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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: avenell ky. 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: avenell ky. J Pharmacol Exp Ther. 2000 Sep;294(3):1154-65. J Pharmacol Exp Ther. 2000. PMID: 10945872
SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.
Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, Avenell KY, Stean T, Upton N, Bromidge S, Forbes IT, Brown AM, Middlemiss DN, Blackburn TP. Kennett GA, et al. Among authors: avenell ky. Neuropharmacology. 1997 Apr-May;36(4-5):609-20. doi: 10.1016/s0028-3908(97)00038-5. Neuropharmacology. 1997. PMID: 9225286