From an Atypical Wake-promoting Agent to Potent Histamine-3 Receptor Inverse Agonists


Corresponding author: Sankar Chatterjee,


Utilizing atypical wake-promoting agent modafinil (inactive in both rH3 and hH3 binding assays) as a launching pad, a series of sulfinyl- and sulfone-derived H3 receptor inverse agonists were developed. Brain-permeable compound 27, a potent member of the series displayed excellent selectivity against related family members (H1, H2, and H4 receptors).