Kratom: Difference between revisions

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Mitragynine has a methyl-ether group that interacts with V143 and C217 present on the opioid receptor. Mitragynine has a secondary and tertiary amine that is capable of interacting with the important D147 residue as well as a ring structure that is capable of orienting across from the histidine residue. A recent study published in August of 2020 on mitragynine and 7-hydroxymitragynine binding to the mu-opioid receptor [3][4] investigated if and how mitragynine was able to enter the active site. The study discovered that not only does mitragynine bind in the active site but it also activates the G-protein pathway. The interesting thing about the activation pathway is that the majority of the time it does not recruit beta-arrestin. Unfortunately, Cytochrome P450 metabolic enzymes have been shown to involve with the metabolism of mitragynine. The enzymes seem to be inhibited by mitragynine and therefore raise concern for adverse drug reactions.[4] Cytochromes P450 are heme-containing enzymes that oxidize steroids, fatty acids, and xenobiotics. These enzymes also play a large role in clearing a hefty amount of compounds from the body and aid in hormone synthesis and decay.[8]
Mitragynine has a methyl-ether group that interacts with V143 and C217 present on the opioid receptor. Mitragynine has a secondary and tertiary amine that is capable of interacting with the important D147 residue as well as a ring structure that is capable of orienting across from the histidine residue. A recent study published in August of 2020 on mitragynine and 7-hydroxymitragynine binding to the mu-opioid receptor [3][4] investigated if and how mitragynine was able to enter the active site. The study discovered that not only does mitragynine bind in the active site but it also activates the G-protein pathway. The interesting thing about the activation pathway is that the majority of the time it does not recruit beta-arrestin. Unfortunately, Cytochrome P450 metabolic enzymes have been shown to involve with the metabolism of mitragynine. The enzymes seem to be inhibited by mitragynine and therefore raise concern for adverse drug reactions.[4] Cytochromes P450 are heme-containing enzymes that oxidize steroids, fatty acids, and xenobiotics. These enzymes also play a large role in clearing a hefty amount of compounds from the body and aid in hormone synthesis and decay.[8]


[[Image: MorphineOrientation.jpg|300px|left|thumb| Morphine Orientation in an Opioid Receptor]]
[[Image: MorphineOrientation.jpg|500px|left|thumb| Morphine Orientation in an Opioid Receptor]] [[Image: MuOpioidReceptor.jpg|300px|left|thumb| Mu-Opioid Receptor]]


== Clinical Significance ==
== Clinical Significance ==