dc.contributor.author | Petzer, Anél | |
dc.contributor.author | Harvey, Brian H. | |
dc.contributor.author | Petzer, Jacobus P. | |
dc.contributor.author | Wegener, Gregers | |
dc.date.accessioned | 2015-10-22T12:40:34Z | |
dc.date.available | 2015-10-22T12:40:34Z | |
dc.date.issued | 2012 | |
dc.identifier.citation | Petzer, 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.issn | 0041-008X | |
dc.identifier.issn | 1096-0333 (Online) | |
dc.identifier.uri | http://hdl.handle.net/10394/14873 | |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0041008X11004625 | |
dc.identifier.uri | https://doi.org/10.1016/j.taap.2011.12.005 | |
dc.description.abstract | Methylene 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.sponsorship | This work was supported by grants from the National Research
Foundation and the Medical Research Council, South Africa. | en_US |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.subject | Methylene blue | en_US |
dc.subject | Azure B | en_US |
dc.subject | Monoamine oxidase | en_US |
dc.subject | Inhibition | en_US |
dc.subject | Reversible | en_US |
dc.subject | Antidepressant | en_US |
dc.title | Azure B, a metabolite of methylene blue, is a high-potency, reversible inhibitor of monoamine oxidase | en_US |
dc.type | Article | en_US |
dc.contributor.researchID | 10727388 - Petzer, Jacobus Petrus | |
dc.contributor.researchID | 12264954 - Petzer, Anél | |
dc.contributor.researchID | 11083417 - Harvey, Brian Herbert | |