Kratom alkaloids are structurally similar to psychedelics however psychedelic activity has never been reported. Kratom effects are opiate like and have been reported to be similar to Codeine and Vicodin. Interestingly Codeine and Vicodin are also used to help with Heroin addiction. Vicodin is currently the most popular drug in the United States with approximately 100 million people receiving a prescription last year.
Even through Mitragynine is an opiate withdrawal suppressant, its effect are not reversed by the opiate antagonist nalorphine. The opiate effects from Kratom are mediated by the delta and mu opiod receptors. Mitragynine in low doses produces a yohimbine-like attaching to alpha-adrenergic receptors(and partial attaching to the delta opioid receptors) - hence the stimulating effects at low doses. At higher doses, attachment to the delta opiod receptors increases and in very high doses we see attachment to the mu receptors - hence the sedative effects. Mu crossover is reportedly increased if opiate drugs are present.
Although delta receptor selective opiate drugs show almost no abuse potential, they can be used as a primer allowing mitragynine to more effectively attach to the mu receptor, which mediates the euphoric high produced by morphine.
Other effects of mitragynine are a reduction in smooth muscle tone, central nervous system depression and local anesthesia. Acute side effects include increased urination, dry mouth, loss of appetite, and constipation coupled with small, very dark stools. As with opiates, kratom in large doses can cause nausea and vomiting. Heavy use can also result in a prolonged sleep - that being said, some find Kratom stimulating and have trouble sleeping.
Thought to be the primary alkaloid in Kratom, 7-hydroxymitragynine, interacts with the three major opiod sites: Kappa, Delta and Mu. 7-hydroxymitragynine binds preferably to Mu's with a pKi value of 8.01+/- 0.02. Its only recently that 7-hydroxymitragynine has been thought to be the primary active. Previously, the majority of research has focused on the whole kratom plant and mitragynine. Subsequently, less is know of 7-hydroxymitragynine and research continues.
One last chemical in Kratom worth a shout is (-)-epicatechin. This is the chemical found in Dark Chocolate, Green Tea and Cranberry juice.(-)-Epicatechin has a wide range of benefits from reducing cancer risks, reducing the effects of free radicals on the body , and is a very powerful antioxidant - helping to prevent fat cells from oxidizing and blocking arteries. It helps with urinary infections and is beneficial to diabetics because it mimics insulin. It helps with blood sugar levels, inhibits alpha-amylase and prevents growth of bacteria such as E-Coli.
7-Hydroxymitragynine is an active alkaloid in Kratom. It has opioid agonistic activity. "The potency, calculated using pD (2) values, was 30- and 17-fold higher than that of mitragynine and morphine, respectively. Antagonism of naloxone on concentration-response curves for 7-hydroxymitragynine confirmed its opioid effect. These results suggest that the opioid effect of M. speciosa is mostly based on the activity of 7-hydroxymitragynine. If your looking to buy 7-Hydroxymitragynine, look here. This alkaloid is the main asspect addeded to Kratom Tincture.
Mitragynine is the most abundant active alkaloid in the Kratom plant. In small doses its activity is reported to be stimulant like, while in higher doses more opiate like. These effects agree with the profile of mitragynine's actions developed by study of its action on the brain. It has been shown to be adrenergic (like some related alkaloids from yohimbe) at lower doses while at higher doses mitragynine acts on the mu and delta opiate receptors. The mu opiate receptors are responsible for the enjoyable effects of the opiates, analgesia, and physical dependence. Its potential for treating drug addiction, perhaps in combination with ibogaine, is being investigated. It is orally active.
Mitragynine was isolated in 1907 by D. Hooper, a process repeated in 1921 by E. Field who gave the alkaloid its name. Its structure was first fully determined in 1964 by D. Zacharias, R. Rosenstein and E. Jeffrey.
It is structurally related to both the yohimbe alkaloids and, more distantly, voacangine. It is even more distantly related to other tryptamine-based psychedelic drugs such as psilocybin or LSD. Chemically, mitragynine is 9-methoxy-corynantheidine.
Mitragynine itself acts primarily via μ-opioid receptors, although its oxidation product mitragynine-pseudoindoxyl, which is likely to be a major component of kratom that has been aged or stored for extended periods, acts as a fairly selective δ-opioid agonist with little affinity for μ or κ receptors. Another alkaloid with a major contribution to the μ-opioid activity of the kratom plant is the related compound 7-hydroxymitragynine (above), which while present in the plant in much smaller quantities than mitragynine, is a much more potent μ-opioid agonist.