RESEARCH MONOGRAPH · KDC-MN-068

Picamilon

May 9, 2026 Kodiac biolabs Research Revised May 30, 2026 2 min read

Our opinion on this compound

48/100

Niacin-GABA prodrug that's been the subject of more enforcement actions than serious research, and probably for good reason

Picamilon is a niacin-GABA conjugate developed at the All-Union Vitamin Research Institute in the late 60s, and the idea was clever in principle: GABA doesn't cross the blood-brain barrier well, niacin does, so attach them and use niacin as a carrier. Once in the CNS, esterase cleavage releases free GABA plus niacin.

Sounds great. The problem is the evidence that this actually works as advertised is much thinner than the elegance of the concept suggests. Pharmacokinetic studies show variable hydrolysis, the released GABA concentrations are probably not high enough to drive meaningful receptor occupancy in most brain regions, and the niacin component is doing some of the perceived effect (the vasodilation flush is real and probably accounts for the "improved cerebral blood flow" claims).

What we like is the basic chemistry concept of using a vitamin as a CNS prodrug carrier. It's an interesting design strategy that informs other prodrug work even if picamilon itself underdelivers.

What we dont like is most of the rest. The Russian clinical literature is old, mostly underpowered, and the indications (anxiety, migraine, post-stroke recovery) are broad enough to be suspicious. The FDA pulled picamilon from the supplement market in 2015 after determining it didn't qualify as a dietary ingredient, which is just a regulatory finding but reflects the underlying issue that the data behind it is weak.

Sourcing is straightforward (the amide coupling is trivial organic chemistry, HPLC purity is achievable), so the compound is honest in that sense. The question is whether anything interesting happens after you take it.

Honestly, for a tool compound to study GABA prodrug strategies or niacin pharmacology, picamilon has some narrow research value. For anything else, the literature just isn't there. We'd rather see researchers work with cleaner GABA-modulating compounds where the mechanism is established than chase the picamilon story.

Evidence: 30
Mechanism: 55
Reliability: 38
Safety: 75
Sourcing: 72
Value: 50
Signal: 35
Staying power: 30

Plain-language summary Intrigue 50 / 100

Picamilon is a Russian-developed conjugate of niacin (vitamin B3) and GABA. The niacin portion carries GABA across the blood-brain barrier. Used in Russia for circulation and anxiety. Not stocked by Kodiac. This monograph is provided for research and educational reference.

Intrigue 0–100 blends mechanism novelty, evidence strength, and translational potential. Kodiac editorial, not peer-reviewed.

Niacin-GABA conjugate

A Soviet-developed niacin-GABA conjugate (N-nicotinoyl-GABA) that crosses the blood-brain barrier and dissociates centrally to release both components.

Abstract

Picamilon (Pikamilon; N-nicotinoyl-GABA; CAS 34562-97-5; molecular formula C10H12N2O3; molecular weight 208.21) is a conjugate of niacin (nicotinic acid) and GABA developed in the Soviet Union in the 1970s. The niacin moiety provides blood-brain barrier permeability that GABA lacks; central hydrolysis releases both components. Niacin produces vasodilation and the GABA produces anxiolytic and mild sedative effects. The combination is approved in Russia for cerebrovascular insufficiency, anxiety, and migraine prophylaxis. Pharmacokinetics: rapid oral absorption; central hydrolysis to niacin and GABA; the niacin component is hepatically conjugated and excreted while GABA is metabolized through normal GABA pathways. Reported research dose ranges in the literature are described in the source monograph. The compound is sold as a research chemical/supplement in the United States though FDA has issued warnings against its sale as a dietary supplement.

Mechanism of action

Niacin-GABA conjugate; central hydrolysis releases both components. Vasodilation + anxiolytic effects.

Reported research dose ranges

50 to 300 mg (reported research dose range).

References

Mirzoyan RS. Picamilon pharmacology. Russian Academy of Medical Sciences publications.

Read the full monograph

The full reference document covers compound identification, discovery and developmental history, mechanism of action, pharmacokinetics, reported research dose ranges, sourcing and quality verification, reconstitution and handling, stack interaction considerations, and a curated reference list. Available as a research-use-only PDF download.

KDC-MN-068

The full reference document is provided strictly for research use only. It reports research dose ranges from the published literature, not instructions for use in humans or animals.

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FOR RESEARCH USE ONLY. Not for medical, diagnostic, or therapeutic purposes. Not for human consumption. All information is provided for research and educational purposes only.

Kodiac sells research compounds for investigative use only.

Picamilon

Abstract

Mechanism of action

Reported research dose ranges

References

Read the full monograph

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Abstract

Mechanism of action

Reported research dose ranges

References

Read the full monograph

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