Misc Flouro-phenibuts now ~2 year use equates to or exceeds some 'normal' clinical trials?

[Deioflaje]

The topic length on this forum is so stingy

I have hesitated trying it due to it's untested nature but if it otherwise sounds right up your alley in terms of effects don't you have to at some point say nothing ventured nothing gained?

F-phenibut has been used now for 2 years or more quite regularly and no untoward complaints from people so far so that ever growing body of usage history must be more than comparable to average clinical trials of normal drug approval. I know it hasn't been studied scientifically at all but still it is worth something right to say there have been no unexpected complaints so far?

I am really not interested in trying original phenibut due to its purported long duration and crash/higher dependency but the effect profile of the F version sounds just about right.

 

[Scrofula]

I believe chloro-phenibut is in fact just baclofen, right?

Checking and . . . indeed it is. The difference between 4-F-phenylGABA and 4-Cl-phenylGABA, is probably as close to nothing as you could get. Fluorine is half the weight of chlorine, and even more electronegative, but it's not exactly pulling any density off some functional group.

Usually those halogens get stuck onto pharmaceuticals to make them more fat-loving and sneak into brain crevices and things, thus increasing potency. That night explain the 10x difference between phenibut and baclofen (there's no other difference anyway), but sometimes an added F will make you excrete the drug faster.


Potency is why side effects might seem more severe with phenibut, since you take 10x the dose, you're also taking 10x the side effects.

Personally I'd prefer the one approved for sale here in the US, with a chlorine atom.

 

[Hodor]

F-phenibut has been used now for 2 years or more quite regularly and no untoward complaints from people so far so that ever growing body of usage history must be more than comparable to average clinical trials of normal drug approval.

I think you're *seriously* underestimating the complexicity of clinical trials.

When you're participating in a clinical trial, you're going to be filling out regular reports, and doing regular check-ups (as in blood work, electrocardiograms, etc.).

When people find out about RC-related toxicity, it's usually because of acute and severe symptoms like people getting Parkinson's from bad MPPP, having their hair fall out after taking MT-45, or dying by the dozens from 4,4'-DMAR.

Many forms of toxicity only become apparent after chronic exposure, and indeed some of them aren't even noticed during clinical trials - just think about how long it took for "ketamine bladder syndrome" to become a recognized medical condition, in spite of ketamine abuse being extremely widespread since the late 90s. I am also pretty sure that Wyeth - a huge pharm company with extensive testing capabilities at its disposal - would have preferred to detect fenfluramine's high cardiotoxicity during the clinical trials, instead of losing over 20 billion dollars to settle a class action lawsuit when Fen-Phen gave thousands of patients cardiac valvulopathy.

That said... in general, substituting a para-fluoro-atom on a phenyl ring tends to be one of the "safer" modifications to make, on account of fluorine being a relatively small atom that forms extremely tough bonds with carbon.

 

[Hodor]

HOWEVER, as Scrofula already pointed out, fluoro-phenibut is closely related to baclofen as well; indeed, baclofen is just "chloro-phenibut", if you will.

While phenibut (and other related "gabapentinoid" drugs, for example pregabalin and gabapentin itself) have a fairly multi-faceted pharmacology, baclofen is so potent as a GABA-B agonist that - at clinically relevant doses (~20mg, i.e. about 1/10th of a normal dose of phenibut) - all other effects are negligible.

And with fluoro-phenibut supposedly still being about 5 times as potent as regular phenibut, it stands to reason that its pharmacology is indeed closer to that of baclofen.

 

[Volsam]

F-Phenibut feels very different from Baclofen IME. Baclofen has no pleasant effects to offer except muscle relaxing, where F-Phenibut feels pretty addictive, euphoria inducing and quite moreish.

I have very low GABA tolerance so 500mg of Phenibut feels pretty strong for me. 150mg of F-Phenibut feels even stronger but with far less dizziness or body discomfort.

The only immediate issue I have with F-Phenibut is nausea - it can be very strong and debilitating, comes in characteristic waves and sometimes I dont get it at all and sometimes it can be pretty bad. It feels similar to Mescaline nausea, which is serotonin induced (5HT-3 as I remember), I speculate that F-Phenibut might have some indirect (or direct?) action on serotonin, which might explain it's pronounced entactogenic effects. I will try low dose Ondansetron with it and see if it mitigates it effectively.

The entactogenic effects noticed with F-Phenibut are a lot stronger and quicker than with Phenibut. Baclofen does not cause anything like that at all for me.

F-Phenibut feels too good and very easy to get hooked on, so I'd be very careful with it if you have a history of alcohol, benzo or opioid addiction.

