Digitoxose and the existence of a glucoreceptor in the beta cells of the islets of langerhans of the rat

Abstract On the basis that digitoxin is the only drug reported up to now that stimulating insulin release per se, partially inhibits glucose stimulated insulin release, in this work the idea that the competition glucose-digitoxin may be at the level of a hypothetical glucoreceptor in the beta cells (binding of the glycoside sugar molecule) has been investigated. Our findings indicate that the integrity of the chemical structure of digitoxin is needed to exert its pharmacological action on insulin release. We also demonstrate that digitoxose inhibits glucose stimulated insulin release without inhibiting the glucose oxidation rates of the islets. The discovery of a sugar (digitoxose) that inhibitis the insulin secretory response to glucose without inhibiting glucose metabolism is a strong evidence that the action of glucose itself is blocked at the level of glucoreceptors located in the cell membrane, which appear to be the regulator sites of insulin release.