The putative selective inhibitors of calcium-activated chloride channels (T16Ainh-A01, CaCCinh-A01, and MONNA) show poor selectivity in vascular tissue, mediating vasorelaxation independently of chloride gradients.
These compounds should not be viewed as selective TMEM16A blockers in vascular tissue; challenges their utility as research tools and leaves open alternative mechanisms.
T16A(inh) -A01, CaCC(inh) -A01 and MONNA concentration-dependently relax rodent resistance arteries, but an equivalent vasorelaxation occurs when the transmembrane chloride gradient is abolished with an impermeant anion. These compounds therefore display poor selectivity for TMEM16A and inhibition of CaCC in vascular tissue in the concentration range that inhibits the isolated conductance.
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Boedtkjer et al. (2015) studied this question.
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