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The identification of a novel phosphodiesterase 4 inhibitor, 1-ethyl-5-{5-[(4-methyl-1-piperazinyl)methyl]-1,3,4-oxadiazol-2-yl}-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine (EPPA-1), with improved therapeutic index using pica feeding in rats as a measure of emetogenicity.
Davis TG, Peterson JJ, Kou JP, Capper-Spudich EA, Ball D, Nials AT, Wiseman J, Solanke YE, Lucas FS, Williamson RA, Ferrari L, Wren P, Knowles RG, Barnette MS, Podolin PL. Davis TG, et al. Among authors: wren p. J Pharmacol Exp Ther. 2009 Sep;330(3):922-31. doi: 10.1124/jpet.109.152454. Epub 2009 Jun 4. J Pharmacol Exp Ther. 2009. PMID: 19498103
Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.
Palin R, Barn DR, Clark JK, Cottney JE, Cowley PM, Crockatt M, Evans L, Feilden H, Goodwin RR, Griekspoor F, Grove SJ, Houghton AK, Jones PS, Morphy RJ, Smith AR, Sundaram H, Vrolijk D, Weston MA, Wishart G, Wren P. Palin R, et al. Among authors: wren p. Bioorg Med Chem Lett. 2005 Feb 1;15(3):589-93. doi: 10.1016/j.bmcl.2004.11.049. Bioorg Med Chem Lett. 2005. PMID: 15664818
GSK356278, a potent, selective, brain-penetrant phosphodiesterase 4 inhibitor that demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in preclinical species.
Rutter AR, Poffe A, Cavallini P, Davis TG, Schneck J, Negri M, Vicentini E, Montanari D, Arban R, Gray FA, Davies CH, Wren PB. Rutter AR, et al. Among authors: wren pb. J Pharmacol Exp Ther. 2014 Jul;350(1):153-63. doi: 10.1124/jpet.114.214155. Epub 2014 Apr 30. J Pharmacol Exp Ther. 2014. PMID: 24784567
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