Sulbutiamine (brand name: Arcalion) is a synthetic derivative of thiamine (vitamin B1). As a dimer of two modified thiamine molecules, it is a lipophilic compound that crosses the blood–brain barrier more readily than thiamine and increases the levels of thiamine and thiamine phosphate esters in the brain.
How Japanese Sailors Discovered the Need for a Synthetic Vitamin B1
During WW1, Japanese sailors began to experience symptoms like loss of mental sharpness and fatigue. These turned out to be symptoms of a disease called Beriberi, caused by a deficiency of Vitamin B1 (Thiamine).
To combat these effects, the Japanese sought to develop a version of Vitamin B1 that lasted longer and reached the brain more easily. Because the blood-brain barrier – the thin safety membrane encasing your noggin – is highly polar, molecules that are non-polar can slip through quite easily. Decreasing the polarity of compounds to help them reach the brain has been a tactic known to scientists for a long time. The application of this tactic to Thiamine was to oxidize the substance without any other compounds present, creating a non-polar “dimer” of two bonded-together Thiamine molecules. In this form (Sulbutiamine), the once-polar Thiamine skips much more easily into the brain.
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