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Chem Biol Drug Des. 2013 Mar;81(3):433-5. doi: 10.1111/cbdd.12094.

From an atypical wake-promoting agent to potent histamine-3 receptor inverse agonists.

Abstract

Utilizing atypical wake-promoting agent modafinil (inactive in both rH(3) and hH(3) binding assays) as a launching pad, a series of sulfinyl- and sulfone-derived H(3) receptor inverse agonists were developed. Brain-permeable compound 27, a potent member of the series displayed excellent selectivity against related family members (H(1), H(2), and H(4) receptors).

© 2012 John Wiley & Sons A/S.

PMID:
23205610
[PubMed - indexed for MEDLINE]
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