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Amfonelic Acid Solution?

R

romealone

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Joined
Jan 28, 2010
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Hi. I was hoping for some suggestions regarding the best solvent to use if one wished to make a solution of amfonelic acid that would be appropriate for IV admin. It isn't soluble
 
sekio said:
Adjust the pH...
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I figured that would be the best way to go, but from the figures I've seen, amfonelic acid is still not particularly soluble in 0.1M NaOH (5mg/mL). This solubility would be fine if the potencies I've seen listed for this substance from numerous sources were anywhere near accurate (many sources list it as being very active in microgram ranges, and that it is 50X the potency of methylphenidate). These estimations are waaaaay off.

For those who have actually researched amfonelic acid, a moderate dose would be in the 15-20mg range via nasal route. Because of the complete lack of PNS effects, it is easy to go far above these dosages without experiencing the negatives usually associated w overdoing it w a stim, however this also poses a potential danger since without the negative PNS feedback (no inc HR, vasoconstriction, etc), I could see one getting into trouble from the dopaminergic effects at higher doses.

Anyhow, back to the solubility issue. Any advice as to how to create a safe (sterile) solution that could reach closer to the 20mg/mL range? Might propylene glycol fit the bill? Can't find any info on its solubility in PEG.

But any suggestions as to how to create a sterile solution with concentrations closer to 15-20mg/mL for a solution that would be safe for Parenteral use if one were so inclined.

Btw...anyone else have any experience with this? Very interesting compound. I know the antibiotic effects of this are potential cause for concern, but considering antibiotics in this class w very similar structures are used at doses in the 500-1000mg range, I doubt the occasional use of this product in the double digit mg range is likely to cause problems. Now if one were to use this daily as they would their adderall script..that might be a recipe for MRSA, but barring that, I don't anticipate issues in that regard


EDIT: I see Sigma lists amfonelic acid as being soluble in ethanol. They don't quote how soluble..just that it's soluble. Obviously injecting ethanol is quite dangerous, but if it is very soluble in ethanol, might the best way of producing a safe solution for Parenteral use be to dissolve it in a small amount of ethanol and then dilute this wayyyyy down with sterile saline? I have no experience with this, but I seem to recall that while concentrated ethanol is quite dangerous to inject, if it's sufficiently diluted, then it is relatively safe. Am I right in this assumption, and if so, what concentration of ethanol would be considered safe to use In this manner?
 
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Apologies for responding to my own thread, but I had a thought regarding a potential alternative ROA from what I was getting at above, but in order for it to be viable, I would need to confirm at amfonelic acid is readily soluble in propylene glycol.

My thought involves dissolving the amfonelic acid in propylene glycol (glycerin would work as well), filling an e-cig tank with the solution, and then using the bottom half of the e-cig to atomize the solution, thus effectively creating a vaporizable form of amfonelic acid.

However, again the success of this depends entirely on whether amfonelic acid is readily soluble in propylene glycol or glycerin.

So does anyone here know if this substance should be soluble in prop glycol or glycerin?

If it is not, I would love to hear any other ideas that would lend themselves to permitting ROA for amfonelic acid other than oral, nasal or plugging.

Would simply vaping off of tin foil work?

Thanks guys-and I would still love to hear other's experiences w amfonelic acid- very promising substance IMO.
 
romealone said:
Apologies for responding to my own thread, but I had a thought regarding a potential alternative ROA from what I was getting at above, but in order for it to be viable, I would need to confirm at amfonelic acid is readily soluble in propylene glycol.

My thought involves dissolving the amfonelic acid in propylene glycol (glycerin would work as well), filling an e-cig tank with the solution, and then using the bottom half of the e-cig to atomize the solution, thus effectively creating a vaporizable form of amfonelic acid.

However, again the success of this depends entirely on whether amfonelic acid is readily soluble in propylene glycol or glycerin.

So does anyone here know if this substance should be soluble in prop glycol or glycerin?

If it is not, I would love to hear any other ideas that would lend themselves to permitting ROA for amfonelic acid other than oral, nasal or plugging.

Would simply vaping off of tin foil work?

Thanks guys-and I would still love to hear other's experiences w amfonelic acid- very promising substance IMO.
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You also need to consider the temperature that amfonelic acid will break down compared to the vaporisation temperature of propylene glycol.
 
Soo what is this drug anyways? Can someone describe its structure and mode of action? I would appreciate it. This is something I have not heard of and I'm guessing it's some highly dopaminergic stimulant RC?
 
Still one of the most bizarre drugs, IMO -- a stimulant that's an antibiotic.8) If this drug is actually any good, I'd have to say the biggest downsides is that fact that its an antibiotic.

I'm even more intrigued since it has little to no actions on nor-epinephrine.
 
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I don't think it's an empathogen just because there's an alpha-methylphenylalanine residue in it.
 
I beleive he is referring to his post on that thread he linked to. Just throw a methylenedioxy on it and you got a empathogen.... Which as we know with mdpv, mdpvp, and various other MD-compounds not related to mdma, mda, or their beta ketone derivatives or mda analogues ( i.e., the apbs), that adding a methylenedioxy ring does not automatically mean it is a serotonin releaser. I assume he was joking i don't know for sure. Maybe he said it with tongue in cheek? ? idk
 
Hey guys

Still hoping for some suggestions regarding a suitable solvent that would allow for safe IV usage (if one were so inclined). I can't find much info on its solubility in various solvents, and what little I have found is often conflicting (for instance one source states it's readily soluble in ethanol, another says sparingly).

