IndraLab

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PAX inhibits KCNMA1. 8 / 8
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"PAX at 100 nM blocks efficiently and specifically SLO1 channels in human spermatozoa [2]."

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"The whole-cell currents of recorded aSMCs were observed for at least 10 min to reach stability before application of drugs in voltage-clamp mode via bath perfusion/puff application.For recording puff application of drugs that induce postjunctional currents mediated by GluRs, a glass pipette was placed rostrally to the recording electrode at the same depth as the recorded cell.To explore the underlying receptor and ionic mechanisms, selective GluR antagonists NBQX (AMPA/kainate receptor antagonist, 20 μM; Tocris) and D-AP5 (NMDA receptor antagonist, 50 μM; Tocris), as well as the selective BK channel antagonist PAX (10 μM; Tocris) were used."

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"The capacity of the IbTX and PAX used in the killing and phospholipase degradation assays to inhibit BK channel currents was confirmed in cells expressing native BK channels and in COS-7 cells transfected with BK channels."

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"Specific modulations of MLT bursting, including local infusion of BK channel antagonist PAX, MLT-specific optogenetic stimulation and closed-loop DBS, effectively suppress SWDs, increase vigilance, and eliminate frequent spontaneous absence seizures (Fig. 8)."

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"The selective membrane permeable BK channel blocker PAX also induced G2 accumulation and S contraction, and additionally, a G1-phase accumulation at 10 -4 M. Finally, the selective external membrane impermanent BK channel blocker IbTX at 10 -6 M concentration induced a G2-phase accumulation along with a slight contraction of G1 cells."

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"PAX blocked the BK channel and attenuated the BK-channel-derived inward currents (Fig. 4E, F)."

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"In our experiments we used the high affinity BK channel blockers PAX and IbTX to investigate on the relationship between their blocking mechanisms and biological effects such as cell cycle progression and the associated intracellular signaling, the morphological changes, and cell proliferation after a short incubation time."

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"We can also hypothesize that the ability of PAX to inhibit SLO1 channels could be reduced when added together with progesterone."