ML133 is a potent and selective blocker of the inwardly rectifying Kir2 potassium channel, IC50s = 1.8, 2.8, 2,9, and 4.0 µM for Kir2.1, Kir2.6, Kir2.2, and Kir2.3, respectively.1 Intrathecal injection of ML133 attenuated the proliferation of microglia and neuropathic pain behaviors after nerve injury.2 ML133 inhibits microglial priming pointing to Kir2.1 channels as a new therapeutic target for neuronal damage.3 Moreover, treatment with ML133 one hour post-injury was sufficient to improve neuronal survival in a traumatic brain injury human organoid model.4
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