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The KCNQ (Kv7) family of voltage-gated potassium (K+) channels consists of five members, KCNQ1-KCNQ5. KCNQ1-KCNQ5 are critical for setting up the excitation threshold of action potentials. KCNQ1 is expressed mainly in cardiac tissue, peripheral epithelial cells, and smooth muscle cells, while KCNQ2-KCNQ5 are predominantly expressed in the peripheral and central nervous system, including hippocampal cells, cortical cells, and dorsal root ganglion. ML-213 is a selective activator of KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) channels (EC50s = 230 and 510 nM for KCNQ2 and KCNQ4, respectively) that demonstrates > 80-fold selectivity against other related K+ channels.1
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1. Discovery, synthesis, and structure-