Kratom Alkaloids as Probes for Opioid Receptor Function: Pharmacological Characterization of Minor Indole and Oxindole Alkaloids from Kratom

This study investigated the pharmacological properties of several minor alkaloids found in the kratom plant, including corynantheidine, mitraciliatine, isopaynantheine, corynoxine, and corynoxine B. The researchers used a variety of in vitro (cell culture) and in vivo (in-life) tests to evaluate the effects of these compounds on opioid receptors in mice and humans.

The key findings were that some of the minor alkaloids, such as corynoxine and mitraciliatine, displayed potent analgesic (pain-relieving) effects that were mediated through the mu-opioid receptor. Interestingly, these compounds also showed reduced side effects like respiratory depression and hyperactivity compared to the prototypical opioid drug morphine. Another alkaloid, isopaynantheine, was found to be a selective agonist of the kappa-opioid receptor, which could have implications for the development of safer opioid-based painkillers.

Key takeaways:

  • Several minor kratom alkaloids have potent analgesic effects mediated through opioid receptors.
  • Some of these minor alkaloids may have improved safety profiles compared to traditional opioids.
  • Kratom contains a diverse array of pharmacologically active compounds that warrant further investigation.
  • This study provides valuable insights into the mechanisms of action of kratom and its potential therapeutic applications

For further reading:

Link: https://pubs.acs.org/doi/10.1021/acschemneuro.1c00149

Full Citation:

Chakraborty S, Uprety R, Daibani AE, Rouzic VL, Hunkele A, Appourchaux K, Eans SO,
Nuthikattu N, Jilakara R, Thammavong L, Pan YX, McLaughlin JP, Che T, Majumdar S. Kratom Alkaloids as Probes for Opioid Receptor Function: Pharmacological Characterization of Minor Indole and Oxindole Alkaloids from Kratom. ACS Chem Neurosci. 2021 Jul 21;12(14):2661-2678. doi: 10.1021/acschemneuro.1c00149. Epub 2021 Jun 16. PMID: 34131071; PMCID: PMC8357174.