Nootropic · Depressant

Picamilon

Also called Nicotinoyl-GABA, GABA-NG, Pikamilon

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Common dose · Oral80–140 mg TS

Dosage

Oral

Source	Threshold	Light	Common	Strong	Heavy
TripSit	–	40–80 mg TS	80–140 mg TS	140–250 mg. TS	–

TripSit dose text

TripSit's factsheet also states its doses as text.

Oral Light: 40-80mg Common: 80-140mg Strong: 140-250mg. TS

What dose are you on? (self-reported, unverified)

Read this first. These numbers come from anonymous visitors typing in a box. Nobody checks them. People misjudge, mistype, troll, or take untested products of unknown strength. They are not a dose guide and never override the sourced table above. They exist only so the sourced ranges can be compared with what people say they take. If you are deciding what to take, use the sourced table, start low, and read the risks section.

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Duration

TripSit factsheet

Onset: 10-45 minutes TS
Duration: 2-4 hours TS
Aftereffects: 1-12 hours TS

Mixing

For best safety practice, don't mix this drug with other depressants.

Why: respiratory depression. PsychonautWiki says:

“Respiratory depression (also known as hypoventilation) can be described as a reduced urge to breathe that can be fatal depending on its intensity.” (PsychonautWiki, Respiratory depression, revision 150612)
“... otherwise safe dosages of these compounds can become fatal when combined with even small amounts of other classes of depressant. For example, benzodiazepines combined with opioids are an extremely common cause of fatal respiratory depression. It is therefore strongly discouraged to combine these depressants at any dosage range.” (PsychonautWiki, Respiratory depression, revision 150612)
“The most common cause of substance-related deaths is the combination of depressants (such as opiates, benzodiazepines, or alcohol) with other depressants.” (PsychonautWiki, Responsible drug use, revision 168206)
“This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration.” (PsychonautWiki, dangerous interactions table, "Depressants" row, revision 156847)

Quotes from PsychonautWiki, CC BY-SA 4.0.

Acute combinations: what happens when these are taken close together. Entries backed by a medical journal or agency are listed first.

Backed by medical journals

Awaiting sourcePeer-reviewed reports on acute combinations, from PubMed and the journals the harm reduction sites cite.

Risks and toxicity

Awaiting sourceToxicity, overdose signs and dependence risk from harm reduction sites and journals.

Testing

Awaiting sourceReagent reactions and test kit guidance from a harm reduction testing service.

Effects

Awaiting sourceSubjective and physical effects from PsychonautWiki or TripSit.

Overview

An analogue of GABA that does pass the brain blood barrier, which is then hydrolyzed into GABA and Niacin. In which the GABA could produce an anxiolytic effect. The Niacin as a vasodilator. And is usually used as part of a nootropic stack. TS

Picamilon (also known as N-nicotinoyl-GABA, pycamilon, and pikamilon) is a drug formed by a synthetic combination of niacin and γ-aminobutyric acid (GABA). It was developed in the Soviet Union in 1969 and further studied in both Russia and Japan as a prodrug of GABA.[1][2][3] WP

In Russia, picamilon is sold as a prescription drug. The rights to the drug belong to the Russian pharmaceutical company NPK ECHO ("НПК ЭХО"). It is not approved for sale in the United States and has been deemed an adulterating agent in dietary supplements, with five American companies required to remove their picamilon products from the market in November 2015. However, as recently as 2020, picamilon has been found in pharmaceutical dosages in over-the-counter supplements in the US.[4][5][6] WP

History

Awaiting sourceHistory and culture from Wikipedia or PsychonautWiki, with their citations.

Legal status

Regulation

In the United States, the Food and Drug Administration ruled in 2015 that picamilon does not fit any of the dietary ingredient categories in the Dietary Supplement Health and Education Act of 1994, namely that it is not a vitamin; a dietary mineral; an herb or other botanical; an amino acid; a dietary substance for use by humans to supplement the diet by increasing the total dietary intake; or a concentrate, metabolite, constituent, extract, or combination of any ingredient described above that had been marketed in the United States before 1994. Despite the FDA ruling, picamilon remains an ingredient in supplements marketed as nootropics in the US.[5][6][7] WP

Pharmacology

A Russian study from 1991 showed that picamilon permeated the blood–brain barrier in cats and increased cerebral blood flow. Further work showed it crosses the blood-brain barrier in mice and rats. It is believed that picamilon is hydrolyzed into GABA and niacin, similar to the way tocopheryl nicotinate (vitamin E nicotinate) is hydrolyzed. GABA in the brain would activate GABA receptors, which in theory should have an anxiolytic effect. The second released component, niacin, is a vasodilator. A 2023 assay study showed that picamilon itself is inactive against 50 biological targets, including GABA receptors, despite being a GABA analogue.[8–13] WP

