A New Pyridazine Series of GABAA α5 Ligands

M.B. Van Niel, K. Wilson, C.H. Adkins, J.R. Atack, J.L. Castro, D.E. Clarke, S. Fletcher, U. Gerhard, M.M. Mackey, S. Malpas, K. Maubach, R. Newman, D. O'Connor, G.V. Pillai, P.B. Simpson, S.R. Thomas, A.M. MacLeod

    Research output: Contribution to journalArticlepeer-review

    16 Citations (Scopus)


    Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABAA receptors. The structural novelty of 6, compared to our advanced series of GABAA α5 inverse agonists, made it an attractive molecule for further exploration. This paper will describe the evolution of 6 into a new series of ligands with nanomolar affinity and functional selectivity for GABAA α5 receptor subtypes.

    Original languageEnglish
    Pages (from-to)6004-6011
    Number of pages8
    JournalJournal of Medicinal Chemistry
    Issue number19
    Publication statusPublished - 22 Sept 2005


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