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    Lightbulb Pharmacology of Methylsynephrine

    Methylsynephrine



    Methylsynephrine
    Methylsynephrine (Oxilofrine, Hydroxyephrine, Oxyephrine) is a mixed-adrenergic agonist with an ephedrine-like pharmacological profile. It is used as a dietary supplement in various products and is marketed as a weight-loss compound. Here, I will explore the nature of this compound in the literature.

    Synephrine
    Synephrine is an adrenergic agonist similar to phenylephrine [1] . Due to its secondary terminal-amine structure, it possesses a stronger affinity for alpha-receptors than norepinephrine and has been used clinically as a vasoconstrictor and pressor (Figure 1). Synephrine is a positional-isomer of phenylephrine and its metabolism is likely similar with extensive MAO elimination in the GI tract and in the liver. Synephrine may also play a role in vesicular exchange-diffusion within synapses with norepinephrine, although this appears weak at therapeutic concentrations.


    Figure 1.



    Physiological effects
    A study using a bitter orange extract standardized for 27 mg synephrine failed to induce any changes in hemodynamics [2]. Conversely, in another study using twice the amount, significant effects were observed for heart rate, systolic pressure, and diastolic pressures, in which all values increased [3]. This would indicate that the minimum threshold dose to elicit adrenergic activity to be somewhere between 27 mg and 54 mg for adult males.

    Pharmacodynamics
    Beta-receptor affinity for phenylethylamine derivatives increases as the nonpolar bulkiness on the terminal amine gets larger (Figure 2). Compared with phenylethylamine, norepinephrine, or other primary amines, synephrine should have greater affinity for beta-receptors due to its secondary amine structure. Similarly, beta-receptor affinity also increases with the addition of nonpolar substituents on the alpha-carbon, which synephrine does not possess. The fact that diastolic pressure also increased in the above study is evidence for very little beta-receptor activation. Although synephrine has demonstrated an ability to induce lipolysis by activating beta-3 receptors en vitro, its efficiency in doing so en vivo is greatly limited because of its inherent affinity for alpha receptors [4]. The dose required to sufficiently trigger lipolysis within adipocytes would be intolerable due to its effects on hemodynamics [5].

    Figure 2.



    Synephrines downsides
    Increasing peripheral vascular resistance is a negative characteristic of a lot of stimulants and is especially exacerbated in compounds which primarily activate alpha-receptors like synephrine. Not only is the incidence of stroke and hemorrhage higher with these agents, but the work-load put on the heart can trigger ventricular fibrillations or other arrhythmias [6, 7, 8]. Using caffeine in conjunction with synephrine will potentiate the peripheral vasoconstriction by synergizing with the transduction mechanism induced by alpha-adrenergic agonism [9, 10]. Adrenergic agonists with high affinity to alpha-receptors also have the unfortunate capacity to induce platelet aggregation by agonizing alpha-2 receptors on platelets which can lead to intravascular clotting [11, 12].

    Methylsynephrine vs. Synephrine
    The primary difference between synephrine and methylsynephrine is the addition of a methyl group on the alpha carbon (Figure 3). As mentioned previously, this has extensive pharmacodynamic implications as it increases the affinity of the compound for beta-receptors.


    Figure 3.



    Pharmacokinetics
    The half-life for phenylephrine is an adequate gauge for the half-life and elimination statistics for synephrine due to its similar structure and chemical characteristics. Similarly, ephedrine and pseudoephedrine can be used to make an educated guess regarding the pharmacokinetics of methylsynephrine. Phenylephrine, a positional isomer of synephrine, has a half-life of 2.1 -3 hours. The half-life of ephedrine is from 3-6 hours, depending on urine pH. Pseudoephedrine enjoys an even longer half-life due to increased steric-hindrance of MAO. The mean half-life of methylsynephrine, as compared to synephrine, would be roughly twice the duration. Neither synephrine, ephedrine, nor methylsynephrine, possess notable central effects due to the common beta-hydroxyl which prevents substantial blood-brain-barrier permeability (Appendix A).

