Herkinorin

Herkinorin is a semi-synthetic opioid analgesic that has been derived from the natural product Salvinorin A. It was discovered in 2005 by a team at Purdue University led by Richard B. Rothman and Kenner C. Rice. Herkinorin is the first compound found to be a full agonist for the peripheral μ-opioid receptor that does not significantly recruit β-arrestin-2 after binding to and activating the receptor.

Chemistry

Herkinorin is a semi-synthetic compound, which means it is not found in nature but is instead synthesized from natural products. It is derived from Salvinorin A, a psychoactive compound found in the plant Salvia divinorum. The chemical structure of Herkinorin is similar to that of other opioids, with a basic nitrogen atom and a phenolic hydroxyl group.

Pharmacology

Herkinorin acts as a full agonist at the μ-opioid receptor, but unlike most other μ-opioid receptor agonists, it does not significantly recruit β-arrestin-2. This is significant because the recruitment of β-arrestin-2 is associated with the development of opioid tolerance and dependence. Therefore, Herkinorin may have potential as a new type of opioid analgesic that is less likely to produce these side effects.

Research

Research on Herkinorin is still in the early stages, but initial studies suggest that it may have potential as a new type of opioid analgesic. Further research is needed to fully understand the pharmacology of Herkinorin and to determine its efficacy and safety in humans.

See also

• Opioid
• Salvinorin A
• Salvia divinorum
• μ-opioid receptor
• β-arrestin-2

References

Herkinorin Resources
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