Picamilon
Picamilon, a nootropic. Conjugate of niacin and GABA, marketed as a nootropic on the premise that the niacin moiety carries GABA across the blood-brain barrier where…
Conjugate of niacin and GABA, marketed as a nootropic on the premise that the niacin moiety carries GABA across the blood-brain barrier where hydrolysis then releases both. The premise is not supported by target data: screened by the FDA against 50 safety-related receptors, ion channels, enzymes and transporters, picamilon bound none of them, in silico or in vitro. Whatever it does is therefore not explained by any characterised receptor interaction, and it is grouped here with the other GABA analogues on structure alone.
PubChem CID 60608 (C10H12N2O3). The mechanism paragraph is a NEGATIVE result and is stated as one: Santillo 2023 (PMID:36668678), an FDA screen, verbatim "picamilon exhibited weak or no binding to the targets when measured in vitro at 10 μM" and "Using two in silico tools, picamilon was not predicted to bind to the targets". This is unusually good evidence for a supplement-market compound and it argues AGAINST the marketed mechanism, so the record says so rather than repeating the vendor claim. cardiovascular is tagged for the niacin moiety's vasodilatory contribution, which is the part of the premise that is chemically uncontroversial. Dose range is supplement-label practice (50-200 mg), NOT from any cited trial.
Sources: PMID:36668678, PMID:20359966