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Coluracetam supplement (MKC-231, BCI-540) is a novel choline absorption enhancer, belonging to the Sitan class derivatives. Its chemical name is N - (2,3-dimethyl-5,6,7,8-tetrahydrofurano [2,3-B] quinolin-4-yl) -2- (2-oxopyrrolidin-1-yl) acetamide. It appears as a white crystalline powder with a solubility of ≥ 20mg/mL in DMSO and is insoluble in water and ethanol. It interacts with the high affinity choline uptake (HACU) process, which is the rate limiting step in the synthesis of the neurotransmitter acetylcholine by inhaling choline into neurons.Coluracetam can increase the HACU rate, allowing more choline to be taken up into neurons, thereby increasing the activity of cholinergic neurons, making it an ideal target for cognitive enhancement.
When cholinergic function is impaired, colchicine can uptake choline into neurons. In the presence of insufficient HACU due to chemical damage, it can maintain cholinergic function or restore cholinergic dysfunction to normal. Through animal experiments, it was found that it can improve the decrease in acetylcholine content in the hippocampus of rats and mice, and alleviate learning disabilities, memory deficits, and cognitive impairments.
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Additional information of chemical compound:
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Coluracetam Supplement COA
Coluracetam supplement (MKC-231), as a novel cognitive enhancement drug, has attracted widespread attention in the fields of neuroscience and drug development in recent years. The following is a detailed description of its uses:
Pharmacological effects
In rat and mouse experiments, Coluracetam demonstrated the ability to improve learning disabilities, memory deficits, and cognitive deficits. For example, in the AF64A induced mouse model of memory impairment, oral administration of Coluracetam at a dose of 0.3-3mg/kg once a day for 11 days can improve memory impairment and hippocampal acetylcholine consumption in mice. AF64A can disrupt the cholinergic system, leading to a decrease in acetylcholine levels and subsequently affecting learning and memory abilities.
Coluracetam improves memory problems induced by AF64A by participating in the high affinity choline uptake (HACU) process, increasing synaptic uptake of choline and promoting acetylcholine synthesis. In a rat model of cognitive and learning disabilities, Coluracetam also showed improvement when administered orally at a dose of 1-3 mg/kg once a day for 8 days. Acetylcholine plays a crucial role in learning and memory processes, and Coluracetam increases acetylcholine levels, enhances the efficiency of information transmission between neural synapses, and helps improve learning and memory abilities.
The main mechanism of action of Coluracetam is to increase the uptake of choline by neural synapses by participating in the HACU process. HACU is the rate limiting step in the synthesis of the neurotransmitter acetylcholine by inhaling choline into neurons. Increasing the HACU rate can enhance the activity of cholinergic neurons. In diseases such as Alzheimer's disease, the cholinergic system is damaged and acetylcholine levels decrease, leading to cognitive dysfunction. Coluracetam improves the function of the cholinergic system and enhances cognitive function by increasing choline uptake and synthesis.
Coluracetam Supplement may have a positive impact on both working memory and long-term memory. From its improvement of AF64A induced working memory deficits in mice and cognitive impairment in rats (which may involve multiple types of memory), it may play a role in different stages of memory formation by regulating the cholinergic system. Working memory mainly involves the temporary storage and manipulation of information, while long-term memory involves the long-term storage and retrieval of information. Coluracetam increases the synthesis and release of acetylcholine, which may affect the neural circuits and synaptic plasticity associated with these memory types, thereby improving different types of memory function
In the model of cerebral ischemia-reperfusion injury, Coluracetam can reduce cerebral infarction volume and neuronal apoptosis, and improve neurological deficits. Cerebral ischemia-reperfusion injury can lead to a series of damage mechanisms such as oxidative stress, inflammatory response, and cell apoptosis in neurons. Coluracetam may exert neuroprotective effects through mechanisms such as antioxidant, anti-inflammatory, and anti apoptotic effects. For example, it may clear free radicals and reduce their damage to neurons.
Coluracetam increases the synthesis and release of acetylcholine, improves cholinergic system function, and helps maintain normal physiological activity of neurons. In addition, its neuroprotective effect may slow down the progression of neurodegenerative diseases and protect neurons from further damage.The neuroprotective mechanism of Coluracetam may involve multiple aspects. In terms of antioxidant activity, it may increase the activity of intracellular antioxidant enzymes such as superoxide dismutase (SOD), glutathione peroxidase (GSH Px), etc., clearing excess free radicals in the body and reducing oxidative stress damage to neurons.
In terms of anti-inflammatory effects, it may inhibit the activation of inflammatory signaling pathways, reduce the production and release of inflammatory factors such as tumor necrosis factor - α (TNF - α), interleukin-1 β (IL-1 β), etc., thereby alleviating the toxic effects of inflammatory reactions on neurons. In terms of anti apoptosis, it may regulate the expression of apoptosis related proteins, such as inhibiting the expression of pro apoptotic protein Bax and increasing the expression of anti apoptotic protein Bcl-2, thereby inhibiting the process of neuronal apoptosis.
Coluracetam may help improve cerebral blood circulation. Although there is relatively little research on this topic, its overall pharmacological effects suggest that good cerebral blood circulation is crucial for maintaining normal neuronal function. Cerebral blood circulation disorders can lead to neuronal hypoxia and malnutrition, which in turn affect the synthesis and release of neurotransmitters and the transmission of information between neurons.
Coluracetam may improve cerebral blood circulation by regulating endothelial cell function, improving hemorheology, and other mechanisms. For example, it may promote the release of nitric oxide (NO) from endothelial cells, which has a vasodilatory effect, thereby increasing cerebral blood flow and ensuring adequate oxygen and nutrient supply to neurons.
