Amentoflavone

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    Amentoflavone


    Amentoflavone

    Mood/CNS effects

    There are a whole host of studies examining the effects of Amentoflavone on various neurological endpoints. Without going into each one individually, research highlights will be presented.
    Amentoflavone interacts with the GABA-A receptor by acting as a negative modulator. This would produce a central stimulant effect by inducing wakefulness/alertness. Amentoflavone uptake into the CNS is limited by P-glycoprotein, an efflux pump that pumps specific compounds back outside of the CNS. There are numerous ways to overcome the P-glycoprotein transporter; a very well-documented one is by consuming grapefruit or its constituents.
    In addition, amentoflavone has demonstrated antidepressant and anxiolytic (anti-anxiety) effects in vivo by interacting with not only the GABA-A receptor, but also the serotonin and alpha-adrenergic receptors. In fact, of all the tested constituents of St. John’s Wort (a known antidepressant/anti-anxiety plant), amentoflavone displayed the strongest anxiolytic activity.

    Summary: CNS stimulant, anxiolytic, anti-depressant

    Sources:
    Determinants of amentoflavone interaction at... [Eur J Pharmacol. 2005] - PubMed - NCBI
    Inhibition of benzodiazepine binding in vitr... [Pharm Acta Helv. 1997] - PubMed - NCBI
    Biflavones from Rhus species with affinity ... [J Ethnopharmacol. 2006] - PubMed - NCBI
    Semisynthetic preparation of amentoflav... [Bioorg Med Chem Lett. 2003] - PubMed - NCBI
    Transport of amentoflavone across the blood-brain... [Planta Med. 2002] - PubMed - NCBI
    Antidepressant and anxiolytic effect... [Pharmacol Biochem Behav. 2012] - PubMed - NCBI
    Review on plants with CNS-effects used in t... [J Ethnopharmacol. 2008] - PubMed - NCBI
    Effects of St. John's wort extract and single con... [Planta Med. 2006] - PubMed - NCBI
    Isolation of amentoflavone from Selaginella rupes... [Planta Med. 1981] - PubMed - NCBI


    Fatty Acid Synthase Inhibition

    Fatty acid synthase, as the name implies, is responsible for the endogenous synthesis of fatty acids in humans. It is currently a drug target for metabolic syndrome. In at least three separate trials, amentoflavone has demonstrated the ability to inhibit fatty acid synthase, and thus fat production.

    Summary: Reduced fatty acid synthesis

    Fatty acid synthase inhibition by amentoflav... [Biol Pharm Bull. 2009] - PubMed - NCBI
    Fatty acid synthase inhibition by amentoflavon... [Phytother Res. 2013] - PubMed - NCBI
    Inhibition of fatty acid synthase by amentoflavon... [Arch Virol. 2012] - PubMed - NCBI



    Phosphodiesterase (PDE) Inhibition

    PDE is the enzyme responsible for breaking down cAMP/cGMP. cAMP/cGMP promote smooth muscle relaxation (vasodilation; this is how PDE5 inhibitors help with erectile dysfunction) and lipolysis. Indeed, Forskolin has documented lipolytic activity by increasing cAMP levels via increased cAMP production. PDE inhibition, as with amentoflavone, hits the opposite side of the coin: reduced cAMP breakdown. By increasing cAMP levels, amentoflavone can synergize with adrenergic agonists (i.e. b-agonists) because second messenger pathways follow the rule of amplification.
    Amentoflavone inhibits a broad array of PDE isoforms, and it is the most potent inhibitor out of all tested flavonoids in Ginkgo biloba. Further, of all tested constituents of Allanblackia monticola, Amentoflavone was the strongest vasodilator, inhibiting norepinephrine-induced vasoconstriction by a whopping 35%.
    Summary: Increased lipolysis (fat loss) and increased vasodilation

    Inhibition of cAMP-phosphodiesterase by biflavone... [J Nat Prod. 1998] - PubMed - NCBI
    Biflavones of Decussocarpus rospigliosii as phosp... [Planta Med. 2007] - PubMed - NCBI
    Inhibition of cGMP-phosphodiesterase-5 by biflavo... [Planta Med. 2006] - PubMed - NCBI
    Antimalarial and vasorelaxant constit... [Ann Trop Med Parasitol. 2007] - PubMed - NCBI
    Vasorelaxation by amentoflavone isolated from Sel... [Planta Med. 2004] - PubMed - NCBI
    Inhibition of human platelet cyclic AMP ph... [Biochem Pharmacol. 1986] - PubMed - NCBI


    Muscular Strength and Endurance

    One well-documented mechanism of increasing exercise performance is vasodilation, which helps supply (oxygen; waste removal) meet the demand of exercising muscle tissue (hypoxia; metabolic waste accumulation). Amentoflavone has a well-documented effect on vasodilation as described above.
    In addition to this, Amentoflavone provides a relatively unique mechanism for increasing power output: increased Ca2+ release from the sarcoplasmic reticulum. By increasing intracellular Ca2+ downstream of the signal for muscle contraction, binding to troponin-C is increased and the force of muscular contraction, on a cell-by-cell basis, also increases.
    Caffeine acts via a similar mechanism to increase strength output, and researchers found that not only does Amentoflavone likely bind to the caffeine-binding site, but it does so with 20 times greater potency than caffeine.

