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Diamant - Liquid Adamantane For R&D

Discussion in 'IdeaLabs' started by haidut, Mar 15, 2017.

  1. haidut

    haidut Member

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    I first became interested in adamantane when I read about it in one of ray's articles. According to Ray it seems to have a stabilizing and structurally protective effects on the water inside the cell, and its commercial derivatives are all know to be anti-excitotoxic.
    The problem of Alzheimer's disease as a clue to immortality Part 1
    "...Things that act directly on the water structure: I think all of the natural regulators have an effect on the structure of water, but some unusual substances seem to act primarily on the water. Noble gases, for example, have no chemical effects, but they tend to form "cages" of water molecules around themselves. Camphor, adamantane, and the antiviral drug amantadine, probably have a similar water-structuring effect, and amantadine, which is widely used as a therapy in Parkinson's disease, has an anti-excitotoxic action."

    Adamantane is the simplest known diamondoid existing naturally. As the Wikipedia page states, it is the core structure of many antiviral, anti-parkinson, and even anti-diabetic drugs.
    Adamantane - Wikipedia
    "...All medical applications known so far involve not pure adamantane, but its derivatives. The first adamantane derivative used as a drug was amantadine – first (1967) as an antiviral drug against various strains of flu[50] and then to treat Parkinson's disease.[51][52] Other drugs among adamantane derivatives include adapalene, adapromine, amantadine, bromantane, carmantadine, chlodantane, dopamantine, memantine, rimantadine, saxagliptin, tromantadine, and vildagliptin. Polymers of adamantane have been patented as antiviral agents against HIV."

    After digging further I discovered many additional properties that make adamantane quite an interesting substance. Those studies are mostly on adamantane derivatives but as you can see from the pictures on Wkipedia, these derivatives are most often nothing more than an addition of a simple group that makes the adamantane more water-soluble. Adamantane itself is extremely lipophilic and this probably accounts for many of its cell stabilizing effects. Many of the studies on those derivatives compared effects of adamantane to the new derivative and found them to be almost the same. As is often the case in drug discovery and design, a generic molecule like adamantane is modified to be patentable and profitable, but the original molecule usually has the same beneficial effects as the patentable derivative and often without the side effects. The same seems to be true of adamantane.
    In summary, based on extensive research and clinical testing adamantane and its derivatives so far seem to possess the following properties: HDAC inhibitor (and thus anti-cancer), anti-cortisol, anti-serotonin, pro-dopamine, anti-diabetes, anti-viral, anti-bacterial, anti-excitotoxic, NMDA antagonism (and thus antidepressant), anticholinergic, antihistamine, etc. In addition, due to it extreme lipophilicity, admamantane can enhance the absorption and effects of many other substances it is administered with including steroids, vitamins, minerals, anti-inflammatory drugs, anesthetics, etc.

    In light of all of these properties, I decided to release the product Diamant, which contains pure admantane dissolved in tocopherols and MCT oil. The studies supporting the properties of adamantane described above are provided in the references section below. The list of studies is a little light because I wanted to post only the studies known to be directly relevant to adamantane and not its derivatives. There over 5,000 studies on all adamantane derivatives and as I go through them slowly I will update the references section accordingly.
    I think the combination of lowering serotonin, lowering cortisol, increasing dopamine synthesis while also acting like a dopamine agonist, lowering systemic inflammation and anti-viral / anti-bacterial effects makes adamantane one of the most versatile and systemically relevant chemicals in Peat-land.


    *******************************************************************************
    Diamant is a liquid product containing the chemical adamantane. Derivatives of adamantane have been in clinical use for decades are known for their anti-viral, anti-bacterial, pro-dopamine, and anti-excitotoxic properties. More recent studies have discovered that adamantane and its derivatives are one of the most powerful inhibitors of HDAC (in nanomolar concentrations: EC50 = ~70 nM/L) known to man. Also, admantane (and its derivatives) is one of the few known direct stimulators of the enzyme tyrosine hydroxylase and thus a direct stimulator of endogenous dopamine synthesis. In addition, adamantane and its derivatives have been shown to inhibit cortisol synthesis, lower plasma serotonin, histamine, blood glucose, insulin, and inflammatory biomarkers. The extreme lipophilicity of adamantane has led to its use as an absorption enhancer for various drugs delivered topically, orally or even IV and this lipophilicity seems to also dramatically enhance the half-life of the chemical administered together with adamantane. For example, several derivatives of aspirin, indomethacin and testosterone have been synthesized using adamantane as the modifier and the bioavailability and half life increases from a few hours to as long as 8 weeks (i.e. see the liphophilicity links in the references below; the steroid Bolmantalate is a direct example Bolmantalate - Wikipedia). Given these properties, admantane may contribute to more optimal physiological balance and oxidative metabolism.