Be safe!

 

[Scrofula]

Well that sounds like expectations, with the fluorinated baclofen in the middle:

[TABLE="width: 500"]
[TR]
[TD][/TD]
[TD]4H-Phenibut[/TD]
[TD]4Cl-Phenibut[/TD]
[TD]4F-Phenibut[/TD]
[/TR]
[TR]
[TD]Relative strength[/TD]
[TD]100[/TD]
[TD]10[/TD]
[TD]30[/TD]
[/TR]
[TR]
[TD](Volsam units)[/TD]
[TD][/TD]
[TD][/TD]
[TD][/TD]
[/TR]
[/TABLE]

I'm pretty sure these are all excreted unmetabolized. It would be pretty amazing if they managed new brain targets somehow.

 

[uncouplingreversed]

The topic length on this forum is so stingy

I have hesitated trying it due to it's untested nature but if it otherwise sounds right up your alley in terms of effects don't you have to at some point say nothing ventured nothing gained?

F-phenibut has been used now for 2 years or more quite regularly and no untoward complaints from people so far so that ever growing body of usage history must be more than comparable to average clinical trials of normal drug approval. I know it hasn't been studied scientifically at all but still it is worth something right to say there have been no unexpected complaints so far?

I am really not interested in trying original phenibut due to its purported long duration and crash/higher dependency but the effect profile of the F version sounds just about right.

Side effects appear to be somewhat dose related as upwards of 750 mg didn't show any concerning side effects or addiction in studies but overdosing does. I think before you try a newer less researched RC trying Phenibut would be a smart baseline to see how you respond.

You could also consider HomoTaurine which is a GABA B partial agonist in lower doses and antagonist in higher so it upregs your receptors.

 

[Scrofula]

Caution again, PM en route.

Homo-Taurine, aka tramiprosate, non-acetyl version of acomprosate, and a bit long otherwise the active ingredient in CLR, enemy of limescale and soapscum, required nutrient for cats and scam ingredient in energy drinks, derivative of plain old cysteine.

It's a weak partial agonist of both GABA-A and GABA-B. It is not something you want if you were looking for a replacement for phenibut or baclofen or 4F-phenibut, gabapentin, pregabalin or benzos, all of which are usually taken not for the GABA-B effects.

Like telling an opioid fan looking to try the latest RC-opioid that he should really look into buprenorphine.

 

[Limpet_Chicken]

Any opioid fan ought to avoid anything with that N-cyclopropylmethyl group. Its the hallmark of a partial agonist or mixed agonist-antagonist.

 

[Scrofula]

You mean an epoxide?

OK, no, epoxides are ethers. That's why I never understood how those drugs weren't hyper-reactive.

And you know what, holy shit and on topic too, look at this fantastic chart of cylcopropyl containing drugs, especially the clear next-gen gabapentinoid but labelled a triple reuptake inhibitor (so it'll never get marketed) from glaxosmithkline: 1360707F.

 

[uncouplingreversed]

Caution again, PM en route.

Homo-Taurine, aka tramiprosate, non-acetyl version of acomprosate, and a bit long otherwise the active ingredient in CLR, enemy of limescale and soapscum, required nutrient for cats and scam ingredient in energy drinks, derivative of plain old cysteine.

It's a weak partial agonist of both GABA-A and GABA-B. It is not something you want if you were looking for a replacement for phenibut or baclofen or 4F-phenibut, gabapentin, pregabalin or benzos, all of which are usually taken not for the GABA-B effects.

Like telling an opioid fan looking to try the latest RC-opioid that he should really look into buprenorphine.

HomoTaurine is a GABA A agonist which may have anti-anxiety effects AND it acts as a GABA-B partial agonist in LOW doses while in HIGHER doses it acts as a GABA-B Antagonist which can enhance or upreg your receptors, which is something you want for especially after downreg your receptors after phenibut or baclofen use. Which would you have more active receptors of GABA-B on your own or to taking an agonist that downregs you? I mean best of both worlds you cycle an antagonist with an agonist to reduce tolerance and withdrawals if done right but it's a tightrope.

Sure if you want a Gabergic go with a straight up benzo or why not even Tolibut.

 

[Scrofula]

No, hon, drugs don't change function depending on dosage. What you mean is a ceiling effect. Once you saturate the receptor with your barely active ligand, you can't get any more signal out, so maybe you can't get any higher; it does not mean that the drug changes the way it interacts with anything.

It is a shitty GABA-A drug as well, and if it was really a GABA-A agonist, and not a modulator like the benzos, it would be illegal, like muscimol.

