Herkinorin is fascinating

[resorcinol]

One interesting thing about it is that is supposedly causes less activation of beta-arrestins than other opioids. Beta-arrestins act to internalize u opioid receptors and this is one mechanism of down regulation and tolerance. So tolerance would rise more slowly with herkinorin in theory. Beta-arrestins don't COMPLETELY ignore herkinorin, so it's no panacea as far as tolerance goes; there are also other methods the brain uses to develop short and long term tolerance to u opioid receptor agonists.

Herkinorin is interesting to me from a chemical standpoint; it's one of the few recognized u opioid receptor agonists out there (possibly the only recognized one at this point) that has no amine functional group in it's chemical structure (ie it has no nitrogen that acts as a lewis base).

This would confer herkinorin some interesting properties. Herkinorin doesn't have a carboxylic acid group in it's structure either. With no amine or carboxylic acid group (or any of the other less common functional groups that confer acidic or basic properties to the molecule), herkinorin is unable to form salts.

Morphine, for example, can exist as the freebase, or as a salt (like morphine sulfate or morphine hydrochloride) because of the amine group it contains that has a lone electron pair, conferring lewis base properties. Other drugs have an acidic carboxylic acid group or an acidic thiol group; thiopental (the barbiturate) is an example. It has an acidic thiol (-SH) group that can have that hydrogen detached as a proton and replaced with another cation, usually a metal. thiopental is pretty much only marketed as its sodium salt, sodium thiopental.

Herkinorin has no organic base or acid groups, so it cannot from salts. This would make it behave more like THC than other opioids. Smoking would likely be an ideal way to consume. It would likely be soluble in nonpolar solvents (like fats) and relatively insoluble in water, like THC.

The chem nerd in me finds an opioid that doesn't form salts extremely interesting. It would be difficult to use via IV, as it wouldn't dissolve well or at all in water.

http://upload.wikimedia.org/wikipedia/en/thumb/e/ef/Herkinorin.svg/200px-Herkinorin.svg.png

Kinda off on a tangent, and getting on the topic of THC and cannabinoids; herkinorin is unusual as an opioid that isn't an organic base. Whereas with cannabinoids, most of them have no organic acid or base group and thus behave like THC, however there are exceptions as synthetic CB1 receptor agonists are being developed.

WIN 55,212-2
http://upload.wikimedia.org/wikipedia/en/thumb/3/3c/WIN55212-2.svg/160px-WIN55212-2.svg.png

Potent CB1 agonist, slightly more potent than THC by weight. It has basic nitrogen atoms, and forms water soluble salts. You could mix something like WIN 55,212-2 hydrochloride into a glass of juice, drink it and get stoned; snort the powder and get stoned, or dissolve in a spoon, draw up and inject and get stoned really, really fast. Reports on this compound are very positive -- it's purported to produce a very high quality pot high with less anxiety than weed.

[jonny-5]

wow man thats interesting stuff. it would be cool to get a hold of some of this WIN 55,212-2 and mix with some heroin and shoot. kind of like a stoneball instead of a speedball haha. maybe it would help with nausea in less experienced users?

[superman]

" stoneball"

hahaha, i love it!

i was checking a site recently and found that win compound has actually hit the net!!! i can't wait to try slamming that stuff!!

[resorcinol]

wow man thats interesting stuff. it would be cool to get a hold of some of this WIN 55,212-2 and mix with some heroin and shoot. kind of like a stoneball instead of a speedball haha. maybe it would help with nausea in less experienced users?

LOL, stoneball, that's a perfect name for it :p

I'm honestly more interested in this WIN compound than herkinorin. Herkinorin is interesting, but it sounds limited in ROAs, and we've got plenty of better opiates out there. I don't mean that I think the opiates commonly available around the world are already so diverse that we don't need new ones -- I think new ones are necessary for better pain control AND recreation. Opioid rotation is proven in pain management to improve efficacy, and there aren't a whole lot of options in the United States right now. Long acting meds are duragesic, mscontin, oxycontin, opana, and methadone. BT meds are dilaudid, msir, roxicodone, vicodin, opana IR, levorphanol, and actiq/fentora, and codeine (I may be forgetting a few). BT meds are a bit more diverse it seems. But we could use a few new formulations of completely new opioids, not just reformulations of opioids that have been in use for a long time.

