Hyperglycaemia has been observed with exposure to organophosphate insecticides. This study was designed to compare the effects of calcium channel blockers, alpha-adrenergic, beta-adrenergic, and muscarinic receptor blockers, and of free radical scavengers on insulin secretion from diazinon-treated islets of Langerhans isolated from the pancreas of rats using standard collagenase digestion, separation by centrifugation, and hand-picking technique. The islets were then cultured in an incubator at 37 °C and 5 % CO 2 . In each experimental set 1 mL of 8 mmol L -1 glucose plus 125 µg mL -1 or 625 µg mL -1 of diazinon were added, except for the control group, which received 8 mmol L -1 glucose alone. The cultures were then treated with one of the following: 30 µmol L -1 atropine, 100 µmol L -1 ACh + 10 µmol L -1 neostigmine, 0.1 µmol L -1 propranolol, 2 µmol L -1 nifedipine, 50 µmol L -1 phenoxybenzamine, or 10 µmol L -1 alphatocopherol. In all experiments, diazinon signifi cantly reduced glucose-stimulated insulin secretion at both doses, showing no dose dependency, as the average inhibition for the lower dose was 62.20 % and for the higher dose 64.38 %. Acetylcholine and alpha-tocopherol restored, whereas atropine potentiated diazinoninduced hyposecretion of insulin. Alpha-, beta-and calcium channel blockers did not change diazinoninduced effects. These fi ndings suggest that diazinon affects insulin secretion mainly by disturbing the balance between free radicals and antioxidants in the islets of Langerhans and by inducing toxic stress.