Also curious about whether this substance would lend itself to effective vaping.
 
why would you IV, is it slow to act weak stimulant in general or what? perhaps orally it doesnt give the same buzz? but i heard its pretty powerful stimulant that last 12 hours or so, is it really a good idea to IV something like that?
 
asecin said:
why would you IV, is it slow to act weak stimulant in general or what? perhaps orally it doesnt give the same buzz? but i heard its pretty powerful stimulant that last 12 hours or so, is it really a good idea to IV something like that?
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Yes it is very slow to act. Most report about an hr before any effects are achieved and 2-3 hrs until it reaches max concentration. Also, I am really just looking for information about solubility and an appropriate solvent. Volumetric dosing is always a better and safer option, esp when dealing with something that has been reported active at <10mg. Unless you have a true lab grade scale, your standard home electronic scale is not very accurate at measuring weights that low. Much easier/safer to weigh out 100mg, for example, mix with appropriate solvent, 10ml for example, and have a homogenous stock solution of approx. 10mg/ml. Of course this only works if you find a solvent in which the solute is readily soluble.

As per your question about whether it's safe to IV a stim that is reported to last 12 hrs...well that's a tricky question. I suppose technically it's not "safe" to IV anything as there are inherent risks such as infection that come with this ROA, but I don't see how it's duration makes it any more or less safe, Meth has a similar duration and that is used IV all the time.

I do know that when testing this chemical, researchers apparently had quite a bit of difficulty finding a lethal dose when administered to rats. It ended up being an insane dose (as in >1000mg/kg). While than doesn't prove it would be similarly safe in humans, it certainly makes me feel better than seeing rats dropped off at .5mg/kg. My guess is the very high LD50 is due to the fact that amfonelic acid has no effect on norepinephrine, being extremely selective for DAT, so you get very minimal PNS effects (vasoconstriction, tachycardia, etc).


I'm still hoping someone in this sub-forum has knowledge of a solvent that this would be readily soluble in, and esp interested in one which could be (relatively) safe for IV purposes. I can't find any info on its solubility in propylene glycol or PEG, and am wondering if this may be a candidate. I'm also happy to hear any speculation on what anyone might infer would be a suitable solvent, based on its amfonelic acid's structure.

https://www.google.com/url?sa=i&rct...5S2FvSctSADNZJYf7_Dc5JVQ&ust=1425842042994713
 
Hey guys,

I'm happy to have this thread closed if there is no interest in further discussion.

However, before closing it, I would truly appreciate any answers or speculation regarding my initial question which is bolded in the above post. I'm hoping someone can help with suggesting a solvent that would be appropriate to make a solution with amfonelic acid. Any solvent in which amfonelic acid is readily soluble would do, though ideally it would be one suitable for safe injection (0.2 micron filters would be used). All I've come up with is an aqueous NaOH solution, however even with that it lists only 9mg/ml and I'm not thrilled with the Idea of using NaOH as it has to be very carefully diluted to make a safe(ish) solution.
Any thoughts on propylene glycol? Thanks again.
 
I think you'd have to experiment and see. Predicting solubilities of compounds in arbitrary solvents can be tricky. More importantly, amfonelic acid is not a commonly come by chemical... there's few enough people that have access to the compound, and I'd imagine most of them are researchers who don't want to IV it.

Injecting glycols or ethanol can be done but is a massive vein irritant. Before the development of midazolam, diazepam was delivered in PG/ethanol mixture for slow IV injection.

I still think the best idea is dissolving it in a mild base like bicarbonate.
 
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romealone said:
I do know that when testing this chemical, researchers apparently had quite a bit of difficulty finding a lethal dose when administered to rats. It ended up being an insane dose (as in >1000mg/kg). While than doesn't prove it would be similarly safe in humans, it certainly makes me feel better than seeing rats dropped off at .5mg/kg. My guess is the very high LD50 is due to the fact that amfonelic acid has no effect on norepinephrine, being extremely selective for DAT, so you get very minimal PNS effects (vasoconstriction, tachycardia, etc).
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You have to take into account species scaling when you compare doses in rats and humans. Although drug dosing is usually based on mass, it should really be based on surface area. In humans the approximation of mg/kg is fairly accurate, but there are huge differences in the surface areas of rats and humans so the approximation breaks down. You can find species scaling calculators on the web that will allow you to convert doses.

This doesn't always work, however, because there can be species differences in sensitivity to a pharmacological mechanism. For example, some rodents are insensitive to MPTP. The calculations will show what doses should yield equivalent blood levels, but you can't necessarily assume that something like binding affinity will be identical in different species.
 
I've been intrigued by this substance lately, I'd love to hear your report on it's effects! I'm not sure if I'll give it a go or not.
 
I was thinking...the first thing i ever IV'd was vodka, when i was a kid. Would amfonelic acid dissolve in vodka? Is this a stupid idea? I snorted between 8 and 12mg and I am not feeling anything special. Sublingual route didn't produce any effects either. From here I can only go higher on the dose, inssuflated. But if it could be injected I would like to try it.
 
Remember this stuff apparently lacks peripheral effects, so you might not technically "feel" much at all, you might have to look for other changes that aren't immediately obvious.
 
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