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Sulbutiamine: A peek on its historical discovery

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Please note: This article is strictly for entertainment purpses only. We do not endorse sulbutiamine or any nootropic drug use. Adverse effects and complications of this drug are sole responsibility of the user.

Discovery and history of sulbutiamine

The discovery of sulbutiamine can be traced back to the history of the debilitating vitamin deficiency disease known as beriberi. A Japanese doctor, Takaki Kanehiro first studied beriberi during the late 19th century. During these years, beriberi was a serious disease amongst Japanese sailors. In 1883, Kanehiro discovered that the prevalence of beriberi is unbelievably high amongst navy who travels on a training mission from Japan to Hawaii. With the sustenance and provision of the Japanese Navy, Kanehiro studied beriberi.

On his attempt, he first observed a group of Japanese sailors who took a journey that lasted for more than 9 months traversing along New Zealand and America before arriving to Hawaii. This journey of 376 men led to 169 cases of morbidity and 25 cases of mortality. Another ship was deployed using the same route, except that this crew was fed with a healthier diet of barley, beans, fish, meant and rice. At the end of the second voyage, it was revealed that only 14 got sick during the entire journey and there were no case of mortality.

The results of this rather simple experiment led the Japanese navy and Kanehiro to believe that beriberi is caused by poor diet. Kanehiro also learned that low ranking crew who are only provided rice for their sustenance are at increased risk for contracting beriberi as compared to Japanese naval officers and Western navies who are able to consume a varied diet. Later on, additional studies were conducted on beriberi revealing that it is deficiency syndrome. It was further discovered that it is caused by inadequate intake of vitamin B1 (thiamine) from ingestion of polished rice. Rice bran is one of the primary dietary resources of thiamine.

Amongst others, beriberi was endemic in Asian countries such as Japan because they are dependent on polished white rice for their staple food. As such, Japan took a huge step forward and established a Vitamin B Research Committee to perform scientific investigations regarding thiamine and its derivatives. Thiamine derivatives were of high interest in hopes of synthesizing one that has better pharmacokinetic properties than thiamine itself.

The very first lipophilic thiamine derivative that was discovered was allithiamine. Allithiamine is isolated from garlic. Interest for thiamine derivatives was high because it is unable to diffuse across plasma membranes (blood brain barrier primarily) due to its positive electric thiazole moiety. This now requires thiamine to be carried by high affinity carriers across plasma membranes leading to low transportation. Through further efforts, sulbutiamine came to life.

Sulbutiamine was created through reducing its compound polarity to help it pass the blood brain barrier and reach the brain. Thiamine was oxidized alone which has created a non-polar dimer of two bonded thiamine molecules resulting to sulbutiamine. Through the conversion of thiamine to sulbutiamine, thiamine can now easily sneak into the brain.

Benefits of sulbutiamine

Activity potentiation

Numerous studies have shown that sulbutiamine can help in boosting intelligence. It has been shown to improve decision-making ability, learning capacity, problem-solving capability, planning skills and synaptic plasticity. These benefits are possible primarily due to the ability of sulbutiamine to modulate glutamate leading to activity potentiation.

Sulbutiamine has the ability to facilitate stimulation of the neurotransmitter glutamate, as such, pairing this smart drug with aniracetam and noopept might increase its potency. A lot of evidence also suggests that sulbutiamine can treat individuals suffering from severe degenerative problems such as schizophrenia and Alzheimer’s disease. One study even shows that combining sulbutiamine with an acetylcholinesterase inhibitor (donepezil) can help in improving day life activities and episodic memories of patients with Alzheimer’s.

Asthenia treatment

Sulbutiamine has been considered as a treatment of asthenia – a type of chronic fatigue that is cerebral in origin. Several studies have shown that this drug is clinically effective in reducing asthenic symptoms. Some studies have shown that it has the ability to eliminate all symptoms of asthenia while some have demonstrated that it is able to relieve asthenic symptoms for individuals who suffered mild craniocerebral trauma. Hence, more study needs to be done to assess the efficiency of this thiamine derivative in treating asthenia.

Increased neuronal communication

Some studies have shown that sulbutiamine has the ability to promote efficient communication between the neurons in our brain. This increased neuronal communication leads to faster and more fluid brain transmissions that embody your perceptions and thoughts. For instance, some users will see an enhancement on their mental alertness, overall attention and reflexes. Anecdotal evidence also shows that it can lead to increased motivation and energy levels.

Before taking sulbutiamine however, it is critical that certain level of precautions are done to avoid unwarranted side effects.