Where Can I Buy Pure Fladrafinil?

I have been following the bullet proof diet, most religiously the bullet proof coffee, but this got me curious about what else  I can do to try and improve my brain, I have been experimenting a with a few nootropics, I tried modafinil based on Dave's recommendation, however I am looking for a legal alternative I can buy in the UK, this led me to Fladrafinil.


 


The only problem is where can I buy it 100% pure, with proof of this?


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  • Fladrafinil is a good replacment for modafinil, as its stronger, cheaper and legal.


     


    If you want it in pure form you are going to have to buy it in pure powder form, and dose it yourself.


     


    The only 100% pure powdered Fladrafinil I could find is here:


    https://www.nootropics.co.uk/product/fladrafinil/


     


    You will see under the analysis tab there is a certificate saying it is 100% pure.


  • BrainSpankingNewsBrainSpankingNews Vitimus Maximus ✭✭

    Based on this, I'm not sure this is a good alternative. It suggests it contains fluoride. You don't want fluoride:


    "CRL-40, 941 is a white crystalline solid substance that has been described as closely related to both adrafinil and modafinil. It was developed by the French pharmaceutical company Lafon Laboratories as a new research chemical. CRL-40, 941 is known for its other names fluorafinil, fladrafinil and its chemical name 2-{[Bis(4-fluorophenyl)methyl]sulfinyl}-N-hydroxyacetamide[1]."



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  • sparefilmssparefilms Post-human Construct ✭✭✭


    Based on this, I'm not sure this is a good alternative. It suggests it contains fluoride. You don't want fluoride:


    "CRL-40, 941 is a white crystalline solid substance that has been described as closely related to both adrafinil and modafinil. It was developed by the French pharmaceutical company Lafon Laboratories as a new research chemical. CRL-40, 941 is known for its other names fluorafinil, fladrafinil and its chemical name 2-{[Bis(4-fluorophenyl)methyl]sulfinyl}-N-hydroxyacetamide[1]."




    Please, explain how the bis(p-fluoro) ring in fluorafinil can be harmful and is something you do not want?


     


    Also, could you explain the similarities and differences between the bis(p-fluoro) ring in fladrafinil/fluorafinil and fluorine, fluoride, sodium fluoride, and hydrogen fluoride, which of these we should not want, why we should not want them, and which dosages they are harmful at?

  • BrainSpankingNewsBrainSpankingNews Vitimus Maximus ✭✭
    Nope, I can't explain that. Definitely not my expertise. I just tend to avoid anything starting with "fluor". ;)


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  • Florine has the same electrical charge as chlorine, bromine, and iodine.  The chemical reactions in our bodies are performed based largely on chemical charge molecular shape.  This is why sodium fluoride is particularly problematic, because when compared to sodium chloride (table salt) fluorine has the same charge as chlorine and they both have a cubical structure.  The body uses sodium chloride as a mechanism in the cellular hydrogen pump and to make hydrochloric acid.  When fluorine is substituted for chloride in this reaction, hydrofluoric acid is created - which is one of the most noxious chemicals out there.  Sodium fluoride has been added to tap water in the United States and is also used as a drug to treat osteoporosis.  Although the data shows that it is not effective:


     


    https://www.ncbi.nlm.nih.gov/pubmed/11034769


     


    https://www.ncbi.nlm.nih.gov/pubmed/17701094


     


    A similar comparison could be made with every combination of 16 VIA 6A elements with non-metals.  Sodium iodide and sodium fluoride is where the neurotoxicity comes in.


     


    I believe I have addressed fluorine, fluoride, and hydrogen fluoride (hydrofluoric acid), now onto calcium fluoride.  Calcium fluoride is found in fluorite, fluorspar, and other naturally occurring minerals.  It is found in spring water and has biological uses in nature. Over consumption of calcium fluoride can lead to fluorosis.  This is because of the way the body uses calcium chloride in BGLAP gene activation.  Calcium fluoride "looks" and "feels" (pardon my anthropomorphism) the same way to the activators.  Too much of it has a negative impact on bone growth.


     


    Fladrafinil (CRL-40,941)is fluoridated adrafinil.  What are the bio-synthetic implications of this?  To even begin experimental procedures, we would have to understand the metabolism of adrafinil - which we know very little about.  Where is the fluorine dumped?  In the liver?  In the brain?  Who knows?  This is also not a substitute equation like my examples above.  I couldn't even begin to speculate over what this will do.  We could look at other organic similarities, as you have suggested with the bis(p-fluoro) ring and compare it to something like bis (4-chloro-phenyl), but how do we know that the metabolism of fladrafinil will produce bis(p-fluoro)?


     


    Best case scenario: Fladrafinil is metabolized basic reactants to include elemental fluorine.  Elemental fluorine is detoxified through the cytochrome P450 pathway over a period of time that is determined by dose, plasma levels, and body weight.  If you take enough fladrafinil over along enough period of time, it could lead to significant accumulation.  Again, this is highly speculative, but using my critical thinking skills, I think that there is probably less risk with adrafinil and there would have to be massive gains to make up for the risk potential.


     


     




    Please, explain how the bis(p-fluoro) ring in fluorafinil can be harmful and is something you do not want?


     


    Also, could you explain the similarities and differences between the bis(p-fluoro) ring in fladrafinil/fluorafinil and fluorine, fluoride, sodium fluoride, and hydrogen fluoride, which of these we should not want, why we should not want them, and which dosages they are harmful at?



