Alpha-GPC (L-alpha-glycerylphosphorylcholine / choline alfoscerate)

Overview

Alpha-GPC is a non-peptide choline-containing phospholipid derivative that serves as an acetylcholine precursor. It is not FDA-approved in the United States, where it is sold as an unregulated dietary supplement and nootropic ingredient. The compound is marketed as a prescription drug in some countries (e.g., Italy as Gliatilin) for cognitive and vascular disorders, though current regulatory approval status has not been confirmed against primary agency databases. Alpha-GPC is not identified as a WADA-prohibited substance in secondary sources.

Mechanism of Action

Choline alfoscerate is hydrolyzed to release choline, which crosses the blood-brain barrier and serves as a substrate for acetylcholine synthesis via choline acetyltransferase; the glycerophosphate moiety can also feed into membrane phospholipid metabolism. In rat hippocampal studies it increased in vivo acetylcholine release, and in aged-rat studies it modulated choline acetyltransferase/acetylcholinesterase activity and attenuated age-related structural changes in hippocampus and frontal cortex. No human pharmacokinetic or mechanistic study (brain uptake kinetics, receptor binding) was located; the mechanism above is sourced to animal and in-vitro pharmacology, not confirmed human mechanistic data.

Research Summary

Human data: A 12-week randomized controlled trial in 100 subjects with amnestic mild cognitive impairment found 600 mg/day improved ADAS-cog scores by 2.34 points versus placebo with no serious adverse events. A single-blind RCT in 39 healthy volunteers showed 400 mg/day for 2 weeks increased self-reported motivation versus placebo. A small crossover study in 7 resistance-trained men (published only as a conference-supplement abstract) reported a single acute 600 mg dose increased post-exercise growth hormone and peak bench-press force versus placebo. A large retrospective Korean cohort study (n=12,008,977 adults ≥50) found chronic alpha-GPC use associated with elevated 10-year stroke risk (total stroke adjusted HR 1.43, ischemic stroke aHR 1.34) in a dose-dependent pattern. Preclinical: Rat studies showed increased hippocampal acetylcholine release, modulation of choline acetyltransferase/acetylcholinesterase activity in aged rats, attenuation of age-related brain structural changes, and increased hippocampal neurogenesis in seizure models.

Prescribers who offer Alpha-GPC (L-alpha-glycerylphosphorylcholine / choline alfoscerate)

1 prescriber in our directory work with Alpha-GPC (L-alpha-glycerylphosphorylcholine / choline alfoscerate), each confirmed from their own website. Peptides like Alpha-GPC (L-alpha-glycerylphosphorylcholine / choline alfoscerate) require a prescription from a licensed provider.

Reported Side Effects

• Elevated 10-year stroke risk (total aHR 1.43, ischemic aHR 1.34) in large Korean cohort, dose-dependent
• Gastrointestinal effects (abdominal pain, constipation, dyspepsia, nausea) in 12-week trial
• Minor, clinically insignificant lab changes (uric acid, cholesterol) in 12-week trial
• No serious adverse events reported in 12-week RCT (600 mg/day)
• No validated long-term safety data beyond 12 weeks

Compare Alpha-GPC (L-alpha-glycerylphosphorylcholine / choline alfoscerate) with Others

Research References

• Choline Alfoscerate, PubChem CID 657272.
• Choline alfoscerate: Uses, Interactions, Mechanism of Action, DrugBank DB04660.
• Efficacy and safety of choline alphoscerate for amnestic mild cognitive impairment: a randomized double-blind placebo-controlled trial. 2024. PMID 39300341.
• Alpha-Glycerylphosphorylcholine Increases Motivation in Healthy Volunteers: A Single-Blind, Randomized, Placebo-Controlled Human Study. 2021. PMID 34207484.

Frequently asked questions

Which prescribers offer Alpha-GPC (L-alpha-glycerylphosphorylcholine / choline alfoscerate) with a prescription?

1 prescriber in the Disclosed Labs directory work with Alpha-GPC (L-alpha-glycerylphosphorylcholine / choline alfoscerate), each confirmed from their own website. Alpha-GPC (L-alpha-glycerylphosphorylcholine / choline alfoscerate) requires a prescription from a licensed provider. Browse them at https://www.disclosedlabs.com/prescribers?peptide=Alpha-GPC%20(L-alpha-glycerylphosphorylcholine%20%2F%20choline%20alfoscerate).

How does Alpha-GPC (L-alpha-glycerylphosphorylcholine / choline alfoscerate) work?

Choline alfoscerate is hydrolyzed to release choline, which crosses the blood-brain barrier and serves as a substrate for acetylcholine synthesis via choline acetyltransferase; the glycerophosphate moiety can also feed into membrane phospholipid metabolism. In rat hippocampal studies it increased in vivo acetylcholine release, and in aged-rat studies it modulated choline acetyltransferase/acetylcholinesterase activity and attenuated age-related structural changes in hippocampus and frontal cortex. No human pharmacokinetic or mechanistic study (brain uptake kinetics, receptor binding) was located; the mechanism above is sourced to animal and in-vitro pharmacology, not confirmed human mechanistic data.

What does the research say about Alpha-GPC (L-alpha-glycerylphosphorylcholine / choline alfoscerate)?

Human data: A 12-week randomized controlled trial in 100 subjects with amnestic mild cognitive impairment found 600 mg/day improved ADAS-cog scores by 2.34 points versus placebo with no serious adverse events. A single-blind RCT in 39 healthy volunteers showed 400 mg/day for 2 weeks increased self-reported motivation versus placebo. A small crossover study in 7 resistance-trained men (published only as a conference-supplement abstract) reported a single acute 600 mg dose increased post-exercise growth hormone and peak bench-press force versus placebo. A large retrospective Korean cohort study (n=12,008,977 adults ≥50) found chronic alpha-GPC use associated with elevated 10-year stroke risk (total stroke adjusted HR 1.43, ischemic stroke aHR 1.34) in a dose-dependent pattern. Preclinical: Rat studies showed increased hippocampal acetylcholine release, modulation of choline acetyltransferase/acetylcholinesterase activity in aged rats, attenuation of age-related brain structural changes, and increased hippocampal neurogenesis in seizure models.