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    Eur J Med Chem. 2009 Oct;44(10):4098-106. Epub 2009 May 13.

    Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.

    Dvorak CA, Apodaca R, Xiao W, Jablonowski JA, Bonaventure P, Dugovic C, Shelton J, Lord B, Miller K, Dvorak LK, Lovenberg TW, Carruthers NI.

    Source

    Johnson & Johnson Pharmaceutical Research & Development, LLC, San Diego, CA 92121, USA. cdvorak@its.jnj.com

    Abstract

    A series of (4-aminobutyn-1-yl)benzylamines were prepared and the SAR around three key areas: (1) the amine attached to the butynyl linker (R(3)R(4)N-); (2) the benzylamine moiety (R(1)R(2)N-); and (3) the point of attachment of the benzylamine group (R(1)R(2)N- in the ortho, meta, or para positions) was examined. One compound, 4-[3-(4-piperidin-1-yl-but-1-ynyl)-benzyl]-morpholine (9s) was chosen for further profiling and found to be a selective histamine H(3) antagonist with desirable drug-like properties. Ex vivo receptor occupancy studies established that 9s does occupy H(3) binding sites in the brain of rats after oral administration. Subcutaneous doses of 9s (10mg/kg) given during the natural sleep phase demonstrated robust wake-promoting effects.

    PMID:
    19524331
    [PubMed - indexed for MEDLINE]

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