I like weed, but I can only smoke a little bit and get a light buzz. Too much gives me anxiety. I don't like the smell, smoking it, and it can be a bit dirty side effects wise (burnout, overly sedated feelings, vision too fucked up, red eyes). This WIN compound sounds like a real winner for a cannabinoid high. The reports I've read suggest that it's a very clean, cerebral high, with little anxiety, less red eyes, and not too sedating. Also, no smell, harsh smoke, and it's far more discreet. More possible ROAs -- just overall much better. It's about time we had more choices of cannabinoids to get high on than weed, as great as weed is. I'm not dissing weed, but choices are good.

[ryan]

SWIM is going to get some herkinorin. Any idea about dose and ROA?

EDIT:

Found a thread on BL that says herky is soluble in DMSO...

If you could help me out with this resourc (or any other chemy person here) I would be eternally grateful!

[Paregoric Kid]

would it be soluble in alcohol or glycerine?
vaporizing would be interesting.

[ryan]

would it be soluble in alcohol or glycerine?
vaporizing would be interesting.

SWIM put 200 mics on foil and smoked.
No effect. Swim then gave 200 mics to an opiate nieve person, smoked it off foil, no effect.

Sucks that SWIM wasted alot of it trying to smoke it :mad:

So...it's soluble in DMSO right? Can you inject DMSO?

[Paregoric Kid]

I'm pretty sure it would be soluble in alcohol and glycerine.

[ryan]

I'm pretty sure it would be soluble in alcohol and glycerine.

Alright, SWIM will try that on monday.
Any idea why smoking it had no effect?

SWIM even had a syringe full of narcan prepped since this stuff is supposed to be active in the microgram range
SWIM was really hoping that this would be something good but was very dissapointed when nothing happened ^_^

This is the only paper I could find on any kind of dosing, and it was with primates...

http://jpet.aspetjournals.org/cgi/reprint/jpet.108.140079v1.pdf

They were able to go up to .32mg/kg IV (in DMSO) with the monkies...

Maybe SWIU didn't smoke enough?

[Paregoric Kid]

could be it didn't hit around the right vaporization temp or maybe not enough. but being as expensive as I assume it is, better try intranasal or IV. maybe try to nebulize it?

[DCBA]

Been wanting to try this for a long time.. And since its supposed easy to make i think this would be a great life long companion for me, i wished..

[ryan]

I don't know about the easy to make part...but it's extremely expensive.

[stvip]

How certain are you that the product you received is as described?

[jacky]

I found a place selling this compound finally.

for 65$ a milligram.
plus you need to have company letterhead, and they wont ship to home addresses.

I am sure the right person, with the right style, could convince this company to ship the product to them...but at the cost of 65$ a milligram, its not going to be a resource for those doing "clandestined" research.

I am very interested in the compound...but dont see the day when I could have access to the compound, and be able to afford it.
does anyone know what dosage is purported to be active for human use?

I wouldnt suspect it would be of much interest, except for long term consideration.

sure, it would be interesting to know if it works for pain, or gets one euphoric...but that is a passing interest for me...what is really interesting about this compound is the potential that it might be less addictive, or at least not have such a quick tolerance curve, or possibly, not cause much tolerance at all.

[resorcinol]

How certain are you that the product you received is as described?

I'm with stvip on this --- your product is suspect if you couldn't get high and you took enough for your tolerance (tough to figure out, I know, since potency data is significantly lacking). Herkinorin is definitely a mu-opioid agonist though.

Try sublingual instead of smoking, injecting alcohol solutions, or DMSO skin application (which I get the feeling prolly only works well for very potent compounds, and we don't know AFAIK exactly how strong this drug is -- for that reason I commend your caution in dosing, though). Smoking might decompose it potentially (don't have data on that... if somebody does, post it). IV is a little too risky for a drug so few people have tried to help zero in on potency ... plus water insolubles are nastier to shoot up due to the harshness of simple alcohols on the veins, and the need to use an alcohol as the solvent so the non-polar carbon terminal end can pull the hydrophobic drug into a solution). DMSO is hit and miss from reports I've seen with more common drugs --- so with herkinorin it's way up in the air. Do not shoot up DMSO (it might not be too toxic, but I don't know whether it is or not. again if somebody does know whether DMSO is harmful to the body, let us know. I still can't imagine it's anywhere near as safe as shooting up a water solution even if it's minimally toxic).

