- From an atypical wake-promoting agent to potent histamine-3 receptor inverse agonists.
From an atypical wake-promoting agent to potent histamine-3 receptor inverse agonists.
Chemical biology & drug design (2012-12-05)
Derek Dunn, Rita Raddatz, Mark A Ator, Edward R Bacon, Sankar Chatterjee
PMID23205610
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).