KCNQ2 (KV7.2) and KCNQ3 (KV7.3) are voltage-gated K+ channel subunits that underlie the neuronal M current. ICA-27243 is a novel, potent and selective activator of M-current and KCNQ2/Q3 channels. ICA-27243 is structurally distinct from other known KCNQ/M-current activators. It enhances KCNQ channel activation by shifting channel opening to more hyperpolarized potentials. ICA-27243 activates KCNQ currents in Chinese hamster ovary cells expressing recombinant KCNQ2/Q3 heteromultimeric channels with an EC50 of 0.4 μM. ICA-27243 exhibits selectivity for KCNQ2/Q3 over KCNQ4 (20-fold) and KCNQ3/Q5 (>100-fold) and has no effect on GABA-activated chloride channels, neuronal Na+ channels, or voltage-gated Ca2+ channels. In addition, it produces minimal displacement of radioligand binding to a range of central nervous system receptors and transporters. ICA-27243 also suppresses seizure-like activity in an ex vivo hippocampal slice model, and protects against maximal electroshock-induced seizures in mice.
产品描述
A Potent and Selective Opener of KV7.2 and KV7.3 K+ Channels.
产品形式
KCNQ2 (KV7.2) and KCNQ3 (KV7.3) are voltage-gated K+ channel subunits that underlie the neuronal M current. ICA-27243 is a novel, potent and selective activator of M-current and KCNQ2/Q3 channels. ICA-27243 is structurally distinct from other known KCNQ/M-current activators. It enhances KCNQ channel activation by shifting channel opening to more hyperpolarized potentials. ICA-27243 activates KCNQ currents in Chinese hamster ovary cells expressing recombinant KCNQ2/Q3 heteromultimeric channels with an EC50 of 0.4 μM. ICA-27243 exhibits selectivity for KCNQ2/Q3 over KCNQ4 (20-fold) and KCNQ3/Q5 (>100-fold) and has no effect on GABA-activated chloride channels, neuronal Na+ channels, or voltage-gated Ca2+ channels. In addition, it produces minimal displacement of radioligand binding to a range of central nervous system receptors and transporters. ICA-27243 also suppresses seizure-like activity in an ex vivo hippocampal slice model, and protects against maximal electroshock-induced seizures in mice.