Sublingual won't break it down, absorbs drugs regardless of solubility in water, absorbs drugs with a higher bioavailability generally than orally dosing (and since this is chemically similar to Salvinorin A it probably has a pretty shitty oral bioavailability), and kicks in faster than oral ingestion such that you've got a chance at figuring out what an active dose is by re dosing a small amt every half hour or so.

If it absolutely does not get you high, one of two things:
1)Herkinorin is on the potent side but not as potent as we'd assumed (it's definitely active and pretty strong, but exactly how strong isn't a certain thing yet. Salvinorin A is a very potent k-agonist, but that doesn't necessarily mean herkinorin will be equally as strong a mu-agonist). Bioavailability being crappy orally is a fairer assumption to make based on Salvinorin A since absorbtion from the GI tract is gonna be more uniform for similar chemicals ... whereas potency extrapolation is borderline ridiculous since Sal A is primarily a kappa agonist and herkinorin is primarily a MU agonist: different receptors... see what I mean? Very different effects, and the receptors are similar chemically (both opioid-class GPCRs) but different enough to make potency extrapolation pretty absurd.
2)Your product is a)fake or b)highly impure

2 is really not entirely unlikely, since this is a really obscure RC as of now and thus more likely to be bunk IMO. It would suck big time if you did get ripped off, though. It could be a deliberate scam or a RC vendor that does not really know how to properly synth herkinorin or got its structure wrong accidentally or something. Either way, you get gypped.

[ryan]

SWIM got it for 84$ per milligram..there were extra costs for shipping, etc
...but it was from a reputable company.
They shipped it in a sealed strafoam thing with a coolerpack inside of it, came with the data sheet and everything..
SWIM faked a company name and they did ship it to swim's house.

SWIM did some background checking on the company and they have been around for more than 20 years and seem to be a very legit supplier. The sheet claimed to be 98% pure with an HPLC Assay and cited references and evrything...

But I guess it's possible they did rip SWIM off...

SWIM is not very keen on ordering any more from this supplier, given the results, but SWIM would like to try a different source..

Maybe some more searching will result in the one the other person in this thread found.
SWIM is not giving up on herky just yet..

BTW, swim never got around to IVing it...didn't want to take the risk, so with the other 600mics it was put in a lightbulb vaporizer and still no effect.

[stvip]

Another possibility is that the compound is unstable. I'm skeptical, though.
Other possibilities: the phenyl group prevents passing the blood-brain barrier (possibly causing herkinorin to be a good substrate for P).

Ryan, you can stop SWIMming and drowning in secrecy, it's a completely legal compound. We're risking its legal status by discussing it openly, but that's already too late. From what company did you buy? (if you still uncomfortable, contact me privately)
Since herkinorin is a close analogue to salvinorin, sublingual administration should be the ROA of choice. Perhaps I'll review the in vivo studies conducted (the nonhuman primate study did use IV adminstration).

By the way, how are you measuring such small quantities? Also, you use buprenorphine - how much, and how long have you waited before dosing with herkinorin?

Lastly, don't become lax about safety precautions. You are still dealing with an experimental compound with incredibly high affinity and agonist activity at the MOR.

I'm not sure the readers fully appreciate the potential contained this substance brings, if it is efficacious (even if it has no benefit in reducing tolerance/dependence - the implications are profound; not sure I should explain why).

[ryan]

Yeah it's a legal compound but it's still not for human consumption, and I've been arrested by the feds before and charged with serious crimes when actually I had little involvement in the whole "conspiracy" so I learned from then on to be as cautious as possible -- therefore SWIM will SWIM till SWIM is blue in teh face :)

SWIM has a friend who has access to a microgram balance. He measured out 200 mic doses from the 1 MG bottle swim received. I don't know about discussing sources here, so again it's best to be cautious about the whole thing. I will say the company is based out of switzerland, but has a US distributor as well (ie. google search: herkinorin switzerland)

The bupe was ceased 3 days prior to the attempt (about 4-8mg per day for 10 days), but there was also a non-tolerant person involved, and they also did not experience anything from smoking it.

After the first failed attempt at smoking swim IV'd 2 bags of EC #4 and was pretty high, so I doubt the bupe had anything to do with it.

And as for safety, thats why SWIU had an antag prepped and ready to go, should one fall out.

EDIT:

http://molpharm.aspetjournals.org/cgi/content/full/71/2/549

"Herkinorin is subject to degradation; therefore, drugs were produced in small batches, protected from light, and not stored in DMSO or extensively as a powder."