Deriglidole (SL 86-0715) is a peripheral adrenergic receptor antagonist that is a selective inhibitor of alpha2 receptors. Deriglidole inhibits colistin and Idazoxan but does not show activity against prazosin and rat cortical and human platelet α2-adrenergic receptors.

Deriglidole is a specific inhibitor of α2-receptors. Deriglidole inhibits the binding of [3H] clonidine and [3H] imidazole x, while showing no inhibitory effect on the binding of [3H] prazosin to rat cortex and human platelet α2-adrenergic receptors. Furthermore, it demonstrates greater effectiveness than idazolide in selectively targeting peripheral receptors.[1]

In mouse pancreatic beta-cells that both deriglidole and SL86.0714 inhibit ATP-sensitive K+ channel with similar potency whereas alpha2-adrenoceptors are blocked only by deriglidole. In diabetic rats, SL84.0418 and deriglidole (10 mg/kg i.p.) fully normalized glucose tolerance whereas SL86.0714 and tolbutamide only slightly improved it. Five min after deriglidole administration in mice a marked and short lasting rise in insulin levels was observed, followed by a progressive reduction of glycemia.[2]