Specifically, ritanserin acts as a potent inhibitor of diacylglycerol kinase alpha (DGKα).

It has also been used as a reference compound to identify putatively more selective and potent DGKα inhibitors to treat these forms of cancer as well as possibly others.

[13] Ritanserin is the generic name of the drug and its INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name, and BANTooltip British Approved Name.

[14][15][16] Ritanserin was tested in clinical trials for depression,[3] anxiety, schizophrenia,[10] and migraine.

Condensation of this β-keto lactone can be visualized to involve initial attack on the reactive butyrolactone by the primary nitrogen; cyclodehydration of that hypothetical intermediate 3 gives 6-(2-hydroxyethyl)-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one, CID:82612453 (4).