Brain-penetrating 2-aminobenzimidazole H1-antihistamines for the treatment of insomnia
2009
Abstract The benzimidazole core of the selective non-brain-penetrating H 1 -antihistamine mizolastine was used to identify a series of brain-penetrating H 1 -antihistamines for the potential treatment of insomnia. Using cassette PK studies, brain-penetrating H 1 -antihistamines were identified and in vivo efficacy was demonstrated in a rat EEG/EMG model. Further optimization focused on strategies to attenuate an identified hERG liability, leading to the discovery of 4i with a promising in vitro profile.
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