Pikamilon-a new vasoactive and nootropic preparation

Picamilon, a γ‐aminobutyric acid (GABA) analogue and marketed nootropic, is inactive against 50 biological targets

“…Among the targets selected in this study, it is possible that picamilon could bind to less common binding sites or subunits that were not considered (although functional cell‐based assays may identify these interactions). Also, since picamilon is hydrolysed to GABA and nicotinic acid, the elevated levels of these two compounds could still affect the brain, which were demonstrated in animal studies 1–3 . Overall, these data show that picamilon, although structurally similar to other GABA analogues, has a different biological target binding profile, which we determined by in silico and in vitro methods.…”

“…Also, since picamilon is hydrolysed to GABA and nicotinic acid, the elevated levels of these two compounds could still affect the brain, which were demonstrated in animal studies. [1][2][3] Overall, these data show that picamilon, although structurally similar to other GABA analogues, has a different biological target binding profile, which we determined by in silico and in vitro methods. Picamilon's lack of target binding fills important data gaps among GABA analogues, a group of structurally related substances found in drugs and products marketed as dietary supplements.…”

“…Picamilon is a structural analogue of γ‐aminobutyric acid (GABA), a neurotransmitter that regulates a variety of brain functions including mood and anxiety, along with nicotinic acid, which are linked by an amide bond. It serves as a prodrug, 3 which can pass through the blood–brain barrier and then hydrolyse to nicotinic acid and GABA, which are believed to be responsible for effects in the brain 2,3 …”

Determination of picamilon concentration in human plasma by liquid chromatography–tandem mass spectrometry

“…Picamilon is a derivative of ␥-aminobutyric acid (GABA) and nicotinic acid developed in 1970 by the All-Union Vitamin Research Institute [1]. Because it can dramatically increase blood flow and circulation within the brain, picamilon is used as a nootropic [2].…”

“…Also used for the treatment of depression, anxiety, and migraine [3], picamilon works by crossing the blood-brain barrier, after which it is hydrolyzed into GABA and nicotinic acid [4]. In addition, picamilon has extremely low toxicity and shows no allergenic or carcinogenic properties [1]. An animal study has shown that picamilon is rapidly absorbed (T max = 0.23 h) and penetrates well through the blood-brain barrier in mice [5].…”