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Background
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An anticonvulsant used in the treatment of epilepsy, anorexia nervosa, panic attack, anxiety disorder, post traumatic stress disorder, migraine and bipolar disorder. Valproate is also a histone deacetylase inhibitor (IC50 = 400 uM) that exhibits anticancer, anti-inflammatory and neuroprotective effects. Displays anticonvulsive activity via an increase in GABA levels and decreases Abeta production in animal models of Alzheimer's disease. Also attenuates NMDA-mediated excitation, blocks voltage-gated Na+ channels and modulates firing of neurons. Enables induction of pluripotent stem cells from somatic cells by Oct4 and Sox2. Valproic acid also inhibits glycogen synthase kinase 3 (GSK3) and depletes cellular inositol-1,4,5-trisphosphate (1,4,5-IP3). Valproic acid shows promise in combination therapy for cancer and in treating Alzheimer's disease. Inhibits Class I HDACs with an IC50 value of approx.2 mM.
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