Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.

Autor: Letavic MA; Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. mletavic@prdus.jnj.com, Aluisio L, Atack JR, Bonaventure P, Carruthers NI, Dugovic C, Everson A, Feinstein MA, Fraser IC, Hoey K, Jiang X, Keith JM, Koudriakova T, Leung P, Lord B, Lovenberg TW, Ly KS, Morton KL, Motley ST, Nepomuceno D, Rizzolio M, Rynberg R, Sepassi K, Shelton J
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Jul 15; Vol. 20 (14), pp. 4210-4. Date of Electronic Publication: 2010 May 16.
DOI: 10.1016/j.bmcl.2010.05.041
Abstrakt: The pre-clinical characterization of novel aryloxypyridine amides that are histamine H(3) receptor antagonists is described. These compounds are high affinity histamine H(3) ligands that penetrate the CNS and occupy the histamine H(3) receptor in rat brain. Several compounds were extensively profiled pre-clinically leading to the identification of two compounds suitable for nomination as development candidates.
(2010 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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