Kratom’s Relationship with Your Opioid Receptors

Popular for its “legal high” effect and loved for its benevolence, Kratom has lately become the main concern of both Eastern medicine advocates and Western government attorneys. Quick to label the plant as an opiate, the government is supported by anecdotal reports of a number of irresponsible users. To deny those claims and vindicate Kratom’s status as a natural remedy, we take up science and examine the relationship between the South Asian plant and our opioid receptors.

 

 

What Are Opioids and Could Kratom Be Considered One?

Science defines opioids as a class of narcotics with strong depressant effects that directly hit the central nervous system. What makes them different is their ability to stimulate endorphin release and thus provide a dizzy sensation of mental euphoria, simultaneously relieving our minds and bodies of pain. By themselves, such effects can be extremely beneficial in general medicine. In practice, however, this class of narcotics has been proven as highly addictive, and turned illegal for their potential for misuse. Why are they so addictive? Well, most of the opiate compounds, like those found in morphine, codeine or heroin, tend to meddle with our brain and body chemistry, hitting the receptors, activating them and forging a long-lasting bond.

 

What Does the Science Say?

Kratom Opioid

Studies show that Kratom in fact does form a relationship with opioid receptors as narcotics do. If that’s the case, then, what is the difference, and should Kratom be labeled as a narcotic, too?

 

The MOR Potency

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As researchers have found, the primary of Kratom’s constituents is mitragynine, an active alkaloid which bonds to our brain’s spinal cord’s and gastrointestinal tract’s µ-opioid receptors, thus providing a sense of relief and general relaxedness. The potency with which this constituent affects opioid receptors – known as MOR potency – is actually much, much lower than that of morphine, for instance. Compared to this narcotic, mitragynine has a MOR potency that amounts to around a one hundredth part of morphine’s, which is already a significant difference.

However, scientist argue that another one of the plant’s compounds is guilty for Kratom’s opioid-like effects. Way more potent than mitragynine, a mitragynine oxidation product called mitragynine pseudoindoxyl seems to be responsible for the common misconception about Kratom being a narcotic. Another one of the plant’s alkaloids, 7-hydroxymitragynine, contributes to the misapprehension even more – its MOR potency is, unlike that of a mitragynine, one tenth of morphine’s.

Potent or not, the presence of these compounds in a Kratom leaf is very small. The low-potent mitragynine is still the plant’s main alkaloid, and its ability to affect the receptors in the same way as other narcotics is way lower in intensity. As Dalibor Sames, a chemist at Columbia University explains: “Mitragynine is not a particularly very potent opioid.“ The dosage of these compounds in a dry Kratom leaf is 1-6% – around 15mg to 65mg, translated to precise measures.

 

Selective Mechanisms

Even though they bond with opioid receptors, Kratom’s alkaloids are not even remotely potent enough for the plant to be considered as a narcotic. Kratom, in fact, doesn’t contain opioids at all. The relationship those compounds form with MOR receptors is much different in comparison to that of a morphine, fentanyl or oxycodone – the mechanisms of Kratom’s alkaloids are more selective, which means that the interaction between them and the opioid receptors includes only a small subset of the receiving end.

 

The protein difference

In relation to this, there is yet another mechanism that Kratom’s alkaloids spur and that’s of the utmost significance for the difference between Mitragyna speciosa and narcotics. The opioid receptors which these compounds partially activate are entirely independent of a protein important for a well-known and well-studied opioid effect narcotics stimulate. β-arrestin, the protein in question, is responsible for all of the undesirable side-effects of narcotics, including constipation, hypoventilation and potential tolerance. To be perfectly clear, the first and most important difference between Kratom and opioids is this – Kratom does affect the same opioid receptors as traditional opioids, but avoids the side-effects of β-arrestin.

 

While functionaries continue to battle against Kratom’s gentle nature, scientific facts are undeniable – as a natural remedy, the plant has a potency for spurring endorphin release in the body, thus stimulating the opioid receptor agonism. Unlike opiates, it avoids the annoying and possibly damaging side-effects and doesn’t form addiction. Basically, this means that Kratom has the ability of relaxing and remedying both the body and mind without any risk of opiate addiction. Ultimately, Mitragyna speciosa is much more than an ordinary “legal high” – to a responsible user, its psychoactive properties are a much-needed remedy.

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