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L-Alpha glycerylphosphorylcholine (alpha GPC, choline alfoscerate) is a choline compound naturally found in the human body and in dietary sources such as milk and soy. It is concentrated in the brain, especially in neuronal membranes, where it acts as a precursor to phosphatidylcholine. Phosphatidylcholine, despite often being referred to in the singular, is actually a class of phospholipids that contain an invariable alpha GPC moiety and two variable fatty acids. In the nervous system, phosphatidylcholines play important roles in membrane fluidity and membrane-mediated cellular signaling processes.
Alpha GPC also provides choline for the synthesis of acetylcholine (ACh), an important neurotransmitter involved in many functions in both the central and peripheral nervous systems. In the central nervous system, ACh is critical to the overarching processes of attention, focus, and plasticity that undergird learning and memory. Alpha GPC is readily absorbed in the digestive tract and effectively passes the blood-brain barrier. Clinical research utilizing alpha GPC has concentrated on functional cognitive effects and neuronal protection.*
A good amount of alpha GPC research has involved simulating cognitive decline and memory impairment in humans through the administration of scopolamine, a renowned compound found in species of the nightshade family, and determining the protective effects of alpha GPC. This is a useful model because scopolamine depletes acetylcholine stores, inducing a transitory cognitive impairment similar to that observed in normal aging. In vitro and animal studies have suggested that alpha GPC enhances hippocampal cholinergic transmission (critical for memory) by increasing acetylcholine synthesis and release.*
In one study, thirty-two healthy, young volunteers received either 1200mg/day of alpha GPC or placebo for 10 days and also received either scopolamine bromidrate or placebo on day 11. Those who received alpha GPC and scopolamine showed significant benefits to attention and recall performance compared to those who received placebo and scopolamine.* Interestingly, even those who received alpha GPC but not scopolamine showed significant enhancement of recall performance compared to those who received neither alpha GPC nor scopolamine.*
In another double-blind, placebo-controlled trial, 48 young men and women were administered 1200mg/day alpha GPC, idebenone, aniracetam, or placebo for 7 days. Idebenone and aniracetam are known cognitive stimulants. On day 8, subjects received scopolamine. Alpha GPC enhanced learning, working memory, and long-term verbal memory, and the effects were significantly better than those seen with idebenone, aniracetam, or placebo usage.*
Generates Protection Cortically*
When choline availability declines, cholinergic cells go through autocannibalism to withdraw choline from phosphatidylcholine. However, when the choline or phosphatidylcholine supply is not replenished, cells lose their ability to efficiently communicate due to the loss of membrane phospholipids that are critical for signal transduction and normal cellular functions. Supplementation of alpha GPC can help replenish both choline and phosphatidylcholine, which help maintain healthy neuronal membranes and neurotransmitter production.*
In one study, animals given alpha GPC were observed to display adaptive and reparative reactions such as an increased number of ribosomes and hypertrophy of endoplasmic reticulum and Golgi complex. Furthermore, the structures of the nuclear membranes and cellular organelles were better preserved compared to animals given the common nootropic agent piracetam. In addition, in vitro work using human brain slices has found that alpha GPC inhibits lysophospholipase, thus modulating membrane phospholipid breakdown and protecting neuronal cells from self-degradation.*
The pharmacokinetic profile of oral alpha GPC has been investigated in male and female rats given alpha GPC radio-labeled with either 14C-glycerol or 14C-choline. Hours after ingestion, both species were found concentrated in the brain. Furthermore, the labeled choline was observed in brain phospholipids within 24 hours of dosing. Excretion of labeled alpha GPC was minimal and comparable for both forms. These results suggest that oral alpha GPC is well absorbed, efficiently crosses the blood brain barrier, and concentrates in the brain.*
Alpha GPC (L-alpha glycerylphosphorylcholine, also known as choline alfoscerate) is a phospholipid metabolite found concentrated in neuronal membranes. Derived from lecithin, alpha GPC is extremely well absorbed and crosses the blood brain barrier.* In the brain, alpha GPC supports brain function and learning processes by directly increasing the synthesis and secretion of acetylcholine.* Alpha GPC protects neurons and improves signal transmission by serving as a precursor to membrane phospholipids
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