title: 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).
authors.forename: Derek
authors.initials: D
authors.lastname: Dunn
authors.forename: Rita
authors.initials: R
authors.lastname: Raddatz
authors.forename: Mark A
authors.initials: MA
authors.lastname: Ator
authors.forename: Edward R
authors.initials: ER
authors.lastname: Bacon
authors.forename: Sankar
authors.initials: S
authors.lastname: Chatterjee
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001559:Benzhydryl Compounds / Q000819:agonists / Q000737:chemistry* / Q000493:pharmacokinetics; D000697:Central Nervous System Stimulants / Q000819:agonists / Q000737:chemistry / Q000493:pharmacokinetics; D054314:Drug Inverse Agonism; D006207:Half-Life; D007700:Kinetics; D000077408:Modafinil; D011485:Protein Binding; D011759:Pyrrolidines / Q000819:agonists / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D018100:Receptors, Histamine H3 / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000819:agonists / Q000737:chemistry* / Q000493:pharmacokinetics; D014851:Wakefulness / Q000187:drug effects
chemical_list: D001559:Benzhydryl Compounds; D000697:Central Nervous System Stimulants; D011759:Pyrrolidines; D018100:Receptors, Histamine H3; D013450:Sulfones; D000077408:Modafinil