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Herkinorin: New extremely potent opioid w/ unusual properties

AlphaOdure

Bluelighter
Joined
Jul 7, 2003
Messages
1,412
Location
eastern U.S; great lakes area; big city
Just thought i'd bring this new chemical to everyone's attention... i know it was discussed in one short thread in ADD but thats it. Anyways, in a nutshell- its called herkinorin; and its synthesized from salvinorin B, i think... The wiki article was sort of confusing, it says:

Herkinorin is a semi-synthetic compound made from Salvinorin B, which is made from Salvinorin A, which is extracted from the plant Salvia divinorum
But thats bullshit. Salvinorin B is a naturally occuring diterpene thats found in 1Salvia Divinorum. I think the information is relatively new as the article cites studies done in 2005, so in time i'm sure it will be corrected, expanded, and refined. But anyways... we at least know its a semi-synthetic opioid (opioid in the pharmacological sense; in chemistry, its not really even a true opioid) made from salvia as opposed from opium.

But interestingly enough, its about as potent an agonist at mu receptors as Salvinorin A is on kappa receptors (thats really strong, we're talking active doses in the high microgram range)! And it is 100x less potent at kappa opioid receptors compared to Salvinorin A. But even more interesting... herkinorin actually inhibits arrestin cellular uptake unlike every other mu-opioid agonist known (in short, arrestin is responsible for our current understanding of physical tolerance. Arrestin are indigenous, intracellular substances used by cells to quiet over stimulated electrical activity, they plug into neurotransmitter receptors that are overactive).

This basically means that herkinorin would produce little to no tolerance even w/ repeated or habitual use. But this could also imply herkinorin may be neurotoxic to opioidergic systems if there is no inherit means for the neuron to limit its own electrical activity. However, some of the medical community disputes the fact that arrestin's intracellular action is soley responsible for the mechanism of tolerance and that we do not understand the full spectrum and pharmacology of tolerance. Arrestin no doubt plays a major role in physical tolerance, but to what extent? We really don't know...

Some other side notes on the herkinorin- like the natural Salvinorin diterpenes, its unlikely to be active orally. IV injection is untested (probably works, solubility would be a factor though. I know there must be some problems with shooting diterpenes). Most likely active routes of administration that are minimally invasive (i.e.- not IV, IM, SUB) include sublingual (efficiency unkown) and smoking. If ever used recreationally, smoking would in all likelyhood be the most effective ROA; as diterpenes and terpenes can usually be smoked very efficiently.

Oh and btw, the drug is still LEGAL! Which means its only a matter of time before its sold as a research chemical; and then all scientific inquiry and investigation into this unique drug will be stopped once its scheduled.

http://en.wikipedia.org/wiki/Herkinorin
 
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Wow, This got me extremely interested. I wish i had a better understanding of the chemical and technical parts of drugs as i do about the "street smarts" part of drugs. Any more info you got, especially in "dumbed down" terms for my ol' uneducated ass would be great. This kinda shit is a lil fascinating Ima say.
 
I always thought it was really interesting how the major component in salvia binds to kappa opiate receptors and just has such extremely bizarre effects.

They developed pharmaceuticals that didn't bind to Mu or Delta receptors but had high affinity for kappa receptors and when they had people try them they always felt disphoric and experienced bizarre side effects, such as depersonalization. But that's all that salvia is, it just binds to that same receptor.

But that's interesting that they developed a synthetic from the salvinorin B. I wonder if overdose would be really easy with that much affinity to the Mu receptor. I also wonder if diterpenes have different feeling effects than what regular opium would be like.
 
^ ^ ^
Yes, anesthetics were developed in the 70s that had selective affinity for kappa opioid receptors. But they were discontinued b/c patients were experiencing hallucinations, dissociative depresonalization, and dysphoria during anesthesia.

And lacey k- i basically posted all the available information on herkinorin. If i find anything new out i will definitely post it in this thread though. I'll re-explain its pharmacology in "dumbed-down-terms" later on, i've got class tomorrow and i need some sleep!

Btw, anyone else w/ info on this substance, or references to new information on it... please post it!
 
Opiate research underway
Dave Mosher

A compound which could potentially replace morphine, a widely used narcotic pain-relief drug, began its journey with a drug user in Mexico.

Dr. Laura M. Bohn of Ohio State's Department of Pharmacology said the curious drug user sent a sample of the mint plant species known as Salvia divinorum to Bryan Roth, a biochemist at Case Western Reserve University. The user knew something about both science and drugs, Bohn said, and wanted to know if the active ingredient in the plant was hitting serotonin receptors - a class of receptors responsible for hallucinogenic experiences.

"This plant is related to Salvia in peoples' gardens," Bohn said, "but this particular species grows in Mexico and has been used by Mazatec Indians in vision ceremonies."

Bohn said after some time Roth's group isolated the active compound in the plant which is now known as salvinorin A. During their research, Roth's group also found that the drug had analgesic, or pain-relieving, properties comparable to morphine.

Dr. Thomas Prisinzano, a medicinal chemist at the University of Iowa, then stepped into the picture to study salvinorin A for potential medical uses.

"I got in touch with Dr. Roth after reading his paper and we used chemistry to enhance its pain-relieving properties," Prisinzano said.

Prisinzano said that salvinorin A served as the lead compound, a substance in medicinal chemistry that has favorable effects but is not clinically tested. The result, Prisinzano said, was a chemical called Herkinorin.

