An extrapancreatic action of diazoxide to inhibit glucose transport activity on adipocytes.

The effect of diazoxide on 3-O-methylglucose (3-O-MG) transport was studied in isolated rat adipocytes to elucidate its extrapancreatic action. Diazoxide (0.3-3 mmol/L) significantly inhibited 3-O-MG uptake into adipocytes in a basal state or an insulin-stimulated state. The inhibitory effect was mainly due to the inhibition of insulin responsiveness for 3-O-MG uptake. The insulin responsiveness is determined by the capacity in the process of insulin action and in the final glucose transport activity, and diazoxide mainly inhibited the 3-O-MG transport activity itself. Based on these findings, this extrapancreatic action of diazoxide is considered to contribute partially to raising the blood glucose level in children receiving the drug. Diazoxide, as a glucose transport inhibitor, may be a useful tool for studying the issues related to glucose transport or insulin action.