Picamilon (also known as nicotinoyl-GABA) is a compound formed by reacting niacin with GABA. It was developed in the Soviet Union in 1969 by the All-Union Scientific Research Institute and further studied in both Russia and Japan as a prodrug of GABA.

Mechanism of action and potential therapeutic applications

Picamilon is able to cross the blood-brain barrier and then is hydrolyzed into GABA and niacin. The released GABA in theory would activate GABA receptors potentially producing an anxiolytic response. The second released component, niacin acts as a strong vasodilator, which might be useful for the treatment of migraine headaches.


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