Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 9, 2010, Pages 2755-2760

  Stocking, Emily M ^a   Aluisio, Leah ^a   Atack, John R ^a   Bonaventure, Pascal ^a   Carruthers, Nicholas I ^a   Dugovic, Christine ^a   Everson, Anita ^a   Fraser, Ian ^a   Jiang, Xiaohui ^a   Leung, Perry ^a   Lord, Brian ^a   Ly, Kiev S ^a   Morton, Kirsten L ^a   Nepomuceno, Diane ^a   Shah, Chandravadan R ^a   Shelton, Jonathan ^a   Soyode Johnson, Akinola ^a   Letavic, Michael A ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Histamine; Histamine H3

Indexed keywords

1 [2 (4 CYCLOBUTYL [1,4]DIAZEPANE 1 CARBONYL) 4 (3 FLUORO PHENOXY) PYRROLIDIN 1 YL]ETHANONE; HISTAMINE H3 RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; DRUG BINDING; DRUG PENETRATION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; MOUSE; NONHUMAN; RAT; SUBSTITUTION REACTION;

ADMINISTRATION, ORAL; ANIMALS; AZEPINES; BRAIN; DOGS; DRUG EVALUATION, PRECLINICAL; HISTAMINE H3 ANTAGONISTS; HUMANS; MICE; PYRROLIDINES; RATS; RECEPTORS, HISTAMINE H3; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 77950863934     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.03.071     Document Type: Article

References (13)

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13. eff of ∼30 nM.