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

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

Author information

1
Neurocrine Biosciences, 12780 El Camino Real, San Diego, California 92130, USA.

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.

PMID:
19663387
DOI:
10.1021/jm900933k
[Indexed for MEDLINE]

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