ICA 27243

ICA 27243 is an activator of heteromeric voltage-gated potassium channels containing K_v7.2 and K_v7.3 subunits (K_v7.2/K_v7.3).¹ It enhances rubidium efflux in an agonist-induced rubidium efflux assay using CHO cells expressing K_v7.2/K_v7.3 channels (EC₅₀ = 0.38 µM). ICA 27243 is selective for heteromeric K_v7.2/K_v7.3 channels over homomeric K_v7.4 channels (EC₅₀ = 7.1 µM) and is 100-300-fold selective for K_v7.2/K_v7.3 over K_v7.3/K_v7.5 channels.² It is also selective for K_v7.2/K_v7.3 channels over a panel of neurotransmitter receptors and voltage-gated sodium channel Na_v1.2 at 10 µM, as well as GABA_A receptors and high voltage-activated calcium channels at 30 µM. ICA 27243 protects against maximal electroshock-induced seizures in a rat model of epilepsy (ED₅₀ = 1.5 mg/kg).¹ It also prevents hyperactivity induced by amphetamine and chlordiazepoxide, but not by amphetamine alone, without affecting basal locomotor activity in a mouse model of manic-like hyperactivity when administered at a dose of 10 mg/kg.³

WARNING This product is not for human or veterinary use.

1. Amato, G., Roeloffs, R., Rigdon, G.C., et al. N-Pyridyl and pyrimidine benzamides as KCNQ2/Q3 potassium channel openers for the treatment of epilepsy. ACS Med. Chem. Lett. 2(6), 481-484 (2011).

2. Wickenden, A.D., Krajewski, J.L., London, B., et al. N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide (ICA-27243): A novel, selective KCNQ2/Q3 potassium channel activator. Mol. Pharmacol. 73(3), 977-986 (2008).

3. Redrobe, J.P., and Nielsen, A.N. Effects of neuronal K_v7 potassium channel activators on hyperactivity in a rodent model of mania. Behav. Brain Res. 198(2), 481-485 (2009).