INSULINOTROPIC ACTION OF THE NON-SULFONYLUREA MOIETY OF GLIQUIDONE INANESTHETIZED RATS

We investigated the insulinotropic action of the non-sulfonylurea moie ty of gliquidone in anaesthetised rats. When administered intravenousl y in 2.5-15.0 nmol g(-1) body weight range, this moiety caused a dose- related biphasic stimulation of insulin release. This coincided with a dose-related decrease in the plasma glucose incremental area over a 3 0-min period after injection of the drug. At close-to-equal dosage (2. 0-2.5 nmol g(-1)), the meglitinide analogue was about 10 times less ef ficient than the parent sulfonylurea in stimulating insulin secretion. We propose that a comparison between the insulinotropic efficiency of distinct hypoglycaemic sulfonylureas and their non-sulfonylurea moiet y may help to identify those structural determinants responsible for t heir insulinotropic action.