Characterization of Novel Selective H1-Antihistamines for Clinical Evaluation in the Treatment of Insomnia.

Analogues of the known H1-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 1dand benzothiophene 2ahad pharmacokinetic properties suitable for evaluation in night time dosing. Compound 2adid not show an in vivo cardiovascular effect from weak hERG channel inhibition. [ABSTRACT FROM AUTHOR]