2015
DOI: 10.3109/00498254.2015.1051604
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Characterization of midazolam metabolism in locusts: the role of a CYP3A4-like enzyme in the formation of 1′-OH and 4-OH midazolam

Abstract: 1. The metabolism of midazolam was investigated in vivo in locusts in order to evaluate the presence of an enzyme with functionality similar to human CYP3A4/5. 2. Hydroxylated metabolites of midazolam identical to human metabolites were detected in locusts and the apparent affinities (Km values) were in the same range as reported in humans (in locusts: 7-23 and 33-85 µM for the formation of the 1'-OH and 4-OH metabolites, respectively). 3. The formation of hydroxylated metabolites could successfully be inhibit… Show more

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Cited by 18 publications
(17 citation statements)
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“…Other hydroxylated toxins that could be X-class EcKL substrates include withanolides, cardenolides, cucurbitacins and flavonoids (Agrawal et al, 2012; Dinan et al, 1997; Glotter, 2011; S. Wang et al, 2017). X-class EcKLs may also phosphorylate the products of phase I hydroxylation reactions or phase II glucosidation reactions, as is speculated to occur in locusts and moths (Boeckler et al, 2016; Olsen et al, 2015; 2014).…”
Section: Discussionmentioning
confidence: 99%
“…Other hydroxylated toxins that could be X-class EcKL substrates include withanolides, cardenolides, cucurbitacins and flavonoids (Agrawal et al, 2012; Dinan et al, 1997; Glotter, 2011; S. Wang et al, 2017). X-class EcKLs may also phosphorylate the products of phase I hydroxylation reactions or phase II glucosidation reactions, as is speculated to occur in locusts and moths (Boeckler et al, 2016; Olsen et al, 2015; 2014).…”
Section: Discussionmentioning
confidence: 99%
“…Other, although quite different, examples of whole‐body imaging are the imaging studies on insects, including MALDI imaging of the rove beetle Paederus riparius by Spengler and co‐workers and DESI imaging of locusts by our group . In our work on the locusts we found cryo‐sectioning of the whole insects, although possible after careful embedding also quite difficult, mainly due to crispy but also very heterogeneous nature of the locust body‐tissue.…”
Section: Introductionmentioning
confidence: 93%
“…Whereas, terfenadine acid, terfenadine glucoside, and terfenadine phosphate were mainly distributed in the unexcreted feces and in the lower part of the intestine, suggesting a very rapid discharge of metabolites through feces. Similarly, Olsen et al (2016) studied the temporal distribution of midazolam and its glucose conjugates in locust, showing that midazolam was detected in abundance after 30 min of midazolam application, and was only found in the feces after 2 hr. Correspondingly, midazolam glucoside was also primarily found in the intestine, gastric caeca, and feces after 2 hr of application.…”
Section: Insect Exogenous Metabolitesmentioning
confidence: 99%