Structural determinants for histamine H1 affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 17, 2009, Pages 5043-5047

  Aslanian, Robert ^a   Piwinski, John J ^a   Zhu, Xiaohong ^a   Priestley, Tony ^a   Sorota, Steve ^a   Du, Xiao Yi ^a   Zhang, Xue Song ^a   McLeod, Robbie L ^a   West, Robert E ^a   Williams, Shirley M ^a   Hey, John A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Antihistamine; Astemizole; H1; hERG; Terfenadine; Torsades de pointes

Indexed keywords

ANTIHISTAMINIC AGENT; ASTEMIZOLE; DELAYED RECTIFIER POTASSIUM CHANNEL; HISTAMINE H1 RECEPTOR; POTASSIUM CHANNEL HERG; TERFENADINE;

ARTICLE; CARDIOTOXICITY; GUINEA PIG; HEART VENTRICLE ARRHYTHMIA; HEART VENTRICLE FIBRILLATION; HUMAN; IN VITRO STUDY; IN VIVO STUDY; LIPOPHILICITY; NONHUMAN; PATCH CLAMP; QT PROLONGATION; SEDATION; STRUCTURE ACTIVITY RELATION; SUDDEN DEATH; TORSADE DES POINTES;

ANIMALS; ELECTROCARDIOGRAPHY; GUINEA PIGS; HISTAMINE H1 ANTAGONISTS, NON-SEDATING; HUMANS; PROTEIN BINDING; RECEPTORS, HISTAMINE H1; STRUCTURE-ACTIVITY RELATIONSHIP; TERFENADINE; TRANS-ACTIVATORS;

EID: 68349146244     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.07.047     Document Type: Article

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