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MOREE, Wilna J; LI, Bin-Feng; HERNANDEZ, Lisa M; JIANYUN WEN; HUA WANG; HOARE, Samuel R. J; PETROSKI, Robert E; JALALI, Kayvon; CHUN YANG; SACAAN, Aida; MADAN, Ajay; CROWE, Paul D; ZAMANI-KORD, Said; BEATON, Graham; JINGHUA YU; COON, Timothy; HUANG, Charles; MARINKOVIC, Dragan; TUCCI, Fabio C; MALANY, Siobhan; BRADBURY, Margaret J
Bioorganic & medicinal chemistry letters, 10/2010, Letnik: 20, Številka: 19Journal Article
Analogs of the known H(1)-antihistamine R-dimethindene with suitable selectivity for key GPCRs, P450 enzymes and hERG channel were assessed for metabolism profile and in vivo properties. Several analogs were determined to exhibit diverse metabolism. One of these compounds, 10a, showed equivalent efficacy in a rat EEG/EMG model to a previously identified clinical candidate and a potentially superior pharmacokinetic profile as determined from a human microdose study.
