Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.

Article Details

Citation

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

Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.

J Med Chem. 2009 Sep 10;52(17):5307-10. doi: 10.1021/jm900933k.

PubMed ID
19663387 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DimetindeneHistamine H1 receptorKi (nM)0.4N/AN/ADetails