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dc.contributor.authorPetzer, Anél
dc.contributor.authorHarvey, Brian H.
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorWegener, Gregers
dc.date.accessioned2015-10-22T12:40:34Z
dc.date.available2015-10-22T12:40:34Z
dc.date.issued2012
dc.identifier.citationPetzer, A. et al. 2012. Azure B, a metabolite of methylene blue, is a high-potency, reversible inhibitor of monoamine oxidase. Toxicology and applied pharmacology, 258(3):403-409. [https://doi.org/10.1016/j.taap.2011.12.005]en_US
dc.identifier.issn0041-008X
dc.identifier.issn1096-0333 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/14873
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0041008X11004625
dc.identifier.urihttps://doi.org/10.1016/j.taap.2011.12.005
dc.description.abstractMethylene blue (MB) has been shown to act at multiple cellular and molecular targets and as a result possesses diverse medical applications. Among these is a high potency reversible inhibition of monoamine oxidase A (MAO-A) that may, at least in part, underlie its adverse effects but also its psycho- and neuromodulatory actions. MB is metabolized to yield N-demethylated products of which azure B, the monodemethyl species, is the major metabolite. Similar to MB, azure B also displays a variety of biological activities and may therefore contribute to the pharmacological profile of MB. Based on these observations, the present study examines the interactions of azure B with recombinant human MAO-A and -B. The results show that azure B is a potent MAO-A inhibitor (IC50=11 nM), approximately 6-fold more potent than is MB (IC50=70 nM) under identical conditions. Measurements of the time-dependency of inhibition suggest that the interaction of azure B with MAO-A is reversible. Azure B also reversibly inhibits the MAO-B isozyme with an IC50 value of 968 nM. These results suggest that azure B may be a hitherto under recognized contributor to the pharmacology and toxicology of MB by blocking central and peripheral MAO-A activity and as such needs to be considered during its use in humans and animals.en_US
dc.description.sponsorshipThis work was supported by grants from the National Research Foundation and the Medical Research Council, South Africa.en_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.subjectMethylene blueen_US
dc.subjectAzure Ben_US
dc.subjectMonoamine oxidaseen_US
dc.subjectInhibitionen_US
dc.subjectReversibleen_US
dc.subjectAntidepressanten_US
dc.titleAzure B, a metabolite of methylene blue, is a high-potency, reversible inhibitor of monoamine oxidaseen_US
dc.typeArticleen_US
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID12264954 - Petzer, Anél
dc.contributor.researchID11083417 - Harvey, Brian Herbert


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