Pharmacokinetics

Plasma picamilon concentrations are generally in the 500–3000 μg/L range during the first few hours after single oral doses of 50–200 mg. It exhibits linear pharmacokinetics with a half-life of 1–2 hours. As discussed previously, the drug undergoes hydrolysis to GABA and nicotinic acid. Urinary excretion of parent drug and the two metabolites accounts for up to 79% of a single dose.[14] WP

Chemistry

Formula: C10H12N2O3 PC
CAS number: 34562-97-5 PC
Molar mass (g/mol): 208.21 PC
IUPAC name (computed by PubChem): 4-(pyridine-3-carbonylamino)butanoic acid PC
SMILES: C1=CC(=CN=C1)C(=O)NCCCC(=O)O PC
InChIKey: NAJVRARAUNYNDX-UHFFFAOYSA-N PC
PubChem CID: 60608
IUPAC name: 4-(Pyridine-3-carbonylamino)butanoic acid WP

User reports

Erowid erowid.org

Listings

Erowid Experience Vault listing

Link as published on TripSit's factsheet.

Bluelight bluelight.org

Listings

Awaiting sourceTrip report threads and this substance's discussion forum.

Reddit reddit.com

Listings

Awaiting sourceTrip report posts and the relevant subreddits.

Pop culture

No references added yet.

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References

Journal / agency Kopelevich VM, Gunar VI. Some approaches to the directed search for new drugs based on nicotinic acid. Pharmaceutical Chemistry Journal. April 1999. doi:10.1007/BF02509934
Journal / agency Mirzoian RS, Gan'shina TS. The new cerebrovascular preparation pikamilon. Farmakologiia i Toksikologiia. 1989. PMID 2707413
Journal / agency Matsuyama K, Yamashita C, Noda A, Goto S, Noda H, Ichimaru Y, Gomita Y. Evaluation of isonicotinoyl-gamma-aminobutyric acid (GABA) and nicotinoyl-GABA as pro-drugs of GABA. Chemical & Pharmaceutical Bulletin. October 1984. doi:10.1248/cpb.32.4089 · PMID 6529802
Journal / agency Avula B, Chittiboyina AG, Sagi S, Wang YH, Wang M, Khan IA, Cohen PA. Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States. Drug Testing and Analysis. March 2016. doi:10.1002/dta.1853 · PMID 26426301
Other FDA sends five warning letters over supplements containing picamilon. 2 December 2015
Journal / agency Cohen PA, Avula B, Wang YH, Zakharevich I, Khan I. Five Unapproved Drugs Found in Cognitive Enhancement Supplements. Neurology. Clinical Practice. June 2021. doi:10.1212/CPJ.0000000000000960 · PMID 34484905 · PMC8382366
Other Welch C. Declaration of Dr. Cara Welch
Journal / agency Dorofeev BF, Kholodov LE. Pikamilon pharmacokinetics in animals. Farmakologiia i Toksikologiia. 1991. PMID 1884802
Journal / agency Duncan KR, Suzuki YJ. Vitamin E Nicotinate. Antioxidants. March 2017. doi:10.3390/antiox6010020 · PMID 28335380 · PMC5384183
Journal / agency Shephard RA. Behavioral effects of GABA agonists in relation to anxiety and benzodiazepine action. Life Sciences. June 1987. doi:10.1016/0024-3205(87)90758-2 · PMID 2884549
Journal / agency Gille A, Bodor ET, Ahmed K, Offermanns S. Nicotinic acid: pharmacological effects and mechanisms of action. Annual Review of Pharmacology and Toxicology. 2008. doi:10.1146/annurev.pharmtox.48.113006.094746 · PMID 17705685
Journal / agency Prousky J, Seely D. The treatment of migraines and tension-type headaches with intravenous and oral niacin (nicotinic acid): systematic review of the literature. Nutrition Journal. January 2005. doi:10.1186/1475-2891-4-3 · PMID 15673472 · PMC548511
Journal / agency Santillo MF, Sprando RL. Picamilon, a γ-aminobutyric acid (GABA) analogue and marketed nootropic, is inactive against 50 biological targets. Basic & Clinical Pharmacology & Toxicology. April 2023. doi:10.1111/bcpt.13836 · PMID 36668678
Journal / agency Cui W, Chen X, Zhan Y, Zhang Z, Zhang Y, Zhong D. Determination of picamilon concentration in human plasma by liquid chromatography-tandem mass spectrometry. Journal of Chromatography B. May 2010. doi:10.1016/j.jchromb.2010.03.013 · PMID 20359966

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), TripSit factsheets, PubChem (public domain). Each value links to the exact revision it came from.