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Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Di Fabio R, Pellacani A, Faedo S, Roth A, Piccoli L, Gerrard P, Porter RA, Johnson CN, Thewlis K, Donati D, Stasi L, Spada S, Stemp G, Nash D, Branch C, Kindon L, Massagrande M, Poffe A, Braggio S, Chiarparin E, Marchioro C, Ratti E, Corsi M. Di Fabio R, et al. Among authors: johnson cn. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. doi: 10.1016/j.bmcl.2011.06.086. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21831639
Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat.
Stemp G, Ashmeade T, Branch CL, Hadley MS, Hunter AJ, Johnson CN, Nash DJ, Thewlis KM, Vong AK, Austin NE, Jeffrey P, Avenell KY, Boyfield I, Hagan JJ, Middlemiss DN, Reavill C, Riley GJ, Routledge C, Wood M. Stemp G, et al. Among authors: johnson cn. J Med Chem. 2000 May 4;43(9):1878-85. doi: 10.1021/jm000090i. J Med Chem. 2000. PMID: 10794704
Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.
Reavill C, Taylor SG, Wood MD, Ashmeade T, Austin NE, Avenell KY, Boyfield I, Branch CL, Cilia J, Coldwell MC, Hadley MS, Hunter AJ, Jeffrey P, Jewitt F, Johnson CN, Jones DN, Medhurst AD, Middlemiss DN, Nash DJ, Riley GJ, Routledge C, Stemp G, Thewlis KM, Trail B, Vong AK, Hagan JJ. Reavill C, et al. Among authors: johnson cn. J Pharmacol Exp Ther. 2000 Sep;294(3):1154-65. J Pharmacol Exp Ther. 2000. PMID: 10945872
Design and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist.
Macdonald GJ, Branch CL, Hadley MS, Johnson CN, Nash DJ, Smith AB, Stemp G, Thewlis KM, Vong AK, Austin NE, Jeffrey P, Winborn KY, Boyfield I, Hagan JJ, Middlemiss DN, Reavill C, Riley GJ, Watson JM, Wood M, Parker SG, Ashby CR Jr. Macdonald GJ, et al. Among authors: johnson cn. J Med Chem. 2003 Nov 6;46(23):4952-64. doi: 10.1021/jm030817d. J Med Chem. 2003. PMID: 14584946
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
Atkinson PJ, Bromidge SM, Duxon MS, Gaster LM, Hadley MS, Hammond B, Johnson CN, Middlemiss DN, North SE, Price GW, Rami HK, Riley GJ, Scott CM, Shaw TE, Starr KR, Stemp G, Thewlis KM, Thomas DR, Thompson M, Vong AK, Watson JM. Atkinson PJ, et al. Among authors: johnson cn. Bioorg Med Chem Lett. 2005 Feb 1;15(3):737-41. doi: 10.1016/j.bmcl.2004.11.030. Bioorg Med Chem Lett. 2005. PMID: 15664848
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