产品描述:
ICA 27243 is an activator of heteromeric voltage-gated potassium channels containing Kv7.2 and Kv7.3 subunits (Kv7.2/Kv7.3).{39323} It enhances rubidium efflux in an agonist-induced rubidium efflux assay using CHO cells expressing Kv7.2/Kv7.3 channels (EC50 = 0.38 µM). ICA 27243 is selective for heteromeric Kv7.2/Kv7.3 channels over homomeric Kv7.4 channels (EC50 = 7.1 µM) and is 100-300-fold selective for Kv7.2/Kv7.3 over Kv7.3/Kv7.5 channels.{69746} It is also selective for Kv7.2/Kv7.3 channels over a panel of neurotransmitter receptors and voltage-gated sodium channel Nav1.2 at 10 µM, as well as GABAA 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).{39323} 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.{69747}