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Eledoisin, usually a white or almost white solid powder, odorless. It is a bioactive peptide belonging to the glucagon like peptide family. Composed of 39 amino acids, with a relative molecular weight of approximately 4414.97. Its primary structure is His Gly Gly Gln Gly Thr Gly Gly Leu Met-NH2. Easy to dissolve in water, as well as in organic solvents such as methanol, ethanol, DMSO, etc. It has certain stability to acids, bases, and heat, but hydrolysis may occur under strong acid or base conditions. It has optical rotation and can be controlled by adjusting the pH value of the solution. It has an absorption spectrum in the UV visible region and can be used for content determination and qualitative analysis. It can emit fluorescence and can be used for fluorescence analysis for detection. As a low calorie sweetener, it has a wide range of applications in the food industry. It can provide sweetness for various foods and beverages, while also having the characteristics of low calories, not causing elevated blood sugar, and not increasing calorie intake. It has been widely used in beverages, candies, baked goods, food seasonings, frozen desserts, sauces, health foods, food preservation, and oral care products.
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Customized Bottle Caps And Corks:
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Chemical Formula |
C54H85N13O15S |
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Exact Mass |
1188 |
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Molecular Weight |
1188 |
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m/z |
1188 (100.0%), 1189 (58.4%), 1190 (16.7%), 1189 (4.8%), 1190 (4.5%), 1190 (3.1%), 1190 (2.8%), 1191 (2.6%), 1191 (2.3%), 1191 (1.8%) |
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Elemental Analysis |
C, 54.58; H, 7.21; N, 15.32; O, 20.19; S, 2.70 |
Eledoisin is a bioactive peptide, and its chemical synthesis methods are relatively complex. The following will provide a detailed introduction to a common synthesis method and its related chemical equations:
(Equation 1) C5H9NO4+H2O4S → γ- Glutamoyl propanediamine hydrochloride
(Equation 2) γ- Glutamoyl propanediamine hydrochloride+C14H10O3 → parent compound of tilurutide
(Formula 3) Tetraglutide parent compound+H4N2 → Tetraglutide cysteine derivative
(Formula 4) Tyrolutide cysteine derivative+HCl → Tyrolutide thioamino acid derivative
(Equation 5) After mixing the above four products, separate and purify them → high-purity Elidoxin product
Starting materials: L-glutamic acid, malondiamine hydrochloride, benzoic anhydride, etc.
Step 1: γ- Synthesis of Glutamoyl Propanediamine Hydrochloride
Add L-glutamic acid and concentrated sulfuric acid as catalysts to the reaction bottle, heat and reflux until γ- The formation of glutamylpropylenediamine hydrochloride. After the reaction is completed, cool to room temperature and filter to obtain intermediate products γ- Glutamoyl propanediamine hydrochloride (formula 1).
Step 2: Synthesis of the parent compound of Tidullutide
Generate intermediate products γ- Mix glutamylpropylenediamine hydrochloride with benzoic anhydride, add triethylamine as a catalyst, heat and reflux to generate the parent compound of tiluride. After the reaction is completed, cool to room temperature and filter to obtain the parent compound of tilurutide (formula 2).
Step 3: Synthesis of Cysteine Derivatives of Tidullutide
Mix the generated prodrug parent compound with hydrazine hydrate, add triethylamine as a catalyst, heat and reflux to generate prodrug cysteine derivatives. After the reaction is completed, cool to room temperature and filter to obtain a derivative of tilurutide cysteine (formula 3).
Step 4: Synthesis of Thioamino Acid Derivatives of Tidullutide
Mix the generated tilurutide cysteine derivatives with hydrogen chloride gas, heat and reflux to generate tilurutide thioamino acid derivatives. After the reaction is completed, cool to room temperature and filter to obtain the thioamino acid derivative of Tidulutide (Formula 4).
