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Page 1
Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
Jaeschke G, Kolczewski S, Spooren W, Vieira E, Bitter-Stoll N, Boissin P, Borroni E, Büttelmann B, Ceccarelli S, Clemann N, David B, Funk C, Guba W, Harrison A, Hartung T, Honer M, Huwyler J, Kuratli M, Niederhauser U, Pähler A, Peters JU, Petersen A, Prinssen E, Ricci A, Rueher D, Rueher M, Schneider M, Spurr P, Stoll T, Tännler D, Wichmann J, Porter RH, Wettstein JG, Lindemann L. Jaeschke G, et al. Among authors: harrison a. J Med Chem. 2015 Feb 12;58(3):1358-71. doi: 10.1021/jm501642c. Epub 2015 Feb 2. J Med Chem. 2015. PMID: 25565255
Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression.
Lindemann L, Porter RH, Scharf SH, Kuennecke B, Bruns A, von Kienlin M, Harrison AC, Paehler A, Funk C, Gloge A, Schneider M, Parrott NJ, Polonchuk L, Niederhauser U, Morairty SR, Kilduff TS, Vieira E, Kolczewski S, Wichmann J, Hartung T, Honer M, Borroni E, Moreau JL, Prinssen E, Spooren W, Wettstein JG, Jaeschke G. Lindemann L, et al. Among authors: harrison ac. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33. doi: 10.1124/jpet.114.222463. Epub 2015 Feb 9. J Pharmacol Exp Ther. 2015. PMID: 25665805
Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.
Glossop PA, Watson CA, Price DA, Bunnage ME, Middleton DS, Wood A, James K, Roberts D, Strang RS, Yeadon M, Perros-Huguet C, Clarke NP, Trevethick MA, Machin I, Stuart EF, Evans SM, Harrison AC, Fairman DA, Agoram B, Burrows JL, Feeder N, Fulton CK, Dillon BR, Entwistle DA, Spence FJ. Glossop PA, et al. Among authors: harrison ac. J Med Chem. 2011 Oct 13;54(19):6888-904. doi: 10.1021/jm200884j. Epub 2011 Sep 20. J Med Chem. 2011. PMID: 21870878 Clinical Trial.
Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
Fray MJ, Fish PV, Allan GA, Bish G, Clarke N, Eccles R, Harrison AC, Le Net JL, Phillips SC, Regan N, Sobry C, Stobie A, Wakenhut F, Westbrook D, Westbrook SL, Whitlock GA. Fray MJ, et al. Among authors: harrison ac. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92. doi: 10.1016/j.bmcl.2010.04.052. Epub 2010 Apr 18. Bioorg Med Chem Lett. 2010. PMID: 20471260
Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability.
Johnson PS, Ryckmans T, Bryans J, Beal DM, Dack KN, Feeder N, Harrison A, Lewis M, Mason HJ, Mills J, Newman J, Pasquinet C, Rawson DJ, Roberts LR, Russell R, Spark D, Stobie A, Underwood TJ, Ward R, Wheeler S. Johnson PS, et al. Among authors: harrison a. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5684-7. doi: 10.1016/j.bmcl.2011.08.038. Epub 2011 Aug 12. Bioorg Med Chem Lett. 2011. PMID: 21885275
Part 3: Design and synthesis of proline-derived α2δ ligands.
Rawson DJ, Brugier D, Harrison A, Hough J, Newman J, Otterburn J, Maw GN, Price J, Thompson LR, Turnpenny P, Warren AN. Rawson DJ, et al. Among authors: harrison a. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3771-3. doi: 10.1016/j.bmcl.2011.04.058. Epub 2011 Apr 20. Bioorg Med Chem Lett. 2011. PMID: 21550802
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.
Wakenhut F, Allan GA, Fish PV, Fray MJ, Harrison AC, McCoy R, Phillips SC, Ryckmans T, Stobie A, Westbrook D, Westbrook SL, Whitlock GA. Wakenhut F, et al. Among authors: harrison ac. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5078-81. doi: 10.1016/j.bmcl.2009.07.049. Epub 2009 Jul 31. Bioorg Med Chem Lett. 2009. PMID: 19647430
Part 2: Design, synthesis and evaluation of hydroxyproline-derived α2δ ligands.
Rawson DJ, Brugier D, Harrison A, Hough J, Newman J, Otterburn J, Maw GN, Price J, Thompson LR, Turnpenny P, Warren AN. Rawson DJ, et al. Among authors: harrison a. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3767-70. doi: 10.1016/j.bmcl.2011.04.056. Epub 2011 Apr 20. Bioorg Med Chem Lett. 2011. PMID: 21550803
Case studies addressing human pharmacokinetic uncertainty using a combination of pharmacokinetic simulation and alternative first in human paradigms.
Harrison A, Gardner I, Hay T, Dickins M, Beaumont K, Phipps A, Purkins L, Allan G, Christian R, Duckworth J, Gurrell I, Kempshall S, Savage M, Seymour M, Simpson M, Taylor L, Turnpenny P. Harrison A, et al. Xenobiotica. 2012 Jan;42(1):57-74. doi: 10.3109/00498254.2011.622418. Epub 2011 Oct 12. Xenobiotica. 2012. PMID: 21992032 Clinical Trial.
Atypical Presentation of Cutaneous Malignancies in Darker Skin.
Mathis A, Harrison A, Harmon C. Mathis A, et al. Among authors: harrison a. Dermatol Surg. 2024 Dec 1;50(12S):S214-S215. doi: 10.1097/DSS.0000000000004478. Epub 2024 Oct 28. Dermatol Surg. 2024. PMID: 39589849 No abstract available.
2,346 results