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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: whitlock ga. J Med Chem. 2014 Jun 26;57(12):5258-69. doi: 10.1021/jm5003292. Epub 2014 Jun 17. J Med Chem. 2014. PMID: 24878222
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.
Wakenhut F, Allan GA, Fish PV, Fray MJ, Harrison AC, McCoy R, Phillips SC, Ryckmans T, Stobie A, Westbrook D, Westbrook SL, Whitlock GA. Wakenhut F, et al. Among authors: whitlock ga. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5078-81. doi: 10.1016/j.bmcl.2009.07.049. Epub 2009 Jul 31. Bioorg Med Chem Lett. 2009. PMID: 19647430
Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
Fray MJ, Fish PV, Allan GA, Bish G, Clarke N, Eccles R, Harrison AC, Le Net JL, Phillips SC, Regan N, Sobry C, Stobie A, Wakenhut F, Westbrook D, Westbrook SL, Whitlock GA. Fray MJ, et al. Among authors: whitlock ga. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92. doi: 10.1016/j.bmcl.2010.04.052. Epub 2010 Apr 18. Bioorg Med Chem Lett. 2010. PMID: 20471260
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: whitlock ga. 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
34 results