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GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization.
Tralau-Stewart CJ, Williamson RA, Nials AT, Gascoigne M, Dawson J, Hart GJ, Angell AD, Solanke YE, Lucas FS, Wiseman J, Ward P, Ranshaw LE, Knowles RG. Tralau-Stewart CJ, et al. Among authors: nials at. J Pharmacol Exp Ther. 2011 Apr;337(1):145-54. doi: 10.1124/jpet.110.173690. Epub 2011 Jan 4. J Pharmacol Exp Ther. 2011. PMID: 21205923
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: nials at. 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
At last, a truly selective EP₂ receptor antagonist.
Birrell MA, Nials AT. Birrell MA, et al. Among authors: nials at. Br J Pharmacol. 2011 Dec;164(7):1845-6. doi: 10.1111/j.1476-5381.2011.01494.x. Br J Pharmacol. 2011. PMID: 21595650 Free PMC article.
29 results