IndraLab

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NS11021 activates KCNMA1. 13 / 13
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"To gain insight into mechanisms underlying pharmacological modulation of BK channel gating , here we studied mechanisms underlying activation of BK channels by the biarylthiourea derivative , NS11021 , which acts as a smooth muscle relaxant ."
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"The cardioprotective effects of NS11021 induced BK channel activation were studied in isolated, perfused rat hearts subjected to 35 min of global ischemia followed by 120 min of reperfusion."
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"NS11021 activates BK channels over a range of [ Ca2 + ] ."
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"Nevertheless , our studies did not rule out the possibility that NS11021 activates BK channels at other non-mitochondrial organelles considering that cross-talk between intracellular organelles is well recognized [ 69,70,71,72,73,74 ] ."
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"BK channel activation by NS11021 decreases excitability and contractility of urinary bladder smooth muscle."
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"In studies of ischemia and reperfusion in isolated, perfused rat hearts, Bentzen et al. found that mitochondria BK channel activation by NS11021 perfusion reduced tissue damage, decreasing infarct size by more than 70%."
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"The results with 10 microM Ca 2+ establish benchmarks for further analysis of BK channel activation by NS11021."
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"For example, NS11021 activates KCa1.1 with an EC 50 of 400 nM and in contrast to NS1609 exerts no effect on L- or T-type Ca 2+ channels at 30 muM."
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"NS11021 increased BK channel opening by driving the channel to gate from single, brief openings toward bursts of two or more openings with longer lifetime durations."
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"The results with 10 muM Ca2 + establish benchmarks for further analysis of BK channel activation by NS11021 ."
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"NS11021 at concentrations above 0.3 microM activated KCa1.1 in a concentration dependent manner by parallel shifting the channel activation curves to more negative potentials."
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"Synthetic BK channel activators capable of increasing channel-open probabilities have been synthesized by several companies, such as benzoimidazolone derivatives (e.g., NS1619, NS 1608, and NS004), carboxylate compound CGS7181 and its analogues (e.g., CGS7184), 1,4-benzothiazine derivatives, and NS11021 [163]."
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"In the present study, we show that NS11021 activation of BK channel is largely due to stabilization of an open state at the PGD."
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