    Summary: Improved strength (Ca2+ release) and improved endurance (vasodilation)
    Properties of amentoflavone, a potent caffei... [Eur J Pharmacol. 1999] - PubMed - NCBI

    Insulin Sensitivity/GDA - PTP1B inhibition

    PTP1B is an enzyme involved in insulin signaling, and inhibition of PTP1B is being investigated as a possible treatment for obesity and diabetes. PTP1B inhibition will chiefly improve insulin sensitivity by augmenting insulin’s actions within the cell at a lower circulating level of insulin. This is a fairly novel approach to improving insulin sensitivity and will continue to be investigated.

    Summary: Improved insulin sensitivity

    Protein tyrosine phosphatase 1B inhibitory a... [Biol Pharm Bull. 2007] - PubMed - NCBI


    Dyslipidemia

    Amentoflavone has been shown in vivo to reduce circulating lipids (LDL/TG), making it of further benefit to obesity/diabetes/metabolic syndrome.

    Summary: Reduced lipids

    Antidyslipidemic and antioxidant activity of t... [Phytomedicine. 2012] - PubMed - NCBI

    Credit and thanks to neuron: http://hightowerpharmacology.blogspo...toflavone.html
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    The above is my own opinion and does not reflect the opinion of PES

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    Thanks for breaking this down Coop! Get my Norcodrene tomorrow...can't wait.
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    Excited to try this out pre-workout now.


    Assuming that taking in EAA's (AminoIV) would somewhat inhibit the fat-loss benefits of this?
    But the energy, focus, and strength boost should still be there?
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    Quote Originally Posted by Driven2lift View Post
    Excited to try this out pre-workout now.


    Assuming that taking in EAA's (AminoIV) would somewhat inhibit the fat-loss benefits of this?
    But the energy, focus, and strength boost should still be there?
    The effects will still be present for amentoflavone
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    Increased Ca2+ release from the sarcoplasmic reticulum


    Hey man, I tried to pm you but your inbox is full so I'll just post it here instead:I have a pretty uniqe goal but I think you would know how to do it. I want to increase Ca2+ release from the sarcoplasmic reticulum as much as possible because this would increase contracts frequency and this would help me incredible a lot especially since I am a sprinter. Bottom line, do you know supplements (other than caffeine since its banned by WADA) that will do this and that I can get a hold of, I can't find a pure source for amentoflavone anywhere. I really need your help, especially since i'm only 18.Thanks a lot in advance man!
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    Any chance AS will make this ingredient a product in the future? I like the ingredient but don't always want to use Uncut and in the future I'm obviously not going to be constantly running Norcodrene.

    In the mean time, I've been using AppNut's other product (non-stim) just so that I can have some amentoflavone in on non-UnCut days but that's not really cost effective.
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    Quote Originally Posted by mr.cooper69 View Post
    Amentoflavone

    Mood/CNS effects

    There are a whole host of studies examining the effects of Amentoflavone on various neurological endpoints. Without going into each one individually, research highlights will be presented.
    Amentoflavone interacts with the GABA-A receptor by acting as a negative modulator. This would produce a central stimulant effect by inducing wakefulness/alertness. Amentoflavone uptake into the CNS is limited by P-glycoprotein, an efflux pump that pumps specific compounds back outside of the CNS. There are numerous ways to overcome the P-glycoprotein transporter; a very well-documented one is by consuming grapefruit or its constituents.
    In addition, amentoflavone has demonstrated antidepressant and anxiolytic (anti-anxiety) effects in vivo by interacting with not only the GABA-A receptor, but also the serotonin and alpha-adrenergic receptors. In fact, of all the tested constituents of St. John's Wort (a known antidepressant/anti-anxiety plant), amentoflavone displayed the strongest anxiolytic activity.