    Pharmacodyamics
    Although the exact pharmacology of methylsynephrine has not been studied in great detail, its pharmacodynamics can be inferred through its effects on systolic blood pressure, diastolic blood pressure, and heart rate. Differing from synephrine, methylsynephrines effects on the heart are mostly beneficial in that it increases the pulse pressure and is a positive inotrope (Appendix B). Diastolic pressure is used clinically as a diagnostic marker for peripheral vascular resistance, especially in relation to the arterial system [13]. Activating beta-2 receptors in the periphery induces vasodilation in vascular beds in the liver and skeletal muscle, which decreases the work-load on the heart. Since it also has some alpha-adrenergic activity, reflexive tachycardia would be avoided. Similarly, activating beta-receptors would increase venous tone, which will increase the amount of blood returning to the heart, and subsequently increase cardiac output, as illustrated by Starling’s Law [14, 15]. The beta-3 receptor, as noted above, directly mediates lipolysis. The genetic homology of the ligand-binding-domain between the beta-3 receptor and the beta-2 receptor is greater than that of the beta-1 receptor. This explains why norepinephrine, which possesses a primary terminal amine, has sufficient affinity for beta-1 receptors, but very little beta-2 or beta-3 affinity, and therefore limited ability to induce lipolysis. This means that compounds which significantly activate beta-2 receptors will also have great predilection to also activate beta-3 receptors.

    Physiological effects
    Methylsynephrine has been used clinically for orthostatic hypotension due to its effects on stroke volume, ejection fraction, and cardiac index [16, 17]. It has been used in doses of up to 120mg in healthy adults with no adverse effects [18, 19]. Even at this dose, diastolic pressure decreased, which is evidence for very little alpha-adrenergic activity. Furthermore, it had no effect on heart rate or mean arterial pressure. Some of methylsynephrines therapeutic efficacy is mediated by acting as a norepinephrine-releasing agent, and also by inhibiting its uptake [20]. The majority of methylsynephrines pharmacological appeal resides in its ability to activate beta receptors, which is exemplified through its effects on the heart and haemodynamics as described above. This also implies significant beta-3 activity and an ability to induce lipolysis which is consistent with some of its marketing claims [21]. Another deviation from synephrine is methylsynephrines limited propensity to activate alpha-2 receptors on platelets. This would avoid the complications of intravascular clotting, which has resulted in myocardial infarction mortality associated with synephrine, although allow for the possibility of cerebral hemorrhage [22].

    Summary
    Methylsynephrine is a unique compound which has not been used frequently in clinical practice. Due to its ephedrine-like pharmacology, and its surprisingly clean safety record, it will likely become a more common ingredient in fat loss supplements in the future. It is currently uncontrolled in the United States [23].

    Appendix A:


    Appendix B:
    Pulse Pressure (Pp) = Systolic pressure – Diastolic pressure

    Relevant links:
    PubMed Compound: http://pubchem.ncbi.nlm.nih.gov/summ...701&loc=ec_rcs
    Methylsynephrine wikipedia entry: http://en.wikipedia.org/wiki/Oxilofrine
    Mirrored site: http://www.recomp.com/wiki/index.php...ne&redirect=no