Bohn said the compound got its name from Herky the Hawkeye, UI's mascot.

"Of course when it's perfected," Bohn said, "I want it to be called Brutusnorin or Buckinorin."

Bohn was cautious, however, to predict a date for clinical trials but speculated it would be at least 10 years before major publicized progress would be made, if at all.

"At this point it's just a compound," she said.

"Chemists have been working since the 1920s to enhance (morphine's) pain relieving properties and eliminate its addictive properties," Bohn said, "and here in 2005 we're still working on this."

full article.

This seemed interesting, but Herky the Hawkeye...
3578bq9.jpg
...really?
BTW, this Herky character certainly looks pissed about something, huh?
 
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AlphaOdure said:
...i basically posted all the available information on herkinorin...

What about a synthesis? Would it be simple or complex? I mean, it probably could be as easy as some type of extraction on some salvia extract. Or, it could be nothing like that at all. Either way, I wanna know. I wanna try this shit.
 
So, would this have opioid effects or psychedelic effects or some bizare mix?
 
Well I found out you can get it, $60 for 1mg ... jesus, unless this is as potent as fentanyl it must be hard as hell to synthesize.
 
I'd be willing to try it if anyone could determine the proper dosage and ROA.
 
Nickatina said:
Well I found out you can get it, $60 for 1mg ... jesus, unless this is as potent as fentanyl it must be hard as hell to synthesize.

PM me please. lol =D

Seriously. Do it.
 
Yeah, somebody needs to determine the proper dosage on this stuff so we can administer new and potentially dangerous and neurotoxic drugs to ourselves without medical supervision! WOOHOO! Seriously, though, somebody needs to get on that.
 
Ness said:
Yeah, somebody needs to determine the proper dosage on this stuff so we can administer new and potentially dangerous and neurotoxic drugs to ourselves without medical supervision! WOOHOO! Seriously, though, somebody needs to get on that.

Well said.
 
Ness said:
So, would this have opioid effects or psychedelic effects or some bizare mix?

People are asking redundant, stupid questions that were answered in my original post... If you'd actually read the fuckin OP instead of just randomly posting questions after you read, "new potent, strong opioid..." most your questions would be answered...

It has MU opioid activity, it has very little KAPPA opioidergic activity. Therefore, it shouldn't really produce much psychedelic effect-- that is, if you could call kappa opioid agonists "psychedelic."

I'd be willing to try it if anyone could determine the proper dosage and ROA.

AGAIN... to repeat myself... this drug is very potent and is ACTIVE IN THE MICROGRAM range (maybe if i type in caps, people will actually fuckin read it this time around?). This drug has the ability to be very strong and easy to overdose on, as diterpenes are usually smoked. And herkinorin itself isn't active orally (like salvinorin A). Furthermore, IV, IM, or SUB use is probably extremely dangerous- not only b/c injecting drugs that are active in the microgram range can very easily instigate overdose; but injecting terpene's can be tricky, due to solubility issues.
 
^I read the entire OP. It was my mistake misinterpreting it and thinking it might have psychedelic properties. And as for being active in the microgram range, that's about as useful as saying something is active in the milligram range. 100ug could be fine, 200ug could be fatal.
 
IForgett said:
What about a synthesis? Would it be simple or complex? I mean, it probably could be as easy as some type of extraction on some salvia extract. Or, it could be nothing like that at all. Either way, I wanna know. I wanna try this shit.

No, it wouldn't be simple. Note how its called a "semi-synthetic opioid." Meaning, its not a naturally found substance. Doing a simple extraction method on Salvia would just leave you w/ Salvinorin A & B; and you definitely wouldn't have anything pharmacologically similar to herkinorin. (I must admit though, the whole terminology of the thing is sort of confusing, if salvinorin A were pharmacologically similar to opioidergic drugs, then what would you call it? It couldn't be an opiate b/c its not from opium.. and it couldn't be an opioid b/c its not synthetic. Thats why the term "semi-synthetic opioid" i think is sort of confusing for herkinorin- its not derived from, based on, or synthesized from opium alkaloids.)

Anyways, if you find a source to herkinorin- do not blindly run into trying this chemical. Its still a very young molecule and significant testing still needs to be performed to determine- dosage levels, full neurological profile, if a lack of arrestin interaction leads to neurotoxicity, side effects, and many other things.

I find it hard to believe that vendors are selling this to individuals in small doses (selling 1 mg basically means its being sold for personal consumption instead of researching purposes). I'd be weary, don't get ripped off. But if it is actually being sold... damn man, in a way thats sort of shitty. Because you know it will eventually lead to the scheduling of Salvia, salvinorin A & B, herkinorin, and any related chemical. Not that i enjoy salvia, but the prohibition of any drug in my eyes is ignorant. And there could be a whole new class of compounds developed from Salvia.
 
Even if we don't take it we should all still buy some just incase it gets emergency scheduled...if any type of drugs woudl be it'd definetley be opiates since they're pretty high up there on the goverments worst drugs list.

But yeah we should buy an mg or two and then once the goverment simultaneously does studies, figures out doses and realizes it's being sold as a research chemical we would HAVE A LARGE SUPPLY OF ILLICIT DRUGS! HOOOORAY!...oh wait we already do.
 
Damn a opiate that possibly produces no tolerance that would be fucking nice. Now if we could get one that doesn't produce dependence we would be all set.
 
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