    Units per container: about 30
    Unit size: 20 drops
    Each unit contains the following ingredients:

    Adamantane: 33mg

    Other ingredients: tocopherols, MCT
    *******************************************************************************

    References:


    1. Anti-cortisol
    Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation. - PubMed - NCBI
    Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors. - PubMed - NCBI
    Novel 11β-HSD1 inhibitors: C-1 versus C-2 substitution and effect of the introduction of an oxygen atom in the adamantane scaffold. - PubMed - NCBI

    2. HDAC inhibitor
    Discovery of adamantane based highly potent HDAC inhibitors. - PubMed - NCBI

    3. Anti-serotonin, lower blood glucose, lower insulin
    Amantadine reduces glucagon and enhances insulin secretion throughout the oral glucose tolerance test: central plus peripheral nervous system mechanisms

    4. Dopamine agonist and increased dopamine synthesis
    Memantine agonist action at dopamine D2High receptors. - PubMed - NCBI
    The effects of ladasten on dopaminergic neurotransmission and hippocampal synaptic plasticity in rats. - PubMed - NCBI
    [Ladasten induces the expression of genes regulating dopamine biosynthesis in various structures of rat brain]. - PubMed - NCBI
    [Cytosine demethylation in the tyrosine hydroxylase gene promoter in the hypothalamus cells of the rat brain under the action of an aminoadamantane... - PubMed - NCBI
    https://link.springer.com/article/10.1007/s10628-005-0057-z

    5. Lipophilicity, enhancement of absorption, half-life and effects
    The Lipophilic Bullet Hits the Targets: Medicinal Chemistry of Adamantane Derivatives
    http://pubs.acs.org/doi/abs/10.1021/jm00329a007
     
  2. ThinkPerceive

    ThinkPerceive Member

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    Thanks! Now I know what's in that bottle I already got :)

    My primary interest and enthusiasm for this product is based on its potential properties around ADHD and ADD*. It turns out that one of those derivatives - Bromantane - is often used for that purpose. Do you have any thoughts on Adamantane for ADD/ADHD, and how it "compares and contrasts" to Bromantane?

    *This would be for me - it's been a serious and lifelong problem around attention, focus, motivation and "sticktoitiveness" - and nothing "Peaty" has yet touched it.
     
  3. Pointless

    Pointless Member

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    Here's a study about adamantane derivatives and blocking the p2x7 receptor, which blocks inflammatory interleukin-1beta and tnf-alpha. If adamantane has this effect, it could be an anti-inflammatory against arthritis and crohn's disease.

    Edit whoops forgot to post the study Selective P2X7 receptor antagonists for chronic inflammation and pain

    I'm curious why you chose the dose/concentration of 33 mg per 20 drops? Is there any research on the dose?

    Can it increase athletic performance like other electron acceptors like memantine or c60-oo?
     
  4. johnwester130

    johnwester130 Member

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    is this similar to cyproheptadine ?
     
  5. encerent

    encerent Member

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    Is that little quote the only thing Peat's ever said about adamantane?
     
  6. BigYellowLemon

    BigYellowLemon Member

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    I had no idea about adamantane esters.

    Amazing.
     
  7. dilantinoid

    dilantinoid Member

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    Memantine is usually titraed when started AFAIK, will this also need to be the case with Diamant?

    and would you consider this product identitical to Memantine in terms of its effects; considering the absence of the additonal chemical group and its liquid (no excipient) nature?
     
  8. haidut

    haidut Member

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    Great, thanks for the tip. In the next few days I will research more on the derivatives and post additional studies if I think it applied to adamantane. It should apply as if you look at bromantane, memantine, rimantadine and amantadine they are just adamantane with a single extra amino group, which makes it a bit more water soluble. It does not change its properties and the studies I posted so far did compare adamantane to its derivatives and found the same effects.
    The dose was chosen since the effects of adamantane to me are very similar to memantine. I have tried both and cannot feel much different except that regular adamantane is much longer acting. The common daily memantine dose is 30mg, so I chose 33mg to approximate that and also because it would make bottling easier since each bottle will hold 1g of adamantane.
    Btw, speaking of P2X7 antagonists the active form of vitamin B6 known as pyridoxal-5-phosphate is a potent antagonist on all PYX receptors, and I think there are even studied with it for Chrons and colitis.
     
