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Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.
Dziadulewicz EK, Bevan SJ, Brain CT, Coote PR, Culshaw AJ, Davis AJ, Edwards LJ, Fisher AJ, Fox AJ, Gentry C, Groarke A, Hart TW, Huber W, James IF, Kesingland A, La Vecchia L, Loong Y, Lyothier I, McNair K, O'Farrell C, Peacock M, Portmann R, Schopfer U, Yaqoob M, Zadrobilek J. Dziadulewicz EK, et al. Among authors: bevan sj. J Med Chem. 2007 Aug 9;50(16):3851-6. doi: 10.1021/jm070317a. Epub 2007 Jul 14. J Med Chem. 2007. PMID: 17630726
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain.
Irie O, Kosaka T, Ehara T, Yokokawa F, Kanazawa T, Hirao H, Iwasaki A, Sakaki J, Teno N, Hitomi Y, Iwasaki G, Fukaya H, Nonomura K, Tanabe K, Koizumi S, Uchiyama N, Bevan SJ, Malcangio M, Gentry C, Fox AJ, Yaqoob M, Culshaw AJ, Allan Hallett. Irie O, et al. Among authors: bevan sj. J Med Chem. 2008 Sep 25;51(18):5502-5. doi: 10.1021/jm800839j. J Med Chem. 2008. PMID: 18754655
Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.
Culshaw AJ, Bevan S, Christiansen M, Copp P, Davis A, Davis C, Dyson A, Dziadulewicz EK, Edwards L, Eggelte H, Fox A, Gentry C, Groarke A, Hallett A, Hart TW, Hughes GA, Knights S, Kotsonis P, Lee W, Lyothier I, McBryde A, McIntyre P, Paloumbis G, Panesar M, Patel S, Seiler MP, Yaqoob M, Zimmermann K. Culshaw AJ, et al. J Med Chem. 2006 Jan 26;49(2):471-4. doi: 10.1021/jm051058x. J Med Chem. 2006. PMID: 16420034
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.
Irie O, Kosaka T, Kishida M, Sakaki J, Masuya K, Konishi K, Yokokawa F, Ehara T, Iwasaki A, Iwaki Y, Hitomi Y, Toyao A, Gunji H, Teno N, Iwasaki G, Hirao H, Kanazawa T, Tanabe K, Hiestand PC, Malcangio M, Fox AJ, Bevan SJ, Yaqoob M, Culshaw AJ, Hart TW, Hallett A. Irie O, et al. Among authors: bevan sj. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5280-4. doi: 10.1016/j.bmcl.2008.08.067. Epub 2008 Aug 22. Bioorg Med Chem Lett. 2008. PMID: 18783943
7-tert-Butyl-6-(4-chloro-phenyl)-2-thioxo-2,3-dihydro-1H-pyrido[2,3-d]pyrimidin-4-one, a classic polymodal inhibitor of transient receptor potential vanilloid type 1 with a reduced liability for hyperthermia, is analgesic and ameliorates visceral hypersensitivity.
Nash MS, McIntyre P, Groarke A, Lilley E, Culshaw A, Hallett A, Panesar M, Fox A, Bevan S. Nash MS, et al. J Pharmacol Exp Ther. 2012 Aug;342(2):389-98. doi: 10.1124/jpet.112.191932. Epub 2012 May 7. J Pharmacol Exp Ther. 2012. PMID: 22566669 Free article.
145 results