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From an Atypical Wake‐promoting Agent to Potent Histamine‐3 Receptor Inverse Agonists
Author(s) -
Dunn Derek,
Raddatz Rita,
Ator Mark A.,
Bacon Edward R.,
Chatterjee Sankar
Publication year - 2013
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12094
Subject(s) - inverse agonist , receptor , histamine , chemistry , pharmacology , stereochemistry , combinatorial chemistry , biochemistry , agonist , biology
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).