Desacetyl-1-nantradol: a selective prostaglandin antagonist.

Progress in understanding the action of specific prostaglandins will be facilitated by the discovery of specific antagonists to different types of prostaglandin receptors. It has been suggested that nantradol, a cannabinoid-related compound with strong analgetic properties, is an antagonist for prostaglandin receptors. The interaction of nantradol with the receptors for prostaglandin D2 and prostaglandin I2/E1 on human platelets was examined. Desacetyl-1-nantradol, the active form of the drug, blocked the binding of prostaglandin D2 to platelets and the PGD2-induced stimulation of adenylate cyclase activity, but had no effect on the interaction of prostaglandin E1 with platelets. The data support the hypothesis that desacetyl-1-nantradol binds selectively to some classes of prostaglandin receptors and also suggest that it may be useful for distinguishing among different types of prostaglandin receptors.