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J Neural Transm Suppl. 2006;(71):105-12.

Inhibition of amine oxidases by the histamine-1 receptor antagonist hydroxyzine.

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Department of Biochemistry, Trinity College, Dublin, Ireland.


The effects of the drug hydroxyzine on the activities of the rat liver monoamine oxidases (EC; MAO) and the membrane-bound and soluble forms of bovine semicarbazide-sensitive amine oxidase (EC; 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.

[Indexed for MEDLINE]

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