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Salvinorin A

Captain.Heroin

Captain.Heroin

Bluelight Crew
Joined
Nov 3, 2008
Messages
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Seems to be some knowledge lacking, that I cannot find, and I would like to ask some theoretical questions.

I can't find any ROA other than smoked or sublingual. I can't find any BA at all.

I imagine with a close to pure powder, it could be injected, IM, for a long duration. I also imagine you could get higher dosages without the need for massive bong hits.

Apparently it is soluble in ethanol, acetone, but not significantly so in water. Would a < 10% alcohol + water solution suffice? Are there other solvents that could be used?

I would like to imagine that it could be injected.
 
Is it soluble in DMSO? It wouldn't need to be THAT soluble, due to the insane weight potency of salvinorin-A.
 
Limpet_Chicken said:
Is it soluble in DMSO? It wouldn't need to be THAT soluble, due to the insane weight potency of salvinorin-A.
Click to expand...

but you would need it soluble enough to get a good idea of the concentration of your solution, and not a guess based on physical data.

The only way to the maximum concentration if water that would allow dissolution in EToH would be to try.
 
Salvinorin has a logp of about 2.2 and lacks any groups that are easily ionizable, so you're not going to be able to dissolve it in water. Ethanol/water mixtures are equally bad.

I recall reading an Erowid page detailing people making sublingual S. divinorum tinctures by using acetone, apparently it has a much higher solvency for salvinorins and you can make the tincture more concentrated.

I imagine with a close to pure powder, it could be injected, IM, for a long duration.
Click to expand...

The duration would be similar to having smoked it, salvinorin is rapidly metabolized by carboxylesterases to inactive compounds.

If you were to formulate this for IV/IM you would need to make an emulsion of some sort or dissolve it in straight DMSO.
 
Well, the point was, it wouldn't need to be fantastically soluble compared to most compounds, for transdermal DMSO administration. One would only need a solubility to allow 50-100ug/ml maybe to dissolve in DMSO.

Here is a thought-what about liposomes? would be a bit more advanced than just sticking it in a solvent but might allow for good body penetration, in a lipid environment, especially if in a micelle-like format, with a double layer to separate hydrophobic vs hydrophilic sides.

As for an acetone sublingual tincture? yuck. Ever actually tasted the stuff? its pretty revolting.

(edit-no, I wasn't drinking the stuff. Just got a taste. Even the fumes are vile tasting, if it gets to the back of the throat, its sickly, revolting fruity sort of smell/taste, like acetaldehyde minus the acridity, only worse and more in-your-face)
 
I'd still sooner take the EtOH burn over acetone. Maybe its just me, but I hate the smell of the stuff. And even the vapors getting in my mouth it makes me dry heave just thinking about it.
 
sekio said:
Salvinorin has a logp of about 2.2 and lacks any groups that are easily ionizable, so you're not going to be able to dissolve it in water. Ethanol/water mixtures are equally bad.

I recall reading an Erowid page detailing people making sublingual S. divinorum tinctures by using acetone, apparently it has a much higher solvency for salvinorins and you can make the tincture more concentrated.



The duration would be similar to having smoked it, salvinorin is rapidly metabolized by carboxylesterases to inactive compounds.

If you were to formulate this for IV/IM you would need to make an emulsion of some sort or dissolve it in straight DMSO.
Click to expand...

I imagine injecting acetone is a no-go...

"Emulsion" is vague, are you talking an oil or what?

Is it impossible to create a pro-drug due to its structure?

I take it dimethyl sulfoxide can be injected?
 
DMSO has a tendency to rapidly penetrate intact skin, and it carries whatever is dissolved in it with it. Facilitating transdermal delivery of substances, and/or (accidental?) poisonings etc. Stuff makes me rather nervous to be honest, it isn't toxic, but a reaction in DMSO with anything nasty in it, spill it and its going in you at a touch.
 
Captain.Heroin said:
Is it impossible to create a pro-drug due to its structure?
Click to expand...

291px-Salvinorin_A2DCSDS.svg.png


See that acetyl group on the top right? That thing comes off *very* quickly, leaving behind a hydroxyl group, just like the acetyl groups on heroin. Except where heroin turns into active morphine, salvinorin A is converted into inactive salvinorin B.

Normally, you'd make a prodrug by sticking an acyl or alkyl group on a polar (i.e. OH or NH2) group of the active form; yet here the one with the OH group is the inactive metabolite, and the one with the acetoxy ester intact is the active form.

So the trick to making longer-lasting salvinorin is to replace the more lipophilic group that readily gets cleaved off (the acetyl ester) with one that doesn't get metabolized quite as quickly (ex.: an ether, as in the case of the much more potent salvinorin B methoxymethyl ether).
259px-Salvinorin_B_methoxymethyl_ether.svg.png

(note: the methoxymethyl ether is located on the left in this pic)
 
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"Emulsion" is vague, are you talking an oil or what?
Click to expand...

Are you familiar with how propofol is formulated for injection? Some sort of oil base to dissolve the drug, an emulsifier (lecithin?) and some water, all as a stable oil-in-water emulsion. There are a few other drugs that use similar delivery systems, usually it's for drugs that will not dissolve in water no matter how hard you coax them.

Some people can't tolerate emulsions IV and get allergic reactions.

I was under the impression that there were some benzos delivered as a glycol injection too (diazepam) and maybe that would do the trick too.

The salvinorins also have a methyl ester & a lactone ring that can be metabolically opened too.
 
Per that link, S. recognita is identified as containing 212.86 ? 20.46 μg/g, that seems to me to be very high, how does it compare to S. divinorum?
 
Yes, I saw that paper too.

Now are we going to have people pilliaging garden stores for those sweet kappa ligands???
 
There is certainly a way to prepare an oily emulsion if you were stubborn, using protocols used for other water-insoluble drugs. After all there are quite a few medications which are insoluble in water and require i.m. or i.v. administration, aside from propofol penicillins and benzodiazepines like diazepam came to my mind right away, but there are much more as I've just found two free reviews on insoluble drug delivery if anyone is interested:
Insoluble drug delivery strategies: review of recent advances and business prospects
Techniques to Enhance Solubility of Hydrophobic Drugs: An Overview

BTW, S. recognita got me interested, I had no idea another species contained salvinorin A and that it originates from a place much closer to me than the home of S. divinorum.
 
To answer my own question, from the results of analysis on dried leaves of S. divinorum, obtained from a headshop, it contains ~400 ug/g. So while S. recognita still contains levels well below S. divinorum it would definitely be a viable source.
 
Thank you Hodor.

I learned something about pharmacokinetics. Just 2 to 3 hour duration though? Seems like a decent increase. I imagine most people would be sick of it long before 2 or 3 hours.

I am quite ignorant and have a lot of learning to do.

I knew if there was a will, that there would be a way.
 
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sekio said:
Are you familiar with how propofol is formulated for injection? Some sort of oil base to dissolve the drug, an emulsifier (lecithin?) and some water, all as a stable oil-in-water emulsion. There are a few other drugs that use similar delivery systems, usually it's for drugs that will not dissolve in water no matter how hard you coax them.

Some people can't tolerate emulsions IV and get allergic reactions.

I was under the impression that there were some benzos delivered as a glycol injection too (diazepam) and maybe that would do the trick too.

The salvinorins also have a methyl ester & a lactone ring that can be metabolically opened too.
Click to expand...

I am familiar (though we have fospropofol now), though I have never used it myself. I am sure I would have intentionally overdosed on it, it sounds lovely and quite euphoric.
 
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