Neuroscience Research Compound · For laboratory research use only

Alpha GPC

Also known as Choline Alfoscerate

Formula
C8H20NO6P
CAS
28319-77-9

Overview

Alpha GPC (L-alpha-glycerylphosphorylcholine, choline alphoscerate) is a choline-containing phospholipid derivative described as a precursor in the biosynthesis of brain phospholipids and as a cholinergic precursor that increases the availability of acetylcholine3,6.

Preclinical studies have examined hippocampal acetylcholine synthesis and release, cholinergic transporters and receptors, protein kinase C translocation and inflammatory markers in rat brain1,2,3,4,5. It has also been examined in clinical research, including the ASCOMALVA trial6,7.

Mechanism of action

As described in the research literature

As described in the research literature, alpha GPC increased hippocampal acetylcholine release in rats, measured by in vivo microdialysis and in tissue slices, and radiolabelled alpha GPC gave rise to radiolabelled acetylcholine in rat studies, consistent with its use as a substrate for acetylcholine synthesis1.

A comparison with CDP-choline in rats reported region-specific changes in acetylcholine levels and in expression of the vesicular acetylcholine transporter (VAChT) and the choline transporter (CHT) across frontal cortex, striatum and cerebellum4. Other work reported protein kinase C translocation in rat cortex in vivo and in cortical slices2, and partial preservation of hippocampal muscarinic M1 receptor sites in aged rats3.

Research areas

What published studies have examined

Cholinergic transmission and scopolamine models

Rat studies examined scopolamine-induced impairment of passive avoidance learning and retrograde amnesia, together with hippocampal acetylcholine synthesis and release by microdialysis and in tissue slices1.

Sources [1]

Transporters, receptors and signalling

Muscarinic M1 and M2 receptors were examined by radioreceptor assay and autoradiography in the hippocampus of young, adult and aged rats3. Other rat studies measured VAChT and CHT expression by Western blot, ELISA and immunohistochemistry4, and protein kinase C activity in soluble and particulate fractions of brain tissue2.

Sources [2] [3] [4]

Neuroinflammation markers

A two-week rat study measured interleukin-1 beta, interleukin-6, TNF-alpha, ICAM-1 and VCAM-1 in the frontal cortex, hippocampus and cerebellum after choline or alpha GPC and reported no change in these markers5. An erratum to this paper was published in 2024.

Sources [5]

Clinical research

ASCOMALVA is a double-blind, multicentre, randomised trial designed to compare donepezil plus choline alphoscerate with donepezil plus placebo in Alzheimer's disease with ischaemic cerebrovascular injury, using cognitive, functional and behavioural assessments that include the MMSE and ADAS-cog7. A review from the same group summarises preclinical and clinical work6.

Sources [6] [7]

Specifications

Molecular formula
C8H20NO6P
Molecular weight
257.22 g/mol
CAS number
28319-77-9
Form
Measured units with a stated amount per unit, 30 to a resealable foil pouch
Storage
Store in a cool, dry place in the sealed pouch, away from direct light. The compound is hygroscopic, so keep the pouch closed between uses.
Solubility and reconstitution
Supplied ready to use: each unit is pre-measured, so no reconstitution is required.

References

  1. 1

    L-alpha-glycerylphosphorylcholine antagonizes scopolamine-induced amnesia and enhances hippocampal cholinergic transmission in the rat.

    Sigala S, Imperato A, Rizzonelli P, et al. European Journal of Pharmacology, 1992.

  2. 2

    PKC translocation in rat brain cortex is promoted in vivo and in vitro by alpha-glycerylphosphorylcholine, a cognition-enhancing drug.

    Govoni S, Battaini F, Lucchi L, et al. Annals of the New York Academy of Sciences, 1993.

  3. 3

    Muscarinic cholinergic receptors in the hippocampus of aged rats: influence of choline alphoscerate treatment.

    Amenta F, Liu A, Zeng YC, et al. Mechanisms of Ageing and Development, 1994.

  4. 4

    Effect of choline-containing phospholipids on brain cholinergic transporters in the rat.

    Tayebati SK, Tomassoni D, Di Stefano A, et al. Journal of the Neurological Sciences, 2011.

  5. 5

    Choline and Choline alphoscerate Do Not Modulate Inflammatory Processes in the Rat Brain.

    Tayebati SK, Martinelli I, Moruzzi M, et al. Nutrients, 2017.

  6. 6

    Choline alphoscerate (alpha-glyceryl-phosphoryl-choline) an old choline- containing phospholipid with a still interesting profile as cognition enhancing agent.

    Traini E, Bramanti V, Amenta F Current Alzheimer Research, 2013.

  7. 7

    The ASCOMALVA trial: association between the cholinesterase inhibitor donepezil and the cholinergic precursor choline alphoscerate in Alzheimer's disease with cerebrovascular injury: interim results.

    Amenta F, Carotenuto A, Fasanaro AM, et al. Journal of the Neurological Sciences, 2012.

This page is provided for research and educational reference only. It does not constitute medical advice, dosing guidance, or a recommendation for use. All compounds are strictly for laboratory and in-vitro research purposes.

RUO. For research purposes only. Not for human consumption. Not for veterinary use.

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