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Methionine-Enkephalin(Met enkephalin), as an endogenous pentapeptide opioid substance, is widely distributed in central and peripheral tissues. Its physiological efficacy is mainly achieved through three dimensions: specific receptor binding, neurotransmitter regulation, and maintenance of gastrointestinal function homeostasis. The three work together to participate in precise regulation of multiple basic physiological activities in the body, and each dimension has a unique mechanism of action and characterization. The following provides a detailed analysis from the designated core points.
Products Overview
Methionine-Enkephalin COA
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| Certificate of Analysis | ||
| Compound name | Met-Enkephalin | |
| Grade | Pharmaceutical grade | |
| CAS No. | 58569-55-4 | |
| Quantity | 33g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202501090061 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.54% |
| Loss on drying | ≤1.0% | 0.42% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.98% |
| Single impurity | <0.8% | 0.52% |
| Total microbial count | ≤750cfu/g | 95 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 500ppm |
| Storage | Store in a sealed, dark, and dry place below -20°C | |
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| Chemical Formula | C27H35N5O7S | |
| Exact Mass | 573.23 | |
| Molecular Weight | 573.67 | |
| m/z | 573.23 (100.0%), 574.23 (29.2%), 575.22 (4.5%), 575.23 (4.1%), 574.22 (1.8%), 575.23 (1.4%), 576.22 (1.3%) | |
| Elemental Analysis | C, 56.53; H, 6.15; N, 12.21; O, 19.52; S, 5.59 | |
Receptor binding characteristics and mediating effects
The physiological activation of Methionine-Enkephalin relies on precise binding to specific receptors on the surface of target cells. There is a significant gradient in its affinity for different receptors, and the physiological effects mediated by Met Enkephalin also exhibit differentiated characteristics, specifically manifested as:
The main mediator of delta opioid receptor activation is Met Enkephalin, which serves as an advantageous binding target and is widely distributed in the limbic system, spinal dorsal horn, and peripheral nerve endings of the central nervous system. The combination of the two can trigger a cascade reaction of the G protein coupled signaling pathway, inhibit adenylate cyclase activity, reduce cyclic adenosine monophosphate (cAMP) production, and block the transmission of nerve impulses. This process is the basis for the subsequent activation of multiple physiological effects, and the specificity of receptor binding is high, making it less likely to cross interfere with other endogenous opioid peptides.
Weakly activated μ - opioid receptors are mainly concentrated in the central pain transmission pathway and gastrointestinal mucosa. The binding affinity of Met Enkephalin to this receptor is significantly lower than that of δ - opioid receptors, and the signal intensity mediated by binding is weaker. Its core function is to assist in enhancing the effect mediated by δ - opioid receptors, while slightly regulating the release rhythm of neurotransmitters, avoiding physiological dysfunction caused by single receptor activation, and forming a synergistic regulatory network with δ - opioid receptors.
Specifically acting on the Zeta receptor (i.e. opioid growth factor receptor, OGFR), this receptor has a significant difference in molecular structure from classical opioid receptors and is mainly distributed in mucosal epithelial cells and nerve endings. After binding to this receptor, Met Enkephalin does not rely on the signaling pathway of classical opioid receptors, but regulates the expression of intracellular signaling molecules through nuclear cytoplasmic transport mechanisms. Its core function is to participate in the maintenance of target organ function homeostasis, complement the effects mediated by the first two receptors, and improve the physiological regulatory system of Met Enkephalin.
The data basis of the above content are:
hea-Donohue T, Donohue J P. Effects of Met-enkephalin and naloxone on gastric emptying and secretion in rhesus monkeys[J]. American Journal of Physiology-Gastrointestinal and Liver Physiology, 1983, 244(4): G396-G402.
Zhang Keying, Du Jian, Dan Fengping New progress in the immunomodulatory effects and applications of methionine enkephalin [J]. Chinese Journal of Immunology, 2017, 33 (5): 788-792
Neurotransmitter regulation and emotional homeostasis maintenance
Methionine-Enkephalin participates in the regulation of emotional states in the body by precisely regulating the metabolic processes of two key neurotransmitters, dopamine (DA) and serotonin (5-HT). Its mechanism of action has multidimensional and refined characteristics, as follows:
The primary effect is the bidirectional regulation of dopamine. Met Enkephalin can inhibit the excessive discharge of central dopaminergic neurons and reduce the excessive release of dopamine through the mediation of delta opioid receptors. At the same time, it can promote the expression of dopamine transporters, accelerate the reuptake of dopamine in synaptic cleft, and avoid emotional excitement caused by dopamine accumulation; On the other hand, when dopamine secretion is insufficient
It can weakly activate μ - opioid receptors, slightly promote the activity of dopaminergic neurons, supplement dopamine secretion, maintain the dynamic balance of dopamine levels, and thereby mediate the generation and maintenance of pleasure.Secondly, Met Enkephalin regulates the synthesis and release of 5-hydroxytryptamine. By regulating the activity of tryptophan hydroxylase, Met Enkephalin promotes the synthesis of 5-hydroxytryptamine while inhibiting the activity of 5-hydroxytryptamine decarboxylase.
