| Autor: |
Abhisheak Sharma, Christopher R. McCurdy, Carolina Lopera-Londoño, Tamara I. King, Bonnie A. Avery, Shyam H. Kamble, Lance R. McMahon, Francisco León, Aidan J. Hampson, Kanumuri Siva Rama Raju, Erin C. Berthold |
| Rok vydání: |
2020 |
| Předmět: |
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| Zdroj: |
ACS Pharmacol Transl Sci |
| ISSN: |
2575-9108 |
| Popis: |
[Image: see text] Kratom is widely consumed in the United States for self-treatment of pain and opioid withdrawal symptoms. Mitragynine is the most abundant alkaloid in kratom and is a μ-opioid receptor agonist. 7-Hydroxymitragynine (7-HMG) is a mitragynine metabolite that is a more potent and efficacious opioid than its parent mitragynine. 7-HMG contributes to mitragynine’s antinociceptive effects in mice, but evidence suggests it may also have a higher abuse potential. This in vitro study demonstrates that 7-HMG is stable in rodent and monkey plasma but is unstable in human plasma. Surprisingly, in human plasma 7-HMG is converted to mitragynine pseudoindoxyl, an opioid that is even more potent than either mitragynine or 7-HMG. This novel metabolite is formed in human plasma to a much greater extent than in the preclinical species tested (mouse, rat, dog, and cynomolgus monkey) and due to its μ-opioid potency may substantially contribute to the pharmacology of kratom in humans to a greater extent than in other tested species. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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