Mitragynine Pseudoindoxyl is a compound derived from the alkaloid Mitragynine that is making its presence known due to its several beneficial properties. In this article, we will be discussing everything related to this alkaloid derivative –including its pharmacology, mechanism of action, health benefits, potential risks, and much more.
Let’s dig in!
What Is Mitragynine Pseudoindoxyl?
Mitragynine Pseudoindoxyl is a semi-synthetic derivative of Mitragynine. Mitragynine is one of the main and most abundantly found alkaloids in the Kratom plant. Historically, it was first isolated by a scientist named Zarembo as a microbial metabolite of Mitragynine by a type of fungus.
Although this derivative compound is usually synthetically manufactured by chemically modifying Mitragynine, it can also be produced naturally in the blood as a metabolite of 7-HydroxyMitragynine – another commonly found alkaloid in Kratom plants.
It has recently started garnering huge attention due to its strong properties of resolving discomfort, while avoiding most of the adverse effects related with usage of the other pharmacological alternatives.
What’s The Science Behind Mitragynine Pseudoindoxyl?
Mitragynine Pseudoindoxyl is a rearranged chemical product of Mitragynine, where the indole ring undergoes oxidation causing the formation of spiro- pseudoindoxyl core in the end product.
This altered chemistry gives it a unique pharmacological profile. It simultaneously acts as μ receptor agonist and δ receptor antagonist. Moreover, it is a G-protein biased agonist at μ receptors, making it suitable for relieving discomfort with lesser side effects than the most opioids.
Unlike the other chemical compounds acting like certain depressants, it acts as a partial agonist, activating specific discomfort signaling pathways rather than the whole. Moreover, it also minimizes the recruitment of β-arrestin-2 at the μ receptors. β-arrestin-2 is most likely the culprit behind the adverse effects associated with some depressant usage; like respiratory depression, constipation, dependence and tolerance
Furthermore, another unique thing about its mechanism of action is that it also shows some affinity for other receptor sites like adrenergic and serotonergic receptors, which adds onto its therapeutic effects by a great deal.
Scientific Reviews On Its Mechanism Of Action
Scientific research on Mitragynine Pseudoindoxyl is still in its early stages and there is still a long way to go. Despite this, from what little data we are able to collect on this compound, it shows favorable therapeutic effects.
A study published in the Journal of Medicinal Chemistry in 2016 showed that Mitragynine Pseudoindoxyl has far greater affinity for receptors than both Mitragynine and 7-HydroxyMitragynine, making it better at relieving discomfort. Moreover, it also found that antinociceptive (inhibition of the detection of stimuli causing discomfort) tolerance and dependence developed after 29 days with Mitragynine Pseudoindoxyl, as compared to morphine that developed after only 5 days. Moreover, it also showed lower chances of respiratory depression and constipation than morphine.
Another study conducted by a scientist named Leonardo T. Yamamoto showed that Mitragynine Pseudoindoxyl has better results than both Mitragynine and Morphine in producing opioid-like effects.
A study published in Cellular and Molecular Neurobiology in 2021 also tested the significance of Mitragynine Pseudoindoxyl by administering it as a treatment for withdrawal in morphine dependent subjects. It showed that this derived alkaloid produces less physical dependence and withdrawal symptoms in Morphine dependent patients.
Comparison Between Mitragynine, 7-HydroxyMitragynine, And Mitragygnine Pseudoindoxyl
Although Mitragynine Pseudoindoxyl is a novel product, it is derived from Mitragynine and 7-HydroxyMitragynine. Here is a comparison between the three to help you understand better which one is the best option:
Mitragynine
Mitragynine naturally occurs in the Kratom plant as the most abundant alkaloid. It is an indole alkaloid, containing an indole core. Indole core usually refers to a bicyclic structure, containing a six membered benzene ring fused to a five membered pyrrole ring.
It is moderately potent alkaloid in terms of efficacy and can relieve any type of discomfort effectively. It also produces other effects like boosting focus and energy. However, it’s excessive quantity can cause some mild side effects like nausea, vomiting, constipation, and others.
Good thing is that it is completely legal in the US on a federal level. However, some states and counties have banned or regulated it independently.
7- HydroxyMitragynine
It is the second most abundant alkaloid in Kratom and a natural metabolite of Mitragynine. Structurally, it is similar to Mitragynine – except, having a hydroxyl group at the 7th position.
Moreover, it has good potency. Yes, it is more powerful than Mitragynine and 13 times more potent than the over-the-counter medication. It effectively manages discomfort, increases energy levels, and improves sleep. At persistently higher doses, it can cause nausea, vomiting, constipation, and whatnot.
Just like Mitragynine, 7-HydroxyMitragynine is also legal in the US, but subjected to either ban or some restrictions in some of the states.
Mitragynine Pseudoindoxyl
It is a semi synthetic Mitragynine derived compound produced by the oxidation of indole rings. Structurally, it is a modified version of Mitragynine with a pseudoindoxyl core. It is receptor agonist with decreased recruitment of β-arrestin-2.
It is quite potent in managing discomfort of any type without causing any side effects that are usually associated with some pharmaceutical products. There are fewer chances of suffering from respiratory depression, constipation, dependence, and tolerance.
Moreover, it also has a lesser risk of causing side effects like nausea and vomiting than the other two alkaloids. It is currently under study for any potential effects; therefore, not being used widely –except, for research purposes.
Risks Associated With Mitragynine Pseudoindoxyl Usage
Although Mitragynine Pseudoindoxyl has positive results in the pre-clinical studies, it still needs further studies before being used therapeutically for discomfort management.
As it is still in experimental phases and has been tested in animals only, there is still much need for clinical trials in humans to be sure of its effects and safety. Moreover, there is no sure data on its long term side effects in humans, making it unsuitable for human usage for now.
Furthermore, as it is a semi-synthetic derivative, it can face stricter regulatory guidelines than naturally occurring alkaloids Mitragynine and 7- HydroxyMitragynine. As it is an depressant receptor agonist and works similarly to the certain dependence causing substances, government regulatory bodies can be wary of approving it, in the wake of the recent strong depressant epidemic. This regulation can also come as a result of it being relatively understudied on its long term therapeutic effects and adverse reactions.
How Can Mitragynine Pseudoindoxyl Impact Our Lives?
Mitragynine Pseudoindoxyl has promising therapeutic applications, especially in discomfort management. People suffering from chronic conditions like cancer, neuropathic discomfort, post-operative discomfort, and whatnot, can benefit from its usage due to its potent functioning.
With the decreased chances of respiratory depression, tolerance, and dependence, it can be a perfect option for those patients who can’t use other opioids due to the risk of suffering from opioids related side effects.
Moreover, its unique pharmacology that enables it to act on multiple receptor sites, including adrenergic and serotonergic receptors, might help the patients suffering from neuropathic discomfort. It’s important to notice that opioids usually seem ineffective in neuropathic discomfort and fail to cause relief. However, this might not be the case with Mitragynine Pseudoindoxyl.
Conclusion
Mitragynine Pseudoindoxyl is a novel chemical compound that has a unique mechanism of action that makes it an ideal option for discomfort management as compared to other opioids.
Although Mitragynine Pseudoindoxyl is still under study, it shows promising results that can change the outlook on discomfort medications for the better. Its potent antinociceptive effects with lesser potential of any associated risks makes it a best option for managing discomfort.
However, there still is a great need for it to be extensively studied on its long term and consistent effects on the human body, while also establishing a side effect profile for its safe usage.
We never know, in the wake of the recent strong depressant crisis, Mitragynine Pseudoindoxyl might just be the right answer to all our discomforts!