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hydroxyzine is a MAO-B inhibitor

Posted by linkadge on July 28, 2007, at 15:51:59

According to the following study, the antihistamine hydroxyzine, sometimes used for sleep, is an inhibitor of MAO-B.

Inhibition of amine oxidases by the histamine-1 receptor antagonist hydroxyzine.
[My paper] J O'Sullivan , M I O'Sullivan , K E Tipton , G Davey
The effects of the drug hydroxyzine on the activities of the rat liver monoamine oxidases (EC 1.4.3.6; MAO) and the membrane-bound and soluble forms of bovine semicarbazide-sensitive amine oxidase (EC 1.4.3.6; SSAO) were studied. Hydroxyzine was found to be a competitive inhibitor of MAO-B (Ki - 38 microM), whereas it had a low potency towards MAO-A (IC50 > 630 microM). Although it was a relatively potent competitive inhibitor of bovine plasma SSAO (Ki approximately 1.5 microM), it was a weak inhibitor of the membrane-bound form of the enzyme from bovine lung (IC50 approximately 1 mM). These findings extend our knowledge of the drug binding capabilities of the amine oxidases and suggest that these interactions may contribute to the complex actions of this drug.


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poster:linkadge thread:772570
URL: http://www.dr-bob.org/babble/20070719/msgs/772570.html