Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 19, 2010, Pages 5874-5878

  Moree, Wilna J ^a   Li, Bin Feng ^a   Zamani Kord, Said ^a   Yu, Jinghua ^a   Coon, Timothy ^a   Huang, Charles ^a   Marinkovic, Dragan ^a   Tucci, Fabio C ^a   Malany, Siobhan ^a   Bradbury, Margaret J ^a   Hernandez, Lisa M ^a   Wen, Jianyun ^a   Wang, Hua ^a   Hoare, Samuel R J ^a   Petroski, Robert E ^a   Jalali, Kayvon ^a   Yang, Chun ^a   Sacaan, Aida ^a   Madan, Ajay ^a   Crowe, Paul D ^a   Beaton, Graham ^a   more..

^a NEUROCRINE BIOSCIENCES INC   (United States)

Author keywords

Biotransformation; CYP2D6; H1 Antihistamine; H1 Receptor; Histamine; Indene; Insomnia

Indexed keywords

CYTOCHROME P450; G PROTEIN COUPLED RECEPTOR; HISTAMINE H1 RECEPTOR ANTAGONIST; POTASSIUM CHANNEL HERG; RACEMIC DIMETINDENE; UNCLASSIFIED DRUG;

ARTICLE; BIOTRANSFORMATION; CONTROLLED STUDY; DRUG EFFICACY; DRUG HALF LIFE; DRUG METABOLISM; DRUG SELECTIVITY; ELECTROENCEPHALOGRAM; ELECTROMYOGRAM; HUMAN; IN VIVO STUDY; INSOMNIA; NONHUMAN; RACEMIC MIXTURE; RAT;

ANIMALS; CYTOCHROME P-450 CYP2D6; DIMETHINDENE; ELECTROENCEPHALOGRAPHY; HISTAMINE H1 ANTAGONISTS; HUMANS; INDENES; MICROSOMES, LIVER; MODELS, ANIMAL; PYRIDAZINES; RATS; RECEPTORS, HISTAMINE H1; SLEEP INITIATION AND MAINTENANCE DISORDERS; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 77957599564     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.07.117     Document Type: Article

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