Drug info - Herkinorin: Psychedelic Opioid (Salvinorin analog)

[snapper]

This is interesting a little disturbing compound I found mentioned on another forum.

NOVEL ANALGESICS FROM SALVINORIN A
Kevin J. Tidgewell, 1 Wayne W. Harding,1 Robert A. Moyer,2 Chad Groer,2 Christina M. Dersch,3 Richard B. Rothman, 3 Laura M. Bohn, 2 Thomas E. Prisinzano 1* 1The University of Iowa; 2 The Ohio State University College of Medicine; 3IRP, NIDA, NIH, DHHS Baltimore, MD

Salvinorin A, the major active component of the hallucinogenic sage Salvia divinorum, has been shown to be a potent and selective ?-opioid receptor agonist. Previous studies by our lab have shown that derivatives of salvinorin A have activity in tests of nociception in rats. Herkinorin, a previously reported analogue with anti-nociceptive characteristics, was evaluated using a chronic drug administration paradigm and animals were tested using the formalin model for nociception. Herkinorin appears to have an altered mechanism of cellular activation which leads to reduced potential for tolerance. This finding is significant because salvinorin A analogues could represent a class of opioid ligands with altered cellular activation leading to analgesics with reduced potential for abuse. These experiments create an intriguing story about a possible longer acting salvinorin A derivative with ?OR activity and a decreased potential for the development of tolerance. This research is funded by a grant from the National Institute on Drug Abuse (DA 18151).

SWIM thinks that new analgesics derived from salvinorin may also lead to prohibition of salvinorin. This is nonetheless interesting as it seems salvia is spawning a whole new class of analgesics. There is actually a lot of information on this compound. It is also purported to be hallucinogenic, as well as not inducing a tolerance.
Here's another abstract.

J Nat Prod. 2006 Jun 23;69:914-918
Synthesis of Salvinorin A Analogues as Opioid Receptor Probes.
Kevin Tidgewell, Wayne Harding, Anthony Lozama, Howard Cobb, Kushal Shah, Pavitra Kannan, Christina Dersch, Damon Parrish, Jeffrey Deschamps, Richard Rothman, Thomas Prisinzano

Several neoclerodanes, such as salvinorin A (1) and herkinorin (3), have recently been shown to possess opioid receptor activity in vitro and in vivo. To explore the structure-affinity relationships of this interesting class of compounds, we have synthesized a series of analogues from 1 isolated from Salvia divinorum. Here, we report the semisynthesis of neoclerodane diterpenes and their structure-affinity relationships at opioid receptors. This work will allow the further development of novel opioid receptor ligands.