Step 5: Synthesis of Eledoisin
Mix the above four products in a certain proportion and separate and purify them to obtain high-purity Elidoxin products. This step requires strict control of conditions such as temperature, pH value, reaction time, etc. to ensure the purity and yield of the product. The specific operation process is as follows: first, dissolve the above four products in an appropriate amount of water, and then add organic solvents (such as methanol or ethanol) for extraction and separation; Then, column chromatography was used for purification treatment; Finally, content determination and quality analysis were carried out using a high-performance liquid chromatograph.
The chemical synthesis method of Elidoxin mainly includes four steps: the first step is γ- Synthesis of glutamylpropylenediamine hydrochloride; The second step is the synthesis of the parent compound of dideluptin; The third step is the synthesis of cysteine derivatives of Tidulutide; The fourth step is the synthesis of Elidoxin. These steps require strict control of conditions to ensure the purity and yield of the product. At the same time, attention should be paid to safety issues to ensure the safety of experimental personnel.
Eledoisin, also known as Eledone peptide, is a peptide compound with specific biological activity that plays an important role in scientific research, particularly in pharmacology and neurobiology. As a specific agonist of NK2 and NK3 receptors, Elidoxine provides scientists with a powerful tool for exploring and understanding the functions and mechanisms of these receptors in vivo.
Application in Pharmacological Research
(1) Research on receptor function
As a specific agonist of NK2 and NK3 receptors, Elidoxine can directly bind to these receptors, activating them and triggering corresponding biological effects. This makes Elidoxine an important tool for studying the function of NK2 and NK3 receptors. By observing the stimulating effect of elidoxine on receptors, scientists can gain a deeper understanding of the mechanisms by which these receptors function in neural transmission, cellular signal transduction, and other areas.
(2) Drug screening and evaluation
In the process of drug development, Elidoxine can be used to screen and evaluate drug targets related to NK2 and NK3 receptors. Through competitive binding experiments with Elidoxine, scientists can determine which compounds can inhibit or enhance the activity of NK2 and NK3 receptors, thereby screening drug candidates with potential therapeutic effects.
(3) Research on Disease Mechanisms
NK2 and NK3 receptors play important roles in the occurrence and development of various diseases, such as inflammation, pain, neurodegenerative diseases, etc. Elidoxine, as an agonist of these receptors, can be used to study the mechanisms of these diseases. By observing the biological effects of Elidoxine in disease models, scientists can reveal the roles of NK2 and NK3 receptors in the disease process and provide theoretical basis for developing new treatment methods.
Application in Neurobiology Research
(1) Research on Neuroregulatory Mechanisms
Elidoxine has a wide distribution and function in the nervous system, as it can affect the excitability and inhibition of neurons, thereby regulating neural transmission processes. By studying the effects of Elidoxine on neurons, scientists can gain a deeper understanding of the neural regulatory mechanisms, providing new perspectives and ideas for research in the field of neurobiology.
(2) Research on neurodegenerative diseases
Neurodegenerative diseases are a type of disease characterized by the gradual loss of neuronal structure and function, such as Alzheimer's disease, Parkinson's disease, etc. NK2 and NK3 receptors play important roles in the pathogenesis of neurodegenerative diseases. Elidoxine, as an agonist of these receptors, can be used to study the mechanisms of these diseases and explore new treatment methods.
(3) Research on Pain Mechanisms
Pain is a complex physiological and psychological phenomenon involving the interaction of multiple neurotransmitters and receptors. NK2 and NK3 receptors play important roles in pain transmission and modulation. As an agonist of these receptors, Elidoxine can be used to study pain mechanisms and provide theoretical basis for the development of new analgesic drugs.
Specific research examples
(1) The impact on the cardiovascular system
A study has shown that injection of esomeprazole (0.1-1 nmol/kg) into rats can produce biphasic cardiovascular responses, including an initial decrease in systemic blood pressure (8-15 mm Hg) followed by an increase (20-22 mm Hg). This discovery reveals the complex mechanism of action of Elidoxine in the cardiovascular system, providing new clues for the study of cardiovascular diseases.
