Aceglutamide CAS 2490-97-3
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Aceglutamide CAS 2490-97-3

Aceglutamide CAS 2490-97-3

Product Code: BM-2-5-170
English name: Aceglutamide
CAS No.: 2490-97-3
Molecular formula: C7H12N2O4
Molecular weight: 188.18
EINECS No.: 219-647-7
MDL No.: MFCD00038159
Hs code: 29241990
Main market: USA, Australia, Brazil, Japan, UK, New Zealand , Canada etc.
Manufacturer: BLOOM TECH Yinchuan Factory
Technology service: R&D Dept.-1
Usage: Pharmacokinetic study, receptor resistance test etc.

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Aceglutamide is an organic compound that is an acetylate of glutamine, with the chemical formula C7H12N2O4, CAS 2490-97-3, White crystalline powder, odorless. Easy to dissolve in water, slightly soluble in ethanol, soluble in ethyl acetate. Has the effect of improving nerve cell metabolism, maintaining nerve stress ability, and reducing blood ammonia. It can also be used for brain injury coma, liver coma, hemiplegia, high paraplegia, sequelae of infantile paralysis, sequelae of brain injury, intellectual disability, neuropathic headache, back pain, etc. through the blood-brain barrier.

Produnct Introduction

Chemical Formula

C7H12N2O4

Exact Mass

188

Molecular Weight

188

m/z

188 (100.0%), 189 (7.6%)

Elemental Analysis

C, 44.68; H, 6.43; N, 14.89; O, 34.01

Aceglutamide structure CAS 2490-97-3 | Shaanxi BLOOM Tech Co., Ltd

Aceglutamide | Shaanxi BLOOM Tech Co., Ltd

Usage

The functions of acetylglutamine mainly include the following:

Aceglutamide blood | Shaanxi BLOOM Tech Co., Ltd

Reduce blood ammonia

 

This substance has the effect of reducing blood ammonia. Related research experiments have shown that it is distributed in various parts of the human body, especially in renal tubular cells, and decomposes ammonia in the blood into acetyl glutamate. Ammonia in the blood is excreted through renal tubular cells.

Detoxification mechanism

 

In addition, the compound also has a detoxification mechanism. After entering the human body, it will pass through the blood-brain barrier and decompose glutamate, which can directly participate in the information transmission process of the central nervous system. However, other substances decomposed can inhibit the excitability of glutamate. These two substances compete with each other and can effectively improve nerve cells, achieving the effect of improving brain function.

Aceglutamide uses | Shaanxi BLOOM Tech Co., Ltd
Aceglutamide neurological | Shaanxi BLOOM Tech Co., Ltd

Improve neurological disorders

 

This compound can be used to treat cerebral embolism and motor dysfunction. Relevant medical experimental data shows that it has the effect of promoting cell growth, and therefore can be used as a nutritional support material during high-intensity training recovery processes. This compound can cross the blood-brain barrier, break down into glutamate and gamma aminobutyric acid (GABA), improve neuronal metabolism, and maintain good stress function. In clinical practice, it is commonly used for severe neurological disorders such as traumatic coma, neurosurgical coma, and hepatic coma.

Relieve neuropathic pain

 

Promoting neurological function recovery: For motor dysfunction caused by neurological injuries such as hemiplegia, high paraplegia, and sequelae of infantile paralysis, this substance can help promote neurological function recovery and improve patients' motor abilities.
Relieve neuropathic pain and headache: This substance can also be used to treat symptoms such as neuropathic headache and lower back pain, by regulating neurotransmitter levels to alleviate patient pain.

Aceglutamide pain | Shaanxi BLOOM Tech Co., Ltd

Manufacturing Information

Aceglutamide synthesis is L- γ- Glutamic acid is obtained by esterification, amination and acetylation.

 

1. Esterification: add methanol into the dry reaction tank, and slowly add sulfuric acid after stirring. Cool to below 20 ℃, add L- γ- Glutamic acid. After dissolution, keep it at 20 ℃ for 4h, and get L- γ- Methyl glutamate solution. The weight proportion of ingredients is L- γ- Glutamic acid: methanol: sulfuric acid=1:10:0.5.

