325457-99-6

ICA-110381 (325457-99-6) is a KCNQ2/Q3 (Kv7.2/7.3) activator, EC50=0.38 μM (KCNQ1 IC50=15 μM).1?KCNQ3/Q5 heterodimers are not affected2. Potently dampens neuronal excitability and displays anticonvulsant activity?in vivo.2

ICA 110381 was used to study the pharmacological activities as it selectively activated human KCNQ2 expressed in Chinese hamster ovary, damped neuronal excitability in rat hippocampal CA1 cell and showed anticonvulsant activity in amygdala-kindled rat.

KV7.1: 0.38 μM (EC₅₀); KV7.3: 0.38 μM (EC₅₀); KV7.1: 15 μM (IC₅₀)

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1) Amato?et al. (2011),?N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy; Sci. ACS Med. Chem. Lett.,?2?481 2) Boehlen?et al. (2013),?The new KCNQ2 activator 4-Chlor-N-(6-chlor-pyridin-3-yl)benzamid displays anticonvulsant potential; Br. J. Pharmacol.,?168?1182