If you have an agonist plugged into your receptors in enormous excess, and they are activating it, just not very well, how would that possibly ever result in lowered tolerance? It could be worse, lots of tolerance, and no response even compared to where you were. Tolerance has different mechanisms for different drug classes anyway, your coupled G-proteins from opioids do not apply in the benzo case.

Hence, a detox drug, when conditions are right, and not something you want for benzos.

Flumazenil WILL PRECIPITATE WITHDRAWAL in benzo dependents. Another word for that is seizures.

 

[Scrofula]

Interesting. Tolibut, like toluene. Basically the 4-me version. Probably still not a gabaergic. Probably less potent than baclofen still.

 

[Limpet_Chicken]

Wikipedia lists affinity for GABAb for fluorobaclofen as 1.70uM, and states stronger as a GABAb agonist than phenibut but less so than baclofen. Wonder if it has affinity either for GHB receptors or for alpha2delta, of either type 1 or type 2 alpha2delta VGCCs

Wonder what the trend would be in the case of bromo or iodo, at least in vitro against these targets.
Wouldn't want to take the iodinated one, too good a leaving group, but I'd test bromobaclofen, a couple of times, since its not likely to be worse than taste-testing bromethiazole (chlormethiazole analog with Br in place of Cl)

 

[Scrofula]

I know that baclofen and phenibut-unadorned are both calcium channel ligands, and I'll make a statistics game indicator of intent to participate, as analogy, that 90% of what brings people back is some nice gabapentinenoid persepective.

It is where a few hundred million R&D dollars were focused. Not even the Russians wanted to develop phenibut further.

And I took another look at the GSK drug in the poster and it's actually a pretty clear tropane alkaloid, as in, cocaine. But if you pretend a methyl is an oxygen, and forget all the chemistry you ever knew, it totally works.

 

[Mycophile]

I don't understand the scientific discussion, but I really enjoy F-Phenibut and have experimented with it a lot at different doses lately with zero dependency and I like it better than regular Phenibut.

I've talked more about it in other threads on here.

 

[Limpet_Chicken]

I don't know about 'even the russians'. They seem to have rather open minds when it comes to novel nootropics, unusual stimulants and the like (I mean really, structures of some russki stuff are plain fucking weird, like mebicar for instance comes to mind. Funky looking molecule or what?)

Inventive lot thats for sure.

 

[Scrofula]

Well, this mebicar at least resembles a cyclic piracetam. Have you tried following any of the wikipedia references through the Russian English, though?

Mkrtchian, VR; Kozhokova, LZ (2012). "Adaptol--verges of possible". Likars'ka sprava / Ministerstvo okhorony zdorov'ia Ukrainy (5): 125–33.


My possible has been stuck on the verge for about eight years now.

 

[Scrofula]

Because I'm an asshole, I'm going to include my pretty picture here. OP was actually quite reasonable a few posts up, and I have no argument with his position. For fairness, I'm gonna include the picture in the far less equitable naysayer thread too.

I'd like the learned women and RC expert-men in the crowd to look at this lineup and tell me--cause I'm still the kind of person who thinks the numbers are pretty important, proving my ignorance--which one gained incredible new abilities for its class, from a slight substitution (antagonists at the same receptor don't count):

If you guessed the little F at the bottom of the one in the middle, you win! A whole new entactogen/convulsant/euphoriant/mass-murderer, with the widest therapeutic/ toxic-at-all- range of any med.

Or just a slight weaker baclofen/ much stronger phenibut.

 

[yteek]

On the topic of phenibut/analogous, this drug/class came in with the worst shit storm of problematic marketing from being a body building supplement, a nootropic/ a nutrient for the brain, and it undermined the serious of it. Phenibut is extremely unpredictable with some individuals, it to be presented as a supplement for self improvement, undermined that this a serious drug, with potential serious consequences, many we don't have a full grasp of the potential this drug has to wreak havoc on the mind, body, and spirt. It really is a drug with little understanding behind it, I dare call it an RC.I rationalized with " oh it is prescribed in Russia, and the Russian Astronauts used it for space anxiety, but now clearer head prevails, it is Russia.

I feel like phenibut worsened my neurolgoical health for sure.


You could probably mass market this in the same fashion kratom has been done, and all that K2 bullshit, and I think it could catch on as next best thing. It could gross large sums of money if it was mass marketed, the same that happened with the Kratom craze, but I would not be one to want to deal with that liability. I could see it being a craze to come about if it was stocked in every local head shop, with the same cray presentations of kratom with names like OPMS and just crazy shit and it would ultimately get banned.