 

2. Amination of L- γ- Methyl glutamate is liquid cooled to 0 ℃, methyl red is added as indicator, and ammonia is added to neutral. Add carbon trisulfide for dissolution, and continue to add ammonia to saturation. Place at 20 ℃ for 4d for filtration, and decompress the filtrate to remove ammonia. Add 4N acetic acid for neutralization. Heat preservation at 60 ℃ for 0.5h, decompress and remove carbon trisulfide. The residue was precipitated by adding twice methanol. Cooling, filtering and drying to obtain crude products. Add water to form 2% aqueous solution, and flow through weakly basic styrene anion exchange resin 303 × 2 (704), collect the effluent and concentrate under reduced pressure. Add methanol to precipitate, filter, wash repeatedly with methanol and ether, and dry to obtain L- γ- Glutamine.

 

3. Acetylation Add sodium hydroxide solution (1N) into the reaction tank, cool to 0 ℃, add glutamine with stirring, dissolve and stir for 1h. At the same time, add acetic anhydride and sodium hydroxide solution (2N), and place the solution at 0-5 ℃. Add 6N hydrochloric acid to pH1-2 and precipitate crystals. Cool, filter, wash with ice-cold non-ionic water until the chlorine meets the requirements, and dry to obtain acetylglutamine. The weight proportion of ingredients is L- γ- Glutamine: acetic anhydride (anhydrous)=1:1.1. Total yield 50% (vs. L- γ- Glutamic acid).

Aceglutamide-Chemical | Shaanxi BLOOM Tech Co., Ltd

Pharmacological mechanism of aceglutamide:

1. The mechanism of acetylglutamide in reducing blood ammonia

Acetoglutamide is distributed in various parts of the body with blood. Ammonia is decomposed in renal tubular cells and converted into acetylglutamic acid. Ammonia in blood is excreted from renal tubular cells.

2. Detoxification mechanism of acetylglutamine

Acetylglutamine is decomposed into glutamic acid and γ- Aminobutyric acid and glutamic acid participate in the information transmission of the central nervous system, γ- Aminobutyric acid can antagonize glutamate excitability. Acetic acid group and fluoroacetamide produce fluoroacetic acid to compete with acetyl coenzyme A, affecting the production of fluorocitrate, thus restoring the normal metabolism of the tricarboxylic acid cycle, playing the detoxification effect of acetamide (defluorin), improving the metabolism of nerve cells and improving brain function.

3. Mechanism of acetylglutamine in the treatment of cerebral embolism and motor dysfunction

It was found that aceglutamine can promote cell growth and can be used as a nutritional support in the recovery process of high-intensity training (racing, swimming, weightlifting, etc.). The protective effect of aceglutamine on motor functional nerves was studied through cerebral ischemia rat model, which can delay neuron death and improve motor dysfunction.

4. Anti-ischemic mechanism of acetylglutamine

Acetoglutamide can protect neurons in hippocampal CA1 area and substantia nigra area in the brain, improve the injury induced by cerebral ischemia and reperfusion, and achieve the effect of anti-cerebral ischemia.

5. Mechanism of Acetylglutamide in the Treatment of Nervous Insufficiency

Acetylcholine deficiency is the cause of the decline of nerve function. The concentration of neurotransmitter acetylcholine in the cerebral cortex and hippocampus of patients with nerve dysfunction is significantly reduced. In the process of nerve cell repair, acetylglutamine is the activator of nerve cells, and its decomposition products γ- Aminobutyric acid (GABA) can promote the synthesis of acetylcholine, improve brain function, increase the concentration of high-density lipoprotein, and accelerate the repair of brain tissue.

 

6. Mechanism of it in the treatment of inflammatory cytokines

The study found that TNF after craniocerebral injury- α, The excessive expression of inflammatory factors such as IL-1, IL-6 and IL-8 in the brain promotes the aggregation and activation of inflammatory cells and further aggravates the degree of brain injury. Acetylglutamine can significantly reduce the inflammatory response of patients with severe brain injury.

Stability and Safety

Aceglutamide indications | Shaanxi BLOOM Tech Co., Ltd

Main indications

 

Main indications: This product is mainly used to promote the recovery of comatose patients after neurosurgery surgery (such as brain tumors, traumatic brain injury, cerebrovascular disease, etc.), brain trauma, liver coma, hemiplegia, high paraplegia, neuroma, neuropathic headache, and lower back pain. Coma, memory and thinking disorders caused by various reasons such as intellectual disability, memory impairment, sequelae of infantile paralysis, and sequelae of mental disorders caused by drugs such as blood defense 846 (such as carbon monoxide poisoning, acute alcohol and drug poisoning, acute purulent meningitis, viral encephalitis, hepatic encephalopathy, pulmonary encephalopathy, electric shock injury, etc.).

 

Memory decline in the elderly and memory decline after cerebrovascular disease. Adjuvant treatment for elderly brain function decline includes chronic mental illness, geriatric psychiatric disorder syndrome, and depression. In psychiatric clinical practice, this product is often administered intravenously in combination with other drugs to improve cellular metabolism and nutritional status.

Aceglutamide memory | Shaanxi BLOOM Tech Co., Ltd
Aceglutamide epidemic | Shaanxi BLOOM Tech Co., Ltd

Epidemic of Japanese encephalitis

 

The literature report on epidemic encephalitis B observed the efficacy of the combination therapy of ribavirin and acetanilide in the treatment of encephalitis B. The cases were divided into two groups, and the two groups were basically the same in terms of gender, age, clinical type, and start date of treatment, which were comparable. Both groups received comprehensive treatment such as cooling, expectorant, sedation, dehydration, reducing intracranial pressure, fluid replacement, and infection prevention. In addition to comprehensive treatment, the treatment group received ribavirin injection at a dose of 15mg/kg per day and acetanilide at a dose of 0.02g/kg per day.

 

Both drugs were added to 10% glucose solution for intravenous infusion until the 10th day of illness, with an average duration of 5.7 days. The efficacy evaluation criteria are: cure: disappearance of symptoms and signs, no recovery period symptoms; effective: symptoms. And the physical signs have improved, with varying degrees of recovery symptoms remaining. The treatment group had a shorter time in terms of fever reduction, consciousness recovery, seizure cessation, and disappearance of cervical resistance compared to the control group. The incidence of central respiratory failure was 17.9% in the treatment group and 43.3% in the control group, with a significant difference between the two groups (x2=4.39, p<0.05).

Aceglutamide solution | Shaanxi BLOOM Tech Co., Ltd
Aceglutamide drug | Shaanxi BLOOM Tech Co., Ltd

 

The incidence of respiratory failure in the treatment group was significantly lower than that in the control group. In the treatment group, 20 cases were cured with a cure rate of 71.4%, 6 cases were effective, 2 cases were ineffective, and the total effective rate was 92.8%; In the control group, 13 cases were cured with a cure rate of 43.3%, 11 cases were effective, 6 cases were ineffective, and the total effective rate was 80%. There was a significant difference in the cure rate between the two groups (x2=4.66, p<0.05), while there was no significant difference in the total effective rate between the two groups (x2=1.08, p>0.05).

 

The early combined use of virazole and acetylglutamine in the treatment of Japanese encephalitis can control the worsening of the condition, improve brain function, promote fever reduction, clear consciousness, reduce the incidence and mortality of central respiratory failure, and increase the cure rate. The combination of two drugs has not yet shown significant aceglutamide side effects and can be used as one of the treatment methods for Japanese encephalitis.

Aceglutamide treatment | Shaanxi BLOOM Tech Co., Ltd
Aceglutamide clinical | Shaanxi BLOOM Tech Co., Ltd

Fluoride rescue

 

In the clinical efficacy report of using acetylglutamine to rescue 30 cases of fluoride poisoning, a 1:5000 potassium permanganate solution was routinely used for gastric lavage, and acetylglutamine was immediately administered at a rate of 0.1-0.3/day, divided into 1-2 intravenous drops, for a total of 7 days or stopped after the child became conscious and the convulsions stopped. Simultaneously use dexamethasone, a large amount of vitamin C, phosphatidylcholine or brain active hormone, and energy mixture to protect organ function. Among all cases, 20 were cured, 8 were effective, and 2 had sequelae, manifested as spasticity and cerebral palsy with intellectual disability.

