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Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.
Letavic, Michael A; Aluisio, Leah; Atack, John R; Bonaventure, Pascal; Carruthers, Nicholas I; Dugovic, Christine; Everson, Anita; Feinstein, Mark A; Fraser, Ian C; Hoey, Kenway; Jiang, Xiaohui; Keith, John M; Koudriakova, Tatiana; Leung, Perry; Lord, Brian; Lovenberg, Timothy W; Ly, Kiev S; Morton, Kirsten L; Motley, S Timothy; Nepomuceno, Diane; Rizzolio, Michele; Rynberg, Raymond; Sepassi, Kia; Shelton, Jonathan.
Affiliation
  • Letavic MA; Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. mletavic@prdus.jnj.com
Bioorg Med Chem Lett ; 20(14): 4210-4, 2010 Jul 15.
Article in En | MEDLINE | ID: mdl-20561786
ABSTRACT
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridines / Azepines / Histamine H3 Antagonists Type of study: Diagnostic_studies Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Document type: Article Affiliation country:
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridines / Azepines / Histamine H3 Antagonists Type of study: Diagnostic_studies Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Document type: Article Affiliation country: