Effects of Dichloroacetate on Brain Pyruvate Dehydrogenase

Abstract
The action of dichloroacetate (DCA) on pyruvate dehydrogenase (PDH) activity of rat brain was studied in vitro and in vivo. In a crude brain mitochondrial fraction, DCA inhibits PDH kinase and in rat brain slices this compound increases PDH activity and stimulates glucose oxidation. In the whole animal, i.p. injection of DCA causes activation of brain PDH, indicating that this inhibitor crosses the blood-brain barrier. The same treatment with DCA also produced a large increase in heart PDH activity. Further studies of the effects of DCA on the CNA should lead to results of considerable importance.