 

Those who died or survived with severe sequelae were children who had ingested large amounts of medication, young children, and those who were unable to use acetylglutamine immediately. The mechanism of action for treating fluoride poisoning is because acetylglutamine has a similar structure to this type of toxin. Acetylglutamine produces amide genes in the body or competition with fluoroacetic acid produced by sodium fluoroacetate to achieve detoxification. At the same time, it has the effects of improving neuronal metabolism, maintaining neural stress function, etc., thus reducing the occurrence of neurological sequelae.

Aceglutamide medication| Shaanxi BLOOM Tech Co., Ltd
Aceglutamide treatment | Shaanxi BLOOM Tech Co., Ltd

 

The successful treatment of two cases of fluoroacetamide poisoning with acetylglutamine demonstrates that the treatment of fluoroacetamide poisoning with acetylglutamine involves the addition of an acetamide group (- CH2CONH2) in the chemical structure of acetylglutamine, which is similar to the chemical structure of acetamide. Clinical application has confirmed definite therapeutic effects. Due to the fact that most primary hospitals do not have acetamide drugs, when encountering fluoroacetamide poisoning, acetyl glutamine can be used as a substitute for treatment.

Cerebrovascular disease

 

Brain hypoplasia was treated with scalp acupuncture combined with acupoint injection for cerebrovascular disease complicated with intellectual disability. Method: 74 patients were randomly divided into two groups. The treatment group consisted of 40 cases, who were treated with scalp acupuncture for the Zhisan needle and the Sishen needle, and were also injected with acetylglutamine and furosemide at acupoints such as Baihui. 34 cases in the control group were treated with intravenous infusion of 20mL of Naohuo Su and 0.9% sodium chloride injection, and the therapeutic effects of the two groups were compared and observed.

Aceglutamide disease | Shaanxi BLOOM Tech Co., Ltd
Aceglutamide effect | Shaanxi BLOOM Tech Co., Ltd

 

The effective rate in the treatment group was 95.0%, while the total effective rate in the control group was 85.3%. There was a significant difference between the two groups (p<0.05). Conclusion: The combination of scalp acupuncture and acupoint injection therapy has the effects of awakening the brain and opening the orifices, strengthening the brain and marrow, improving brain cell vitality, and enhancing brain function. It has a definite therapeutic effect on treating cerebrovascular disease complicated with intellectual disability. 50 cases of cerebral hypoplasia were treated with head acupoint injection of acetylglutamine and furothiamine, with good therapeutic effects.

 

Initially, scalp acupuncture was used to treat sequelae of brain disease, and later alternating treatment with scalp acupuncture and water acupuncture (acetylglutamine and furothiamine) was tried, and it was found that the latter had better therapeutic effects than the former. Immediately switched to using water needles instead of scalp needles to treat this disease, resulting in improved efficacy compared to before. From the analysis of the relationship between treatment outcomes and age, the younger the age, the better the therapeutic effect. Therefore, aceglutamide is believed that early treatment is appropriate for cerebral hypoplasia. Acetylglutamide and furosemide head acupoint injection therapy for cerebral hypoplasia showed a significant effect of 74%, an effective rate of 14%, and a total effective rate of 88%.

Aceglutamide drug | Shaanxi BLOOM Tech Co., Ltd
FAQ
 

What is acetyl glutamine?

Chemically speaking, acetyl glutamine is the amide formed from the reaction of acetic acid chloride and glutamine. Glutamine is the most abundant amino acid in the body (as a skin care ingredient, this can be produced synthetically).

What is glutamic acid used for?

Glutamic acid is an alpha-amino acid used in protein biosynthesis by nearly all living beings. Glutamic acid is also an excitatory neurotransmitter in the vertebrate nervous system. It is used in protein biosynthesis in the human body and helps in metabolism, brain, and cardiac function.

Is glutamine good for the brain?

Glutamine supports the production of GABA, the neurotransmitter that acts as the brain's natural "brake pedal." By calming the nervous system and reducing excessive neural stimulation, glutamine helps prepare your brain for deeper, more restful sleep.

Who should not take L-glutamine?

Liver disease: Glutamine can increase the risk for brain function issues in people with advanced liver disease. Do not use it if you have liver disease. Bipolar disorder: Glutamine might increase the risk for mania or hypomania in people with this condition.

 

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