(2) The impact on mouse behavior
Another study showed that injection of eredoxine into the lateral ventricle can enhance grooming and scratching behavior in mice. This discovery suggests that elidoxine may regulate mouse behavior by affecting the central nervous system. This provides a new perspective for research in the fields of neurobiology and behavior.
(3) Application in pain models
In pain models, it is used as a tool molecule to study pain mechanisms. By observing the effects of elidoxine on pain transmission and modulation, scientists can gain a deeper understanding of the mechanism of pain and provide theoretical basis for the development of new analgesic drugs.
(4) Application in neurodegenerative disease models
In neurodegenerative disease models, it is used to study the role of NK2 and NK3 receptors in the disease process. By observing the effects of elidoxine on neuronal structure and function, scientists can reveal the mechanisms of action of these receptors in the pathogenesis of neurodegenerative diseases and provide theoretical basis for the development of new treatment methods.
Elidoxine, as a peptide compound with specific biological activity, plays an important role in the field of scientific research. As a specific agonist of NK2 and NK3 receptors, it provides scientists with a powerful tool for exploring and understanding the functions and mechanisms of action of these receptors in vivo. In the future, with the deepening of research and the continuous development of technology, Elidoxine is expected to demonstrate its potential application value in more fields. However, before applying it to new fields, sufficient research and validation are needed to ensure its safety and effectiveness. At the same time, scientists also need to continue exploring more mechanisms of action and potential uses of elidoxine, providing more clues and ideas for research in related fields.
Adverse reactions
Eledoisin is a ten peptide compound extracted from marine mollusks, with the chemical formula C ₅₄ H ₈₅ N ₁∝ O ₁₅ S and a molecular weight of 1188.4. As a member of the tachykinin family, it exerts biological effects by activating NK1, NK2, and NK3 receptors, including vasodilation, neuronal excitation, and regulation of cardiovascular responses. Although it has shown potential application value in the fields of cardiovascular disease, neurodegenerative diseases, and skincare products, the complexity of its adverse reactions limits its clinical promotion.
Types of adverse reactions
Cardiovascular system response
Eledoisin produces contradictory effects by activating NK1 receptors (which dominate hypotension) and NK2 receptors (which dominate pressor). The clinical manifestation is in the initial stage: vasodilation leads to a brief decrease in blood pressure, accompanied by facial flushing and headache. Delay stage: Overactivation of NK2 receptors triggers a rebound increase in blood pressure, which may induce arrhythmia. Activation of NK1 receptors promotes histamine release, leading to capillary leakage. Hypoproteinemia patients may worsen edema. Combination use of anticoagulants increases the risk of bleeding. It is recommended to monitor plasma albumin levels and avoid co administration with warfarin and other medications.
Neurological response
Mild: Anxiety, insomnia, tremors (with an incidence rate of about 15%).
Severe: Seizures (rare, only seen at doses>5 mg/kg).
Mechanism: Eledoisin enhances glutamatergic neurotransmission through NK3 receptors. After intraventricular injection in mice, the frequency of grooming behavior increased by 300%, indicating a potential risk for obsessive-compulsive disorder spectrum disorder.
Skin reactions
Type I: Urticaria and angioedema (with an incidence rate of approximately 2% -5%).
Type IV: Contact dermatitis (delayed response, appearing within 48-72 hours). Individuals with a history of allergies to marine organisms have a 10 fold increased risk. Repeated use of skincare products may cause sensitization. Transient erythema (incidence about 20%). Burning sensation (lasting 15-30 minutes). It is recommended to use it locally during initial use, observe for 24 hours without any reaction, and then expand the area.
Digestive system response
Nausea (incidence about 8%).
Diarrhea (rare, only seen in high-dose treatment).
Mechanism: NK1 receptor activation stimulates the vomiting center, while NK2 receptor promotes gastrointestinal peristalsis.
Case: A patient with cardiovascular disease developed watery diarrhea after taking Eledoisin analog orally, which was relieved after adjusting the dosage.
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