Mitragynine is the most abundant indole-receptor-based indole and active alkaloid activists in the Mitragyna speciosa plant, commonly known as kratom and < biak . The dried kratom leaves contain about 1.2-2.1% mitragynine.
Video Mitragynine
Subjective perception
Despite the fact that mitragynine is sometimes touted and used as a "legal opioid," several scientific studies have discussed the psychoactive nature of mitragynine. Most of the information available is based on anecdotal reports and patient experiences. The general subjective effects of mitragynine have been summarized in various reviews and include increased mood and analgesia, with some subjects experiencing relaxation and other stimulation (paradoxical effects).
Maps Mitragynine
Pharmacology
Mitragynine itself acts primarily through the -opioid receptors, although its oxidation product mitragynine pseudoindoxyl, acts as a selective opopic agonist but with less affinity for? or? receptors. Other alkaloids with a large contribution to the activity of kratom plant -opioids are 7-hydroxymitragynine-related compounds, which, while present in the plant in much smaller amounts than mitragynine, are much stronger partial agonists.
Derivatives
Research on the relationship of structure-activity of mitragynine leads to the discovery of new potential opioid agonists, especially some C10-halogen derivatives and 2,3-ethylene glycol bridged 7-hydroxymitragynine. The most powerful is the 10-fluoro ethylene glycol adduct of 7-hydroxymitragynine with potency 4 times higher than 7-hydroxymitragynine. Other modifications lead to 2,3-dihydro derivatives such as MGM-15, prepared by a 7-hydroxymitragynine reduction with sodium borohydride. The antinociceptive effect of MGM-15 is about 15 and 50 times stronger than morphine after subcutaneous and oral administration.
Pharmacokinetics
Mitragynine has been studied in chronic users. It undergoes extensive liver metabolism with linear and long-term kineticism.
Detection in body fluids
The concentration of blood mitragynine is expected to be in the range of 10-50? G/L in people taking recreational drugs. Detection in body fluids is usually by liquid chromatography mass spectrometry.
Structure
Structurally associated with yohimbine but exhibiting a completely different pharmacology.
Synthesis
The first total synthesis of mitragynine was reported by Takayama et al. in 1995.
See also
- 7-Hydroxymitragynine
- Mitragynine pseudoindoxyl
- Mitraphylline
- Yohimbine
References
External links
- Journal of Malay Analytical Science, Vol 15 No. 1: Simple and cost-effective mitragynine mitigation isolation protocol of Mitragyna speciosa leaf korth (ketum).
Further reading
- Mitragynine on ToxNet CASRN: 4098-40-2
Source of the article : Wikipedia
0 Comments