2017
DOI: 10.1038/srep42481
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Abstract: Ivermectin (IVM) is a broad-spectrum anthelmintic drug used to treat human parasitic diseases like river blindness and lymphatic filariasis. By activating invertebrate pentameric glutamate-gated chloride channels (GluCl receptors; GluClRs), IVM induces sustained chloride influx and long-lasting membrane hyperpolarization that inhibit neural excitation in nematodes. Although IVM activates the C. elegans heteromeric GluClα/β receptor, it cannot activate a homomeric receptor composed of the C. elegans GluClβ subu… Show more

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Cited by 7 publications
(7 citation statements)
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“…Our IPSC and single channel data suggest that the potentiating effect of IVM at GluClRs requires several minutes to stabilise [35]. This relatively long delay could reflect the slow binding of IVM directly from the aqueous solution or slow IVM-induced conformational effects at GluClRs once bound [46, 47]. Alternatively, it may reflect a slow accumulation rate of IVM into the membrane, possibly coupled with a slow lateral diffusion rate within the membrane that controls its access to receptor binding sites.…”
Section: Resultsmentioning
confidence: 99%
“…Our IPSC and single channel data suggest that the potentiating effect of IVM at GluClRs requires several minutes to stabilise [35]. This relatively long delay could reflect the slow binding of IVM directly from the aqueous solution or slow IVM-induced conformational effects at GluClRs once bound [46, 47]. Alternatively, it may reflect a slow accumulation rate of IVM into the membrane, possibly coupled with a slow lateral diffusion rate within the membrane that controls its access to receptor binding sites.…”
Section: Resultsmentioning
confidence: 99%
“…In addition, IVM interacts with nAChR (IC 50 156 nM) ( Degani-Katzav et al, 2017 ). It has been hypothesized that inhibition of nAChR downregulates angiotensin-converting enzyme 2 (ACE2) expression and thus reduces the points of entry for SARS-CoV-2 ( Oakes et al, 2018 ).…”
Section: Methodsmentioning
confidence: 99%
“…Others also reported irresponsiveness to Glu in human embryonic kidney (HEK) cells transfected with the wild type GluClβ subunit alone (Slimko et al, 2002; Frazier et al, 2013; Daeffler et al, 2014). Most recently, we succeeded to obtain responses of a few hundred picooamperes in CHO cells transfected with the WT GluClβ subunit alone using the X-tremeGENE HP DNA Transfection Reagent (Roche Life Science); but, in this case, we challenged the cells with 100 mM Glu, and only 4 of 46 cells responded (Degani-Katzav et al, 2017). In contrast, CHO cells co-transfected with both WT GluCl α and β subunits commonly display robust responses to both Glu and IVM (Degani-Katzav et al, 2016).…”
Section: Resultsmentioning
confidence: 99%