  • sparefilmssparefilms Post-human Construct ✭✭✭
    edited November 2015

    Jason that is an awesome summary! In your best case scenario I wonder what the threshold of accumulation-to-detoxification would be, I have a feeling it would be far above the daily nootropic dosage for an average healthy adult. 


     


    Have you looked at hydrafinil/fluorenol-9 in the same way? From the little look I've given it, rather than being an altered analog of adrafinil or modafinil it has a novel structure and different metabolic pathway. As far as reported effectiveness it is suppose to last ~4 hours per dose, be 1.5x the potency of modafinil, is a research compound rather than a prescription, and cost wise runs slightly cheaper than modafinil if you adjust for the increased number of doses required.


     


    Here's the Wiki bit on it:


    "A study published by chemists working for the biopharmaceutical company Cephalon to develop a successor to the wakefulness-promoting agent (or eugeroic) modafinil reported that fluorenol was 39% more effective than modafinil at keeping mice awake over a 4-hour period.[6] It is a weak dopamine reuptake inhibitor with an IC50 of 9 μM, notably 59% weaker than modafinil (IC50 = 3.70 μM) despite being a stronger wakefulness-promoting agent, potentially making it even less liable for addiction.[7] It also showed no affinity for cytochrome P450 2C19, unlike modafinil."


    https://en.wikipedia.org/wiki/Fluorenol


    http://www.ceretropic.com/buy-hydrafinil/


  • Jason HooperJason Hooper ✭✭✭
    edited November 2015

    It looks like an interesting compound.  The only thing that I can definitively say about it is that it has a very high chance of crossing the blood-brain barrier.  I am not sure why it is being compared to modafinil.  Maybe because it is also a wakefulness-promoting agent?  From a pharmakenetics standpoint, they don't have a lot in common.  At first, I thought it was just marketing, but the study that came to the conclusion that it was more potent than modafanil was funded by Cephalon biopharmaceutical company which is the same company that makes Provigil, so maybe they are researching a better alternative.  I am hesitant to try it because we know even less about fluorenol than we do about modafinil, and we know almost nothing about modafinil.  I'll let you guys play around with it first and see if you develop flippers, or something.  I've got kids now.  I can't take these kinds of risks anymore.


     


    Imagine if fluorenol became a prominent insecticide in the 1940s.  Back then, there was less mono-cropping and farmers didn't loose as many crops to bugs as they do today, even with modern pesticides, so there probably wasn't a market for it, but can you imagine all the nooted up farmers selling their land and becoming entrepreneurs?


  • sparefilmssparefilms Post-human Construct ✭✭✭


    I am not sure why it is being compared to modafinil.  Maybe because it is also a wakefulness-promoting agent?  From a pharmakenetics standpoint, they don't have a lot in common.  At first, I thought it was just marketing, but the study that came to the conclusion that it was more potent than modafanil was funded by Cephalon biopharmaceutical company which is the same company that makes Provigil, so maybe they are researching a better alternative. 




    It is one of the research compounds that was being developed by Cephalon as a next-gen successor to Provigil, which is why they funded the study. From what I understand they abandoned that line of research in favor of other compounds. There is an exhaustive list on longecity detailing the past and current research compounds being investigated, though hydrafinil is the only one that I have seen readily available, being experimented with by nootropic fiends, and anywhere near a reasonable price point.

  • sparefilmssparefilms Post-human Construct ✭✭✭


    Imagine if fluorenol became a prominent insecticide in the 1940s.  Back then, there was less mono-cropping and farmers didn't loose as many crops to bugs as they do today, even with modern pesticides, so there probably wasn't a market for it, but can you imagine all the nooted up farmers selling their land and becoming entrepreneurs?




    That would be at once amazing and terrifying. We would probably never wash our produce, since the residue would be chocked full of noots and friendly bacteria! No supermolds, GMO wouldn't be a dirty word, people in rural areas would be intelligent, isn't that what they call a utopia? Of course, we would either quickly develop farming robots or all die of starvation when the farmers joined the .com bubble and sunk their time into startups so...might be worth it!

  • edited November 2015

    I wouldn't worry overly much about the fluor substitutions. Avoiding halogens isn't a bad rule of thumb, but it doesn't apply across the board. When we're talking halogen substituted hydrocarbons, the main problem is reactivity; halogens make good leaving groups, causing halogenated hydrocarbons to attach themselves easily to endogenous molecules. However, this applies less for the lower molecular weight halogens, with fluor and to a lesser degree chlorine being toxic far less often. Additionally, aromatic rings hold on to their halogen groups much more soundly than do most carbon atoms; the fluor substituted phenyl rings in fladrafinil are the single safest halogen substitution possible, and something medicinal chemists commonly try to add when optimizing a candidate molecule on account of their favorable pharmacological properties.*


     


    True best case scenario is that the molecule is metabolised normally, typically being split into chunks and/or made more water soluble, and the chunks are excreted with the fluor groups still on them without ever engaging in any halogen-typical behavior. I think that would be typical for a fluoridised aromatic ring, but of course, whether  general rules actually apply to a given molecule is always somewhat uncertain.


     


    *Source: Gareth Thomas (2007). Medicinal chemistry, second edition.


  • Why does it become legal in the UK when fluoride is added?


  • I've never heard of this compound... has anyone tried it? I'm in the U.K. too so would welcome an alternative product.


  • I would stick to adrafinil or modafinil.  Adrafinil is harder on the liver, but at least those two have been around since the 1970s/1980s


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