    References:
    1. http://www.ncbi.nlm.nih.gov/pubmed/19721332
    2. http://www.ncbi.nlm.nih.gov/pubmed/16305290
    3. http://www.ncbi.nlm.nih.gov/pubmed/16317106
    4. http://www.springerlink.com/content/uemq7ml1lcee6a3c/
    5. http://www.ncbi.nlm.nih.gov/pubmed/15337824
    6. http://www.ncbi.nlm.nih.gov/pubmed/20055074
    7. http://www.ncbi.nlm.nih.gov/pubmed/18700609
    8. http://www.ncbi.nlm.nih.gov/pubmed/16610576
    9. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1175678/
    10. http://www.ncbi.nlm.nih.gov/pubmed/18341680
    11. http://www.ncbi.nlm.nih.gov/pubmed/18637307
    12. http://www.ncbi.nlm.nih.gov/pubmed/20069086
    13. http://www.ncbi.nlm.nih.gov/pubmed/3229871
    14. http://www.ncbi.nlm.nih.gov/pubmed/3119915
    15. http://www.springerlink.com/content/vmw352074216g871/
    16. http://www.ncbi.nlm.nih.gov/pubmed/1530677
    17. http://www.ncbi.nlm.nih.gov/pubmed/3119915
    18. http://www.ncbi.nlm.nih.gov/pubmed/3229871?ordinalpos=1&itool=EntrezSystem2.PEntrez.P ubmed.Pubmed_ResultsPanel.Pubmed_SingleItemSupl.Pu bmed_Discovery_RA&linkpos=2&log$=relatedarticles&l ogdbfrom=pubmed
    19. http://www.ncbi.nlm.nih.gov/pubmed/3403107?ordinalpos=1&itool=EntrezSystem2.PEntrez.P ubmed.Pubmed_ResultsPanel.Pubmed_SingleItemSupl.Pu bmed_Discovery_RA&linkpos=1&log$=relatedarticles&l ogdbfrom=pubmed
    20. http://www.ncbi.nlm.nih.gov/pubmed/7191269
    21. http://www.ncbi.nlm.nih.gov/pubmed/12439645
    22. http://www.ncbi.nlm.nih.gov/pubmed/20179577
    [23] Wikipedia contributors. "Oxilofrine." Wikipedia, The Free Encyclopedia. Wikipedia, The Free Encyclopedia, 17 Feb. 2010. Web. 14 Mar. 2010.
    Last edited by Cytokine; 03-14-2010 at 11:08 AM.
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    Great post!!
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    Nice!

    I've always loved learning about stimulants.
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    Originally Posted by Angelbolic View Post
    Great post!!
    Originally Posted by Adjusting View Post
    Nice!

    I've always loved learning about stimulants.
    Thanks. The purpose of the article is to highlight some of the potential benefits of methylsynephrine, while also debunking some of the myths about synephrine (and other agents with limited beta-3 affinity). If one follows the axioms I layed out above, it should be clear why 1,3-dimethylamylamine cannot directly trigger lipolysis as is commonly claimed in marketing write-ups.

    One of the things which I wanted to elaborate upon was the transduction mechanisms inherent to different adrenergic receptors.

    For example, alpha1-receptors activate the IP3-DAG transduction cascade which ultimately results in calcium release and contraction/vasoconstriction (in smooth muscle). This mechanism is potentiated by caffeine co-consumption since caffeine enhances calcium release. Conversely, beta-receptors (all three of them) work through elevation of intracellular cAMP. Since caffeine also functions as a PDEi, cAMP levels will be prolonged. This explains why ephedrine alone (a beta-3 agonist) is only a weak lipolytic-inducing agent, but extremely potent in concert with caffeine.

    Here's a good reveiw: http://www.sciencedirect.com/science...ca039e1e6c4368
    Last edited by Cytokine; 03-14-2010 at 05:18 PM.
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    Originally Posted by Cytokine View Post
    Thanks. The purpose of the article is to highlight some of the potential benefits of methylsynephrine, while also debunking some of the myths about synephrine (and other agents with limited beta-3 affinity). If one follows the axioms I layed out above, it should be clear why 1,3-dimethylamylamine cannot directly trigger lipolysis as is commonly claimed in marketing write-ups.

    One of the things which I wanted to elaborate upon was the transduction mechanisms inherent to different adrenergic receptors.

    For example, alpha1-receptors activate the IP3-DAG transduction cascade which ultimately results in calcium release and contraction/vasoconstriction (in smooth muscle). This mechanism is potentiated by caffeine co-consumption since caffeine enhances calcium release. Conversely, beta-receptors (all three of them) work through elevation of intracellular