Kratom is a plant that has been traditionally used for pain relief and to treat opioid dependence. The main active chemicals in kratom are mitragynine and 7-hydroxymitragynine. In this study, the researchers made new versions of these chemicals and tested them to see if they could provide pain relief without the serious side effects of opioids like respiratory depression and constipation.
They found that one new compound, 6 (SC13), was able to block pain signals in mice just as well as the opioid painkiller morphine, but it did not cause the same level of respiratory problems, constipation, or addictive behaviors. The researchers think this is because 6 (SC13) only partially activates the mu opioid receptor, the same receptor that standard opioids target, rather than fully activating it.
This study was conducted in a lab, using experiments on cells and animals (mice).
Key takeaways:
- Kratom is a tetraploid plant, meaning it has extra copies of its genes.
- The kratom genome was sequenced and assembled, providing a resource for future research.
- Genes potentially involved in alkaloid biosynthesis were identified.
- This study was a lab-based genomic analysis, not an animal or human study.
For further reading:
Link: https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01273
Full Citation:
Chakraborty, S., DiBerto, J.F., Faouzi, A., Bernhard, S.M., Gutridge, A.M., Ramsey, S., Zhou, Y., Provasi, D., Nuthikattu, N., Jilakara, R., Nelson, M.N.F., Asher, W.B., Eans, S.O., Wilson, L.L., Chintala, S.M., Filizola, M., van Rijn, R.M., Margolis, E.B., Roth, B.L., McLaughlin, J.P., Che, T., Sames, D., Javitch, J.A., and Majumdar, S. (2021). A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects. Journal of Medicinal Chemistry, 64, 13873-13892.
