Opiorphin tablet is a peptide composed of three amino acids with neuroprotective properties. Molecular formula C29H48N12O8, CAS 864084-88-8, can prevent the accumulation of reactive oxygen species (ROS) and inhibit the activation of ERK 1/2. It can stimulate the functional activity of the main cellular components of brain tissue and reduce spontaneous cell death. Protect offspring of rats from prenatal hyperhomocysteinemia. This content is for scientific research purposes only. Do not use directly on the human body!
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Opiorphin COA
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| Certificate of Analysis | ||
| Compound name | Opiorphin | |
| Grade | Pharmaceutical grade | |
| CAS No. | 864084-88-8 | |
| Quantity | 60g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090088 | |
| 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: | C29H48N12O8 |
| Exact Mass: | 692 |
| Molecular Weight: | 693 |
| m/z: | 692 (100.0%), 693 (31.4%), 694 (4.7%), 693 (4.4%), 694 (1.6%), 694 (1.4%) |
| Elemental Analysis: | C, 50.28; H, 6.98; N, 24.26; O, 18.48 |
Opiorphin tablet is a peptide substance with powerful analgesic effects first discovered in human saliva, and its unique chemical structure and mechanism of action have brought new hope to the field of pain management.
Inhibition of enkephalin degrading enzyme
1. The function and degradation of enkephalin
Enkephalin is an endogenous opioid peptide that can bind to opioid receptors in the body and produce analgesic effects. However, under normal circumstances, enkephalins are rapidly degraded by two enkephalin degrading enzymes - human neutral endopeptidase (hNEP, enzyme code EC 3.4.24.11) and human exogenous aminopeptidase (hAP-N, enzyme code EC 3.4.11.2), resulting in a short duration of action. This degradation process limits the sustained analgesic effect of enkephalin in the body.
2. Inhibition effect
As a potent inhibitor of human enkephalin inactivating zinc heteropeptidase, it can bind to hNEP and hAP-N, inhibiting their degradation of enkephalin. Specifically, by occupying the active sites of these enzymes, they are prevented from binding to enkephalin, thereby protecting enkephalin from degradation. This mechanism maintains a high concentration of enkephalin in the body, continuously activating endogenous opioid dependent transmission and ultimately producing analgesic effects.
3. Experimental evidence
A large number of in vitro experiments have confirmed the inhibitory effect of Opiorphin on hNEP and hAP-N. For example, in ex vivo colon experiments in mice, Opiorphin (1-100 μ M) can induce distal colon contraction in mice in a concentration dependent manner and enhance the contraction response induced by methionine enkephalin. This indicates that it can protect enkephalin from degradation, thereby enhancing its physiological function. In addition, inhibition of the enzymatic hydrolysis of recombinant hNEP on the cell surface within Mca-BK2 resulted in an IC50 value of 33 μ M, and inhibition of Ala pNA cleavage of hAP-N resulted in an IC50 value of 65 μ M, further demonstrating its inhibitory effect on these two enzymes.
Information sources: Sohu, CSDN Blog, Chemical Instrument Network
Activate endogenous opioid dependent transmission
1. Activation of endogenous opioid system
By inhibiting enkephalin degrading enzymes, endogenous enkephalins are protected from degradation, thereby activating endogenous opioid dependent transmission. The endogenous opioid system includes endogenous opioid peptides such as enkephalin and dynorphin, as well as opioid receptors such as μ, δ, and κ. It does not directly act on opioid receptors, but indirectly activates opioid receptors by increasing the concentration of enkephalin, producing analgesic effects.
2. Experimental verification of analgesic effect
Animal experiments have shown significant analgesic effects. In mouse experiments, injecting different doses of Opiorphin (1.25-10 μ g/kg) into the ventricles can induce strong analgesic effects in a dose - and time-dependent manner.
At 10 minutes after injection, there was a significant change in the percentage of tail flick latency (TWL) in different dose groups, with 28.90% in the 1.25 mg/kg group and as high as 91.89% in the 10 mg/kg group. This indicates that opiorphin tablet has great potential in relieving pain.
3. Comparison with traditional opioid analgesics
Compared with traditional opioid analgesics such as morphine, it has lower addiction risk and tolerance. This is because it produces analgesic effects by protecting endogenous enkephalins, rather than directly activating opioid receptors. Therefore, it reduces the likelihood of addiction and dependence, providing new options for pain management.
Information sources: Sohu, Baijiahao, Chemical Instrument Network
Regulating effect of cardiovascular system
1. Experimental observation of cardiovascular reactions
In addition to its analgesic effect, it also has a certain impact on the cardiovascular system. Experiments have found that intravenous injection can dose dependently cause a rapid increase in mean arterial pressure and heart rate in Uratan anesthetized rats. This cardiovascular response may be related to the upregulation of endogenous circulating angiotensin levels, in which the sympathetic nervous system is also involved.
