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BMS 204352 is an activator of large-conductance calcium-activated potassium (KCa1.1/BK) channels that increases KCa1.1 currents in X. laevis oocytes expressing human KCa1.1 in a calcium- and concentration-dependent manner.1 It decreases electrically induced population excitatory postsynaptic potentials (pEPSPs) in vitro in CA1 rat neurons and in anesthetized rats when administered at doses ranging from 0.005 to 1 mg/kg. BMS 204352 (0.001 and 0.3 mg/kg) reduces infarct volume in a rat model of ischemic stroke induced by middle cerebral artery occlusion (MCAO). It decreases edema in the ipsilateral hippocampus, thalamus, and adjacent cortex and time to find the platform in the Morris water maze in a rat model of fluid percussion-induced traumatic brain injury (TBI).2 BMS 204352 also reverses cortical hyperexcitability and reduces hyperactivity and grooming behaviors in the FmrI-/- mouse model of Fragile X syndrome.3 Formulations containing BMS 204352 have been used in the treatment of ischemic stroke.
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1. Targeting acute ischemic stroke with a calcium-
2. The maxi-
3. Potential involvement of impaired BKCa channel function in sensory defensiveness and some behavioral disturbances induced by unfamiliar environment in a mouse model of fragile X syndrome. Neuropsychopharmacology 43(3), 492-502 (2018).