Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.
Basic Information
ID: ALA1153519
Journal: J Med Chem
Title: Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.
Authors: Moree WJ, Li BF, Jovic F, Coon T, Yu J, Gross RS, Tucci F, Marinkovic D, Zamani-Kord S, Malany S, Bradbury MJ, Hernandez LM, O'Brien Z, Wen J, Wang H, Hoare SR, Petroski RE, Sacaan A, Madan A, Crowe PD, Beaton G.
Abstract: Analogues of the known H(1)-antihistamine R-dimethindene were profiled as potential agents for the treatment of insomnia. Several highly selective compounds were efficacious in rodent sleep models. On the basis of overall profile, indene 1d and benzothiophene 2a had pharmacokinetic properties suitable for evaluation in night time dosing. Compound 2a did not show an in vivo cardiovascular effect from weak hERG channel inhibition.
CiteXplore: 19663387
DOI: 10.1021/jm900933k
Patent ID: ┄