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Synonyms:COLURACETAM;N-(2,3-Dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide;1-Pyrrolidineacetamide,2-oxo-N-(5,6,7,8-tetrahydro-2,3-dimethylfuro[2,3-b]quinolin-4-yl)-;Coluracetam, MKC-231;1-[N-(2,3-DiMethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)carbaMoylMethyl]pyrrolidin-2-one;BCI-540;Coluracetam, >=99%;2-oxo-N-(5,6,7,8-tetrahydro-2,3-dimethyl-furo[2,3-b]quinolin-4-yl)-1-pyrrolidineacetamide
Coluracetam acts primarily as a choline uptake enhancer that selectively affects memory function. It specifically enhances high-affinity choline uptake, increasing levels of the neurotransmitter acetylcholine by providing more of the choline from which it is made. Since acetylcholine is the neurotransmitter most closely associated with memory and cognition, it is believed that this function is the primary source of coluracetam’s nootropic capabilities.
Coluracetam is particularly potent and requires a much smaller dose than other racetam class nootropics. It’s fast-acting, reaching high levels in plasma within 30 minutes of ingestion, but within three hours levels are in decline.
Coluracetam is unregulated in the US and is sold as a dietary supplement, but its legal status varies from country to country. In Canada and the UK, it cannot be legally sold except by prescription, but it can be legally imported and possessed.
Coluracetam (BCI-540) is a nootropic drug of the racetam family.Coluracetam (formerly known as MKC-231) was initially developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer's disease. Coluracetam enhances high-affinity choline uptake (HACU) which is the rate-limiting step of acetylcholine (ACh) synthesis, and is the only known choline uptake enhancer to currently exist. Studies have shown Coluracetam to improve learning impairment on a single oral dose given to rats which have been exposed to cholinergic neurotoxins. Subsequent studies have shown that it may induce long-lasting procognitive effects by changing the choline transporter regulation system.
After the drug failed to reach endpoints in its clinical trials it was in-licensed by BrainCells Inc for investigations into major depression disorder (MDD), after being awarded a "Qualifying Therapeutic Discovery Program Grant" by the state of California.
Findings from its Phase 2a clinical trials have suggested that it would be an ideal medication for co-morbid MDD with generalized anxiety disorder (GAD). BrainCells Inc is currently out-licensing the drug for this purpose. It may also have potential use in prevention and treatment of ischemic retinopathy and retinal and optic nerve injury.
According to BrainCells Inc, Coluracetam is a potential treatment for various diseases and disorders that affect the brain and nervous system. Such diseases and disorders that Coluracetam has the potential of treating and preventing include; ischemic retinopathy and optic nerve injuries. The ability of Coluracetam to reverse the loss of choline production makes it a potential drug for treatment of schizophrenia. These refer to the clinical benefits of Coluracetam.
Coluracetam also has various other benefits that are not clinical. It is helpful in enhancing cognition, improving the memory and better decision making; it does this by increasing choline uptake and synthesis of Acetylcholine. It is also able to reduce cytotoxicity (a state of being toxic to body cells) of the brain, which is usually caused by an influx of calcium in cultured cortical neurons. This occurs when supply of oxygen to the brain is limited. Coluracetam is also an anti-depressant and can therefore be used in treating various forms of depression. It can be effectively used to deal with stress and hangovers by creating feelings of contentment and peace. This is a motivation boosting nootropic, a distinct feature from the other nootropics. Another unique benefit of Coluracetam is that it is beneficial for eyesight. It improves visual recognition and color vision. Coluracetam has also been found to be effective in the treatment of patients experiencing major depressive disorder and general anxiety disorder making this nootropic supplement an effective anti-depressant.
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