    Summary: CNS stimulant, anxiolytic, anti-depressant

    Sources:
    Determinants of amentoflavone interaction at... [Eur J Pharmacol. 2005] - PubMed - NCBI
    Inhibition of benzodiazepine binding in vitr... [Pharm Acta Helv. 1997] - PubMed - NCBI
    Biflavones from Rhus species with affinity ... [J Ethnopharmacol. 2006] - PubMed - NCBI
    Semisynthetic preparation of amentoflav... [Bioorg Med Chem Lett. 2003] - PubMed - NCBI
    Transport of amentoflavone across the blood-brain... [Planta Med. 2002] - PubMed - NCBI
    Antidepressant and anxiolytic effect... [Pharmacol Biochem Behav. 2012] - PubMed - NCBI
    Review on plants with CNS-effects used in t... [J Ethnopharmacol. 2008] - PubMed - NCBI
    Effects of St. John's wort extract and single con... [Planta Med. 2006] - PubMed - NCBI
    Isolation of amentoflavone from Selaginella rupes... [Planta Med. 1981] - PubMed - NCBI

    Fatty Acid Synthase Inhibition

    Fatty acid synthase, as the name implies, is responsible for the endogenous synthesis of fatty acids in humans. It is currently a drug target for metabolic syndrome. In at least three separate trials, amentoflavone has demonstrated the ability to inhibit fatty acid synthase, and thus fat production.

    Summary: Reduced fatty acid synthesis

    Fatty acid synthase inhibition by amentoflav... [Biol Pharm Bull. 2009] - PubMed - NCBI
    Fatty acid synthase inhibition by amentoflavon... [Phytother Res. 2013] - PubMed - NCBI
    Inhibition of fatty acid synthase by amentoflavon... [Arch Virol. 2012] - PubMed - NCBI

    Phosphodiesterase (PDE) Inhibition

    PDE is the enzyme responsible for breaking down cAMP/cGMP. cAMP/cGMP promote smooth muscle relaxation (vasodilation; this is how PDE5 inhibitors help with erectile dysfunction) and lipolysis. Indeed, Forskolin has documented lipolytic activity by increasing cAMP levels via increased cAMP production. PDE inhibition, as with amentoflavone, hits the opposite side of the coin: reduced cAMP breakdown. By increasing cAMP levels, amentoflavone can synergize with adrenergic agonists (i.e. b-agonists) because second messenger pathways follow the rule of amplification.
    Amentoflavone inhibits a broad array of PDE isoforms, and it is the most potent inhibitor out of all tested flavonoids in Ginkgo biloba. Further, of all tested constituents of Allanblackia monticola, Amentoflavone was the strongest vasodilator, inhibiting norepinephrine-induced vasoconstriction by a whopping 35%.
    Summary: Increased lipolysis (fat loss) and increased vasodilation

    Inhibition of cAMP-phosphodiesterase by biflavone... [J Nat Prod. 1998] - PubMed - NCBI
    Biflavones of Decussocarpus rospigliosii as phosp... [Planta Med. 2007] - PubMed - NCBI
    Inhibition of cGMP-phosphodiesterase-5 by biflavo... [Planta Med. 2006] - PubMed - NCBI
    Antimalarial and vasorelaxant constit... [Ann Trop Med Parasitol. 2007] - PubMed - NCBI
    Vasorelaxation by amentoflavone isolated from Sel... [Planta Med. 2004] - PubMed - NCBI
    Inhibition of human platelet cyclic AMP ph... [Biochem Pharmacol. 1986] - PubMed - NCBI

    Muscular Strength and Endurance

    One well-documented mechanism of increasing exercise performance is vasodilation, which helps supply (oxygen; waste removal) meet the demand of exercising muscle tissue (hypoxia; metabolic waste accumulation). Amentoflavone has a well-documented effect on vasodilation as described above.
    In addition to this, Amentoflavone provides a relatively unique mechanism for increasing power output: increased Ca2+ release from the sarcoplasmic reticulum. By increasing intracellular Ca2+ downstream of the signal for muscle contraction, binding to troponin-C is increased and the force of muscular contraction, on a cell-by-cell basis, also increases.
    Caffeine acts via a similar mechanism to increase strength output, and researchers found that not only does Amentoflavone likely bind to the caffeine-binding site, but it does so with 20 times greater potency than caffeine.

    Summary: Improved strength (Ca2+ release) and improved endurance (vasodilation)
    Properties of amentoflavone, a potent caffei... [Eur J Pharmacol. 1999] - PubMed - NCBI

    Insulin Sensitivity/GDA - PTP1B inhibition

    PTP1B is an enzyme involved in insulin signaling, and inhibition of PTP1B is being investigated as a possible treatment for obesity and diabetes. PTP1B inhibition will chiefly improve insulin sensitivity by augmenting insulin's actions within the cell at a lower circulating level of insulin. This is a fairly novel approach to improving insulin sensitivity and will continue to be investigated.