3. The opioid system is not involved in cardiovascular reactions
It is worth noting that the opioid system did not participate in the cardiovascular response caused. The experiment found that the non selective opioid receptor antagonist naloxone had no significant effect on the cardiovascular effects caused. This indicates that the mechanism of action in the cardiovascular system is different from its analgesic effect.
2. Exploration of the mechanism of cardiovascular response
Further research has shown that the induced cardiovascular reactions can be significantly antagonized by the angiotensin-converting enzyme inhibitor Captopril and the angiotensin II type 1 receptor antagonist Valsartan. This indicates that the renin-angiotensin system (RAS) is involved in the cardiovascular effects of this substance. In addition, intravenous pre injection of alpha adrenergic receptor antagonist phentolamine and beta adrenergic receptor antagonist propranolol can also inhibit the increase in mean arterial pressure caused by them. However, propranolol can significantly inhibit the tachycardia response it causes, while phentolamine cannot. This suggests that its cardiovascular effects may involve multiple mechanisms, including activation of RAS and regulation of the sympathetic nervous system.
Information source: Docin.com Douding.com, none (top 30 relevant literature in China Journal Full text Database)
Antidepressant effect
1.Experimental findings on antidepressant effects
In addition to its analgesic and cardiovascular regulatory effects, it also has antidepressant properties. In the forced swimming experiment of mice, injection of Opiorphin (50, 100, 200, and 300 μ g/kg) into the lateral ventricle dose dependently shortened the cumulative immobility time of mice, indicating that Opiorphin has antidepressant properties.
3. Impact on independent activities
In order to exclude the possibility that its antidepressant effect in the forced swimming experiment was caused by nerve excitation, the experiment also examined its impact on the autonomous activity of mice. The results showed no effect on the autonomous activity of mice that did not adapt in advance, but slightly enhanced the autonomous activity ability of mice that adapted in advance. This indicates that its antidepressant effect is not achieved through excitatory nerves.
2. Exploration of the mechanism of antidepressant effect
Further research suggests that its antidepressant effect is mediated through the opioid pathway of enkephalin. The non selective opioid receptor antagonist naloxone, when administered in combination, can completely counteract the antidepressant effect of this substance. Given that enkephalin has two receptors, μ - and δ -, further experiments will use μ - and δ - opioid receptor selective antagonists β - DNA and naltrindole in combination to investigate specific receptor types. The results showed that the δ receptor antagonist naltrindle could completely counteract its antidepressant effect, while the μ receptor antagonist β - RNA partially inhibited this effect. This indicates that it increases the extracellular concentration of enkephalin by inhibiting its degradation, indirectly activating μ and δ opioid receptors to exert antidepressant effects.
Information source: Wanfang Data Knowledge Service Platform, none (top 30 relevant literature in China Journal Full text Database)
Other potential effects
1. Impact on intestinal related pain
In addition to the aforementioned effects, it has also found a place in research on gut related pain. Research has shown that it can enhance the intestinal response to methionine enkephalin, which may provide a new approach for treating pain caused by diseases such as irritable bowel syndrome. In the ex vivo colon experiment of mice, opiorphin tablet (1-100 μ M) can induce distal colon contraction in mice in a concentration dependent manner and enhance the contraction response induced by methionine enkephalin.
2. Impact on the immune system
Although there is currently limited research on the impact on the immune system, other components in saliva such as lysozyme and mucin have the ability to clean wounds and inhibit bacteria. This indicates that the components in saliva play an important role in immune defense. Future research can further explore whether it is also involved in immune regulation processes.
Information sources: Sohu, Weibo
FAQ
Is opiorphin stronger than morphine?
In cooperation with the ETAP team from the Nancy-Brabois Technopole, the Institut Pasteur scientists demonstrated in vivo that, for the same doses, Opiorphin produces a comparable analgesic potency as morphine, in both thermal and mechanical acute pain and in chemical-induced tonic pain.
Can you extract opiorphin from saliva?
The HFBA-based SUPRAS is, therefore, capable of efficiently extracting opiorphin from saliva samples and shows a high potential for the determination of several amino acids and oligopeptides from biological samples.
What is the strongest human painkiller?
It is the strongest opioid available in medical settings, being 50 to 100 times more potent than morphine. Carfentanyl, a fentanyl analog is considered the most potent opioid, roughly 10,000 times stronger than morphine. Due to its extreme potency, carfentanil is rarely used in human medical treatment.
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