IndraLab

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Emodepside activates KCNMA1. 5 / 5
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"Intriguingly we found that emodepside modulated nematode (Ce slo-1), insect (Drosophila, Dm slo) and human (hum kcnma1) SLO channels but that there are discrete differences in the features of the modulation that are consistent with its anthelmintic efficacy."
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"Electrophysiological studies on Ascaris suum are consistent with emodepside activation of SLO-1, but with a slow time course, possibly indicative of a non extracellular binding site within the transmembrane domains [XREF_BIBR]."
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"XREF_BIBR proposed that emodepside either directly or indirectly activates SLO-1 that is present in body wall muscle and motor neurons to produce its inhibitory effects in nematodes."
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"The prevailing view is that emodepside directly or indirectly activates SLO-1 XREF_BIBR, XREF_BIBR."
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"Thus in the presence of low intracellular Ca 2+ (52 nM) where the Dm Slo channel was closed at most voltages and also at higher intracellular Ca 2+ (e.g. 290nM) where the Dm Slo channel shows outward rectification, emodepside consistently induced a linear current-voltage behaviour of the Dm Slo channel (XREF_FIG) indicating a reduction in the rectifying properties of the channel without any shift in reversal potential."
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