    Summary: Improved insulin sensitivity

    Protein tyrosine phosphatase 1B inhibitory a... [Biol Pharm Bull. 2007] - PubMed - NCBI

    Dyslipidemia

    Amentoflavone has been shown in vivo to reduce circulating lipids (LDL/TG), making it of further benefit to obesity/diabetes/metabolic syndrome.

    Summary: Reduced lipids

    Antidyslipidemic and antioxidant activity of t... [Phytomedicine. 2012] - PubMed - NCBI

    Credit and thanks to neuron: http://hightowerpharmacology.blogspo...toflavone.html
    Definitely an ingredient to have in the arsenal, I believe it also increases the capsases 3 and 9 causing apoptosis is certain cell lines through down regulation on bcl-2.
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    How would standalone amentoflavone stack with the new combustion?
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    Quote Originally Posted by PharmAnalyst View Post
    How would standalone amentoflavone stack with the new combustion?
    Could you post the profile
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    The above is my own opinion and does not reflect the opinion of PES
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    Would the increase in strength result in a increase in muscle building or is it just a temporary thing?
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    Any stims we should BOLO to not stack with amentoflavone?

    I picked up two bottles with the AS sale and I plan on starting them next week for an 8 week run with EC leading Into summer. I was impressed by 4 weeks of norco so I'm very hopeful for an additional 4
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    Quote Originally Posted by raekwonse View Post
    Would the increase in strength result in a increase in muscle building or is it just a temporary thing?
    Increased strength will result in improved body composition (not to mention the fat loss benefits)
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    Quote Originally Posted by chedapalooza View Post
    Any stims we should BOLO to not stack with amentoflavone?

    I picked up two bottles with the AS sale and I plan on starting them next week for an 8 week run with EC leading Into summer. I was impressed by 4 weeks of norco so I'm very hopeful for an additional 4
    I don't know what BOLO means but it will work fine with EC
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    BOLO I think stands for be on the look out.
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    Quote Originally Posted by mr.cooper69 View Post

    Could you post the profile
    Best I can do on mobile...

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    Quote Originally Posted by mr.cooper69 View Post

    I don't know what BOLO means but it will work fine with EC
    Be on the lookout
    "no failure is final, nor is any success"
    Follow my 2014 training and supps!
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    Quote Originally Posted by mr.cooper69 View Post
    Could you post the profile

    Amount Per Serving % Daily Value
    Higenamine 22 mg **
    Alstonia Scholaris 40% 125 mg **
    Caffeine 125 mg **
    Piperine 5 mg **
    b-PEA 125 mg **
    Morus Alba 20:1 200 mg **
    Forskolin 40 mg **

    (Used Jimbuick's Link)
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    It would work well with the formula. It should synergize with the forskolin too
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    Starting 8 week run today til July 1st. Can't believe July 1st is only 8 weeks away. Looking forward to some happy moods and fat loss!
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    Bought some of the AS amentoflavone, any idea how I should time my dosing to maximize the strength/endurance benefits?
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    2 caps 15 minutes prior to exercise!
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    Quote Originally Posted by mr.cooper69 View Post
    2 caps 15 minutes prior to exercise!
    Coop, is it okay to take a dose 45minutes to an hour pre work out?
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    Is there any drug interaction in conjunction with amentoflavone administration?

    Sounds like a thing worth to try. Was thinking on Katana pwo, looks solid.
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    Quote Originally Posted by cbsharpe View Post
    Coop, is it okay to take a dose 45minutes to an hour pre work out?
    Probably doesn't matter; I think the effects last for several hours iirc. neuron used to have a great writeup on it but its gone from his blog now
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    Quote Originally Posted by Quadzilla99 View Post
    Probably doesn't matter; I think the effects last for several hours iirc. neuron used to have a great writeup on it but its gone from his blog now
    Thanks Quadz!
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    Due to the antagonistic effects on angiogenesis from amentoflavone and (transdermal) ursolic acid respectively, would it be ideal to run them separately for maximum benefit?
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    Quote Originally Posted by PharmAnalyst View Post
    Due to the antagonistic effects on angiogenesis from amentoflavone and (transdermal) ursolic acid respectively, would it be ideal to run them separately for maximum benefit?
    Nah, neither matters unless you have a pre-cancerous condition
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    Given that both affect the GABAergic system, would it be advisable to avoid combining picamilon and amentoflavone?
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    Quote Originally Posted by PharmAnalyst View Post
    Given that both affect the GABAergic system, would it be advisable to avoid combining picamilon and amentoflavone?
    Yes, take the picamilon away from when you dose your amentoflavone.
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