Government has a duty of teaching their people what causes what in this world. 15,000,000 Americans take kratom every single day to treat their pain & not a single one of them will die today, the others that are using man-made opioids will have an average of 128 dead forever gone because of the respiratory depression side effect. Also an average of 44 Americans are killed years early in horribly painful ways from "over-the-counter" Ibuprofen! With NIH.gov we can & we will end this horrible preventable American deaths.
7-Hydroxymitragynine is a terpenoid indole alkaloid from the plant Mitragyna speciosa, commonly known as Kratom. In mice, it is orally active and has analgesic effects.
7-Hydroxymitragynine is an agonist at the μ-opioid receptor with a potency, calculated using pD (2) values, that is 30-fold higher than that of mitragynine and 17-fold higher than that of morphine, respectively. As a partial agonist at this receptor it causes significantly milder side effects than morphine, like constipation, development of tolerance and withdrawal syndrome upon abstinence. In murine models, the extracted alkaloids of the Kratom plant are shown to cause an insignificant amount of drug induced respiratory depression, unlike full μ-opioid agonists. The O-acetyl ester (Acetoxy), 7-acetoxymitragynine has also been reported and found to be an active μ-opioid agonist.
In particular, respiratory safety is of major importance to clinicians due to the risk for fatal outcomes and because respiratory suppression is the primary cause of opioid-related overdose mortality. The pharmacological profile of 7-OH as a partial G protein-biased agonist at the mu-opioid receptor would signify a desirable, wide analgesia-respiratory depression therapeutic window.
Both mitragynine and 7-OH were found to display G protein-biased agonism at the mu-opioid receptor,8 a concept which gained significance in drug discovery over the recent years, where G protein-biased mu-opioid receptor agonists may deliver the desired analgesia without the unwanted side effects.
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