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Page 1
Improving the in vitro prediction of in vivo central nervous system penetration: integrating permeability, P-glycoprotein efflux, and free fractions in blood and brain.
Summerfield SG, Stevens AJ, Cutler L, del Carmen Osuna M, Hammond B, Tang SP, Hersey A, Spalding DJ, Jeffrey P. Summerfield SG, et al. Among authors: stevens aj. J Pharmacol Exp Ther. 2006 Mar;316(3):1282-90. doi: 10.1124/jpet.105.092916. Epub 2005 Dec 5. J Pharmacol Exp Ther. 2006. PMID: 16330496
Toward an improved prediction of human in vivo brain penetration.
Summerfield SG, Lucas AJ, Porter RA, Jeffrey P, Gunn RN, Read KR, Stevens AJ, Metcalf AC, Osuna MC, Kilford PJ, Passchier J, Ruffo AD. Summerfield SG, et al. Among authors: stevens aj. Xenobiotica. 2008 Dec;38(12):1518-35. doi: 10.1080/00498250802499459. Xenobiotica. 2008. PMID: 18979396
The cyclooxygenase-2 inhibitor GW406381X [2-(4-ethoxyphenyl)-3-[4-(methylsulfonyl)phenyl]-pyrazolo[1,5-b]pyridazine] is effective in animal models of neuropathic pain and central sensitization.
Bingham S, Beswick PJ, Bountra C, Brown T, Campbell IB, Chessell IP, Clayton N, Collins SD, Davey PT, Goodland H, Gray N, Haslam C, Hatcher JP, Hunter AJ, Lucas F, Murkitt G, Naylor A, Pickup E, Sargent B, Summerfield SG, Stevens A, Stratton SC, Wiseman J. Bingham S, et al. Among authors: stevens a. J Pharmacol Exp Ther. 2005 Mar;312(3):1161-9. doi: 10.1124/jpet.104.075267. Epub 2004 Nov 30. J Pharmacol Exp Ther. 2005. PMID: 15572651
SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats.
Thomas DR, Melotto S, Massagrande M, Gribble AD, Jeffrey P, Stevens AJ, Deeks NJ, Eddershaw PJ, Fenwick SH, Riley G, Stean T, Scott CM, Hill MJ, Middlemiss DN, Hagan JJ, Price GW, Forbes IT. Thomas DR, et al. Among authors: stevens aj. Br J Pharmacol. 2003 Jun;139(4):705-14. doi: 10.1038/sj.bjp.0705290. Br J Pharmacol. 2003. PMID: 12812993 Free PMC article.
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.
Forbes IT, Douglas S, Gribble AD, Ife RJ, Lightfoot AP, Garner AE, Riley GJ, Jeffrey P, Stevens AJ, Stean TO, Thomas DR. Forbes IT, et al. Among authors: stevens aj. Bioorg Med Chem Lett. 2002 Nov 18;12(22):3341-4. doi: 10.1016/s0960-894x(02)00690-x. Bioorg Med Chem Lett. 2002. PMID: 12392747
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.
Beswick P, Bingham S, Bountra C, Brown T, Browning K, Campbell I, Chessell I, Clayton N, Collins S, Corfield J, Guntrip S, Haslam C, Lambeth P, Lucas F, Mathews N, Murkit G, Naylor A, Pegg N, Pickup E, Player H, Price H, Stevens A, Stratton S, Wiseman J. Beswick P, et al. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5445-8. doi: 10.1016/j.bmcl.2004.07.089. Bioorg Med Chem Lett. 2004. PMID: 15454242
Discovery of small molecule antagonists of TRPV1.
Rami HK, Thompson M, Wyman P, Jerman JC, Egerton J, Brough S, Stevens AJ, Randall AD, Smart D, Gunthorpe MJ, Davis JB. Rami HK, et al. Among authors: stevens aj. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3631-4. doi: 10.1016/j.bmcl.2004.05.028. Bioorg Med Chem Lett. 2004. PMID: 15203132
Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.
Beswick PJ, Billinton A, Chambers LJ, Dean DK, Fonfria E, Gleave RJ, Medhurst SJ, Michel AD, Moses AP, Patel S, Roman SA, Roomans S, Senger S, Stevens AJ, Walter DS. Beswick PJ, et al. Among authors: stevens aj. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4653-6. doi: 10.1016/j.bmcl.2010.05.107. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20579878
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
Swarbrick ME, Beswick PJ, Gleave RJ, Green RH, Bingham S, Bountra C, Carter MC, Chambers LJ, Chessell IP, Clayton NM, Collins SD, Corfield JA, Hartley CD, Kleanthous S, Lambeth PF, Lucas FS, Mathews N, Naylor A, Page LW, Payne JJ, Pegg NA, Price HS, Skidmore J, Stevens AJ, Stocker R, Stratton SC, Stuart AJ, Wiseman JO. Swarbrick ME, et al. Among authors: stevens aj. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4504-8. doi: 10.1016/j.bmcl.2009.02.085. Epub 2009 Feb 26. Bioorg Med Chem Lett. 2009. PMID: 19520573
132 results