Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2 / Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2 / Kv7.3 , Kv7.4 , and Kv7.5 with EC 50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with K i values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and K v7.2 / 3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons.
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