Agmatine is not a good candidate as endogenous ligand for imidazoline sites of pancreatic B cells and vascular bed.

In order to determine whether agmatine could be a putative endogenous ligand for imidazoline receptors mediating insulin secretion and vasoconstriction, we compared its effects with those of the imidazoline, efaroxan. Agmatine exhibited a much lower potency and efficacy than efaroxan on insulin secretion from rat pancreas perfused with 8.3 mM glucose. On the other hand, in contrast to efaroxan (100 microM), agmatine (3 mM) did not increase arginine-induced insulin release. In addition, agmatine failed to reproduce the vasoconstrictor effect of efaroxan on pancreatic vessels. These results show that agmatine does not behave like efaroxan, an agonist for the imidazoline receptors mediating insulin secretion or vasoconstriction in the pancreas.