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  • Title: Novel H3 receptor antagonists with improved pharmacokinetic profiles.
    Author: Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Semple G, Ren A, Pereira G, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Lorea J, Grottick AJ.
    Journal: Bioorg Med Chem Lett; 2008 Jul 15; 18(14):4133-6. PubMed ID: 18554904.
    Abstract:
    A new series of H(3) antagonists derived from the natural product Conessine are presented. Several compounds from these new series retain the potency and selectivity of earlier diamine based analogs while exhibiting improved PK characteristics. One compound (3u) demonstrated functional antagonism of the H(3) receptor in an in vivo pharmacological model.
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