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AZA1 inhibits KCNH2. 7 / 7
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"To determine if AZA1 inhibition of hERG1 current depends on the state of the channel, we compared the time-course of currents recorded during single test pulses applied in the absence of AZA1 and again after a prolonged pulse-free period of AZA1 exposure."
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"AZA1 blocks hERG1 channels heterologously expressed in oocytes."
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"At a saturating concentration (10 muM), AZA1 reduced the peak outward hERG1 current measured at -10 mV in oocytes to 19.0 +/- 2.4% of control (n = 6)."
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"These findings suggest that AZA1 preferentially blocks the open state of hERG1 channels."
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"The mechanism of hERG channel inhibition by AZA1 was investigated further in Xenopus oocytes where it was shown to be an open state dependent blocker and, using mutant channels, to interact with F656 but not with Y652 within the S6 transmembrane domain that forms the channel 's central pore."
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"We propose that AZA1 physically blocks the K + conductance pathway of hERG1 channels by occluding the cytoplasmic mouth of the open pore."
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"Representative traces and replicated experimental data illustrate that hERG currents were inhibited by AZA1 in a concentration dependent manner with a maximum inhibition of 79.5 +/- 1.8% (mean +/- SEM, n = 3) elicited by 1.9 muM AZA1 (XREF_FIG)."
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