In addition to its effect on acetylcholine, Coluracetam may also regulate the activity of other neurotransmitters. Neurotransmitters coordinate with each other in the nervous system, jointly regulating various physiological and psychological processes. Coluracetam may regulate neurotransmitter levels by affecting the synthesis, release, reuptake, and metabolism of neurotransmitters.
For example, it may affect the activity of neurotransmitters such as glutamate and gamma aminobutyric acid (GABA). Glutamate is the most important excitatory neurotransmitter in the central nervous system, while GABA is the main inhibitory neurotransmitter. The balance between them is crucial for maintaining the normal function of the nervous system. Coluracetam regulates the activity of these neurotransmitters, helping to maintain the balance of the neurotransmitter system and further improve neurological function.
Coluracetam may exert antidepressant and anti anxiety effects by increasing the concentration of neurotransmitters such as serotonin and dopamine in the synaptic cleft. Serotonin and dopamine are neurotransmitters closely related to emotion regulation, and their abnormal levels are associated with the occurrence of diseases such as depression and anxiety. Coluracetam promotes choline uptake, which may indirectly affect the metabolism and release of these neurotransmitters.
In addition, it may also affect neural plasticity, promote the growth of neurons and the formation of synapses, improve the function of neural circuits, and thus alleviate symptoms of depression and anxiety.Compared to some existing antidepressant and anti anxiety drugs, Coluracetam may have unique advantages. The existing antidepressant and anti anxiety drugs may have problems such as slow onset and multiple side effects. Coluracetam, as a novel drug, may have a different mechanism of action from existing drugs, with a faster onset time and fewer side effects. However, more clinical studies are currently needed to validate its efficacy and safety in humans.
Coluracetam Supplement may have the ability to scavenge free radicals, which are one of the important factors leading to oxidative stress. In the process of neurological diseases and injuries, a large amount of free radicals are generated, such as superoxide anions, hydroxyl radicals, etc. These free radicals attack the cell membrane, proteins, DNA and other biomolecules of neurons, leading to neuronal damage and death.
Coluracetam may react with certain groups in its chemical structure to eliminate free radicals, thereby reducing the damage of free radicals to neurons. It may also increase the activity of intracellular antioxidant enzymes such as SOD, GSH Px, etc. SOD can dismutate superoxide anions into hydrogen peroxide and oxygen, while GSH Px can reduce hydrogen peroxide to water, thereby reducing oxidative stress damage to cells. Coluracetam enhances the antioxidant defense ability of cells and protects neurons from oxidative stress by increasing the activity of these antioxidant enzymes.
Precautions
Coluracetam presents an intriguing option for those seeking cognitive enhancement, particularly in memory, focus, and mood. While scientific evidence remains preliminary, its unique mechanism of action and low toxicity profile make it a popular choice among nootropic enthusiasts.However, users should approach Coluracetam with caution:
Start with low doses to assess tolerance.
Combine with choline sources to minimize side effects.
Consult a healthcare professional if pregnant, nursing, or on medication.
As research progresses, Coluracetam may cement its place as a safe, effective cognitive enhancer-or reveal new applications in neuroprotection and mental health.
Chemical mechanism of action
The chemical mechanism of the product mainly revolves around the high-affinity choline uptake (HACU) process. It enhances the uptake and utilization of choline by neurons, improving the efficiency of cholinergic neural transmission, thereby exerting cognitive enhancement and neuroprotective effects. The specific mechanism is as follows:
Participation in the HACU process: HACU is the rate-limiting step for choline entering neurons to synthesize the neurotransmitter acetylcholine. Coluracetam enhances the efficiency of this process, increasing the uptake of choline by nerve synapses, thereby accelerating the synthesis of acetylcholine.
Increase cholinergic neuron activity: Acetylcholine is an important neurotransmitter in the central nervous system, involved in cognitive functions such as learning, memory, and attention. Coluracetam enhances the activity of cholinergic neurons by increasing the synthesis of acetylcholine, thereby improving cognitive function.
Restore cholinergic function: In cases where the cholinergic system is impaired (such as in neurodegenerative diseases like Alzheimer's disease), Coluracetam can maintain or restore cholinergic function to normal levels.
Studies have shown that it has a repairing effect on HACU deficiency caused by chemical damage, thereby improving learning disorders, memory deficits, and cognitive deficits.
Neuroprotective effect: Coluracetam also exhibits certain neuroprotective effects. It may protect neurons from damage by regulating neurotransmitter activities and improving cerebral blood circulation, thereby delaying the progression of neurodegenerative diseases.
1. Main Synthetic Route (Convergent Synthesis)
This process adopts a two-fragment condensation method. First, furoquinolinamine and pyrrolidone acetate intermediates are prepared separately, followed by amidation to obtain the final product.
2. Synthesis of Intermediates
2,3-Dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-amine: Using 2-amino-4,5-dimethylfuran-3-carbonitrile and cyclohexanone as raw materials, cyclization is carried out in hot xylene with zinc chloride as the catalyst to yield the key amine intermediate in one step.
Methyl 2-(2-oxopyrrolidin-1-yl)acetate: 2-pyrrolidone reacts with methyl chloroacetate via nucleophilic substitution under alkaline conditions to produce the acylation reagent.
3. Condensation and Purification of Final Product
The two intermediates undergo amidation in a sodium hydride/N-methylpyrrolidone system to form crude coluracetam. The product is purified by recrystallization and chromatographic separation. Its purity is determined to be no less than 98% by HPLC, meeting the quality standards for supplement raw materials.
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