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The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.
Knust H, Achermann G, Ballard T, Buettelmann B, Gasser R, Fischer H, Hernandez MC, Knoflach F, Koblet A, Stadler H, Thomas AW, Trube G, Waldmeier P. Knust H, et al. Among authors: achermann g. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4. doi: 10.1016/j.bmcl.2009.08.053. Epub 2009 Aug 15. Bioorg Med Chem Lett. 2009. PMID: 19762240
Discovery of the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine scaffold as a novel, potent and selective GABA(A) alpha5 inverse agonist series.
Achermann G, Ballard TM, Blasco F, Broutin PE, Büttelmann B, Fischer H, Graf M, Hernandez MC, Hilty P, Knoflach F, Koblet A, Knust H, Kurt A, Martin JR, Masciadri R, Porter RH, Stadler H, Thomas AW, Trube G, Wichmann J. Achermann G, et al. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5746-52. doi: 10.1016/j.bmcl.2009.07.153. Epub 2009 Aug 4. Bioorg Med Chem Lett. 2009. PMID: 19726184