 17. J Med Chem. 2014. PMID: 24878222
38 results