Picamilon (Pic)

Picamilon is a dietary supplement formed by combining niacin with GABA. 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. A rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the determination of picamilon concentration in human plasma. Picamilon was extracted from human plasma by protein precipitation. The injections of piracetam and picamilon showed a tendency to restoration of the number of active GABA-A receptors and to normalization of the behavioral parameters.