Cytochalasin B inhibition of brain glucose transport and the influence of blood components on inhibitor concentration.

The effect of cytochalasin B on cerebral glucose transport and metabolism was investigated in 19 isolated perfused dog brain preparations. Cytochalasin B is a potent, non-competitive inhibitor of glucose transport at the blood-brain interface. Both glucose transport into (Ki = 6.6 +/- 1.9 micrometer) and out of the capillary endothelial cell are inhibited. The inhibition is readily reversible by perfusion with blood containing no cytochalasin B. After 2 min of exposure to 30 micrometer cytochalasin B, the cerebral oxygen consumption decreases by 31% probably due to decreased availability of glucose for oxidative metabolism. About one-half of the cytochalasin B that is dissolved in blood is bound to erythrocytes and other blood components while the remainder is free.