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A new pyridazine series of GABAA alpha5 ligands.
van Niel MB, Wilson K, Adkins CH, Atack JR, Castro JL, Clarke DE, Fletcher S, Gerhard U, Mackey MM, Malpas S, Maubach K, Newman R, O'Connor D, Pillai GV, Simpson PB, Thomas SR, MacLeod AM. van Niel MB, et al. J Med Chem. 2005 Sep 22;48(19):6004-11. doi: 10.1021/jm050249x. J Med Chem. 2005. PMID: 16162003
Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.
Ladduwahetty T, Gilligan M, Humphries A, Merchant KJ, Fish R, McAlister G, Ivarsson M, Dominguez M, O'Connor D, MacLeod AM. Ladduwahetty T, et al. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12. doi: 10.1016/j.bmcl.2010.04.090. Epub 2010 Apr 24. Bioorg Med Chem Lett. 2010. PMID: 20493697
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
van Niel MB, Collins I, Beer MS, Broughton HB, Cheng SK, Goodacre SC, Heald A, Locker KL, MacLeod AM, Morrison D, Moyes CR, O'Connor D, Pike A, Rowley M, Russell MG, Sohal B, Stanton JA, Thomas S, Verrier H, Watt AP, Castro JL. van Niel MB, et al. J Med Chem. 1999 Jun 17;42(12):2087-104. doi: 10.1021/jm981133m. J Med Chem. 1999. PMID: 10377215
Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction.
Jones P, Atack JR, Braun MP, Cato BP, Chambers MS, O'Connor D, Cook SM, Hobbs SC, Maxey R, Szekeres HJ, Szeto N, Wafford KA, MacLeod AM. Jones P, et al. Bioorg Med Chem Lett. 2006 Feb 15;16(4):872-5. doi: 10.1016/j.bmcl.2005.11.012. Epub 2005 Nov 21. Bioorg Med Chem Lett. 2006. PMID: 16303300
2,713 results