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Merck

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
RESUMEN

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).

MATERIALES
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Descripción del producto

Sigma-Aldrich
Modafinil, ≥98% (HPLC)
Supelco
Modafinil solution, 1.0 mg/mL in acetonitrile, ampule of 1 mL, certified reference material, Cerilliant®