  9. haidut

    haidut Member

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    I think it may help. To me adamantane works very similarly to memantine and they both have strong dopaminergic properties.
     
  10. haidut

    haidut Member

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    Nope, not at all. It is not a serotonin receptor antagonist. It may be a dopamine agonist but its bigger role is as a promoter of dopamien synthesis, antagonist of NMDA and inhibition of cortisol synthesis.
    Actually, a small clarification. It may have antagonism effects on 5-HT3, so could be similar to ondansetron and thus help with digestive issues.
    Memantine - Wikipedia
    "..Memantine acts as a non-competitive antagonist at the 5-HT3 receptor, with a potency similar to that for the NMDA receptor.[35] The clinical significance of this serotonergic activity in the treatment of Alzheimer's disease is unknown."
     
  11. encerent

    encerent Member

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    Everything of yours opposes cortisol. Which ones are most effective?
     
  12. haidut

    haidut Member

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    Yes, as far as I know. Why do you need more quotes from Peat? He mentioned only once things like uridine, camphor, DHT, etc and they are all quite beneficial and he has spoken favorably of them when asked. There is a ton of evidence on the adamantane derivatives going back 50 years and most of the work was done in Soviet Block so there was not much commercial motive to tout their benefits, which means the findings are probably legit.
     
  13. Makrosky

    Makrosky Member

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    It sounds amazing @haidut! Thanks! Care to comment the subjective feeling you experience on it? Well... yours and your betatesters team.

    Does it feel similar to another idealabs product so we can get an idea?

    Thanks again!
     
  14. haidut

    haidut Member

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    Lapodin is probably the most potent as it contains emodin and it inhibits 11b-HSD1 in nanomolar concentrations. Adamantane inhibits 11b-HSD1 in low micromolar concentrations but it also lowers serotonin and increases dopamine, which also drives cortisol lower. So, it's hard to say which one has a more potent overall effect on cortisol. Progesterone, DHEA, 11-keto DHT, cyproheptadine, metergoline, etc are all quite potent as well. I don't release supplements that specifically target cortisol. The lowering if cortisol is more of a symptom of systemic benefit and all of our supplements have systemic beneficial effects.
     
  15. haidut

    haidut Member

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    If you have tried memantine, it feels very similar but adamantane lasts much longer. The effects are a very relaxed feeling and ability to focus during the day. Makes me very calm too, to the point of annoying people around me with how little I get disturbed by situations that drive others nuts. So, not sure if that last part if very good if you work/live around stressed people :)
    It makes me hungry too, so it probably lower blood sugar, which is expected given its cortisol and serotonin inhibition.
     
  16. Makrosky

    Makrosky Member

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    I never tried memantine, in my country I think you can't even get it with a script from your regular GP, only one from a hospital. It looks like serious stuff.

    Do you think it can have lasting modifications on neurons like lisuride ? I'm thinking about DAWS and stuff like that.
     
  17. Makrosky

    Makrosky Member

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    LOL! Reminds me about people experiences on the androsterone threads.
     
  18. haidut

    haidut Member

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    I don't think it has the same side effects as dopamine agonists. This is why the derivatives are used as long term treatment for Parkinson - it stimulates endogenous dopamine synthesis instead of activating dopaminergic neurons. In combination with a little tyrosine/BCAA this can be quite a nootropic tool for the people interested in experimenting. I think it may help quite a bit with sugar control issues. After all, it was originally developed and proven to work as antidiabetic drug.
    Memantine - Wikipedia
    "...Memantine
    is the first in a novel class of Alzheimer's disease medications acting on the glutamatergic system by blocking NMDA receptors. It was first synthesized by Eli Lilly and Company in 1968 as a potential agent to treat diabetes; the NMDA activity was discovered in the 1980s."
     
  19. Dan Wich

    Dan Wich Member

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  20. chimdp

    chimdp Member

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    Looking forward to trying it! @haidut Have you dosed this to your rats orally as well as topically? Is this something that would need to be taken near the full dose for rats to feel the effects or have there been observation of effects at lower doses?
     
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