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7-Hydroxymitragynine (7-OH) is a terpenoid indole alkaloid from the plant Mitragyna speciosa, commonly known as kratom. [2] It was first described in 1994 [3] and is a human metabolite metabolized from mitragynine present in the Mitragyna speciosa, commonly known as kratom. 7-OH binds to opioid receptors like mitragynine, but research suggests that 7-OH binds with greater efficacy.
Mitragynine is the most abundant active alkaloid in kratom. In Thai varieties of kratom, mitragynine is the most abundant component (up to 66% of total alkaloids), while 7-hydroxymitragynine (7-OH) is a minor constituent (up to 2% of total alkaloid content).
Mitragynine pseudoindoxyl is a rearrangement product of 7-hydroxymitragynine, an active metabolite of mitragynine. [1] Mitragynine pseudoindoxyl can be produced in the blood as a metabolite of 7-hydroxymitragynine. [2]
Mitragyna speciosa is a tropical evergreen tree of the Rubiaceae family (coffee family) native to Southeast Asia. [3] It is indigenous to Cambodia, Thailand, Indonesia, Malaysia, Myanmar, and Papua New Guinea, [4] where its leaves, known as kratom, have been used in herbal medicine since at least the 19th century. [5]
Some recent research on 7-hydroxymitragynine discovered that compared to morphine who is a full agonist. It has an intrinsic activity between 99%-104% so we can say that 7-Hydroxymitragynine is a full agonist not a partial agonist like it was said before.
Acute use (1–3 days) yields a potency about 1.5× stronger than that of morphine and chronic use (7 days+) yields a potency about 2.5 to 5× that of morphine. Similarly, the effect of tramadol increases after consecutive dosing due to the accumulation of its active metabolite and an increase of the oral bioavailability in chronic use.
More specifically, it is an antagonist/inverse agonist at most or all sites of the histamine H 1 receptor, serotonin 5-HT 1D, 5-HT 1F, 5-HT 2A, 5-HT 2B, 5-HT 2C, 5-HT 3, 5-HT 6, and 5-HT 7 receptors, and adrenergic α 1-and α 2-adrenergic receptors, and additionally a norepinephrine reuptake inhibitor.
Alvimopan (trade name Entereg) is a drug which behaves as a peripherally acting μ-opioid receptor antagonist.With the limited ability to cross the blood–brain barrier and reach the μ-opioid receptors of the central nervous system, the clinically undesirable effects of centrally acting opioid antagonists (like reversal of opioid-mediated analgesia) are avoided without affecting the intended ...
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