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).

MATERIALS

Product Number

Brand

Product Description

M-084

Supelco

Modafinil solution, 1.0 mg/mL in acetonitrile, ampule of 1 mL, certified reference material, Cerilliant^®

M6940

Sigma-Aldrich

Modafinil, ≥98% (HPLC)

Y0000635

Modafinil, European Pharmacopoeia (EP) Reference Standard

Y0000636

Modafinil for system suitability, European Pharmacopoeia (EP) Reference Standard