Reducing the degradation of 5-hydroxytryptamine and thereby increasing the concentration of 5-hydroxytryptamine in the synaptic cleft; In addition, it can also regulate the sensitivity of serotonin receptors, enhance the binding efficiency between serotonin and receptors, thereby exerting sedative and anti anxiety effects, and relieving emotional tension and irritability.
The data basis of the above content are:
Xia Yanjie, Sun Liqun, Li Ronghui, etc Study on the effects of methionine enkephalin alone or in combination with IL-2 and IFN - γ on CD4+T cells in mice [J]. Microbiology Journal, 2013, 33 (2): 34-38
Konturek S J, Brzozowski T, Konturek P C. Role of endogenous opioids in the regulation of gastrointestinal function[J]. Journal of Physiology and Pharmacology, 2004, 55(4): 7-24.
Gastrointestinal function regulation and related symptom relief
Met Enkephalin, as an important regulatory factor of gastrointestinal function, achieves relief of abdominal pain and diarrhea symptoms by regulating gastrointestinal motility rhythm and gastric acid secretion efficiency. Its mechanism of action is closely related to receptor binding and local neural regulation. The specific analysis is as follows:
Fine tuned regulation of gastrointestinal peristalsis.
Met Enkephalin mainly acts on the enteric nerve plexus within the gastrointestinal tract wall, binding to δ - opioid receptors and μ - opioid receptors, inhibiting excessive contraction of gastrointestinal smooth muscle, slowing down the frequency and amplitude of gastrointestinal peristalsis, prolonging the residence time of food in the gastrointestinal tract, and promoting the digestion and absorption of nutrients; At the same time, it can regulate the coordination of gastrointestinal peristalsis, avoid smooth muscle spasms, reduce the causes of abdominal pain caused by gastrointestinal motility disorders, and especially have a significant inhibitory effect on intestinal peristalsis hyperactivity.
Accurate regulation of gastric acid secretion.
Methionine-Enkephalin inhibits the secretion of gastrin by acting on receptors on the surface of gastric wall cells, thereby reducing the synthesis and release of gastric acid. At the same time, it promotes the secretion of mucus on the surface of the gastric mucosa, enhances the barrier function of the gastric mucosa, reduces the stimulation of gastric acid on the gastric mucosa, and avoids gastrointestinal discomfort caused by excessive gastric acid; In addition, it can also regulate the rhythm of gastric acid secretion, matching it with the eating process and maintaining the acid-base balance in the gastrointestinal tract.
The soothing mechanism of abdominal pain and diarrhea symptoms.
For abdominal pain, Met Enkephalin reduces pain perception by inhibiting smooth muscle spasms in the gastrointestinal tract, blocking the transmission of harmful signals in the gastrointestinal tract, and regulating the sensitivity of gastrointestinal nerves to lower pain thresholds and alleviate pain symptoms; For diarrhea, it can alleviate symptoms by inhibiting excessive gastrointestinal peristalsis, reducing the secretion of intestinal fluids, enhancing the absorption function of intestinal mucosa, and reducing the water content in feces. Moreover, this soothing effect is mild and does not lead to excessive inhibition of gastrointestinal function.
The data basis of the above content is:
Liu Jinling, Dan Fengping The effect of methionine enkephalin on the expression of TLR-4 and TNF - α in GM-CSF induced mouse bone marrow-derived dendritic cells [J]. Journal of Northeast Agricultural University, 2013, 44 (3): 102-106
References
Garcia-Dominguez M. Enkephalins and Pain Modulation: Mechanisms of Action and Therapeutic Perspectives[J]. Biomolecules, 2024, 14(8): 926.
Holzer P. Opioid receptors in the gastrointestinal tract[J]. Regulatory Peptides, 2009, 155(1-3): 17-27.
Li Yanbo, Liu Feifei, Qu Hengyan Study on the growth inhibition and apoptosis effects of methionine enkephalin combined with doxorubicin on neuroblastoma SH-SY5Y [J]. Chinese Journal of Drug Application and Monitoring, 2015, 12 (5): 273-276
Waldhoer M, Bartlett S E, Whistler J L. Opioid Receptor Function: New Insights from Knockout Mice[J]. Annual Review of Pharmacology and Toxicology, 2004, 44: 399-423.
FAQ
Methionine enkephalin (MENK), an endogenous neuropeptide has a crucial role in both neuroendocrine and immune systems. MENK is believed to have an immunoregulatory activity to have cancer biotherapy activity by binding to the opioid receptors on immune and cancer cells.
ACTH4–10 and Met-enkephalin share a phenylalanine and a methionine residue. The possibility was studied that these amino acid residues are a structural requirement for this effect.
Chemistry. Met-enkephalin is a pentapeptide with the amino acid sequence Tyr-Gly-Gly-Phe-Met. The tyrosine residue at position 1 is thought to be analogous to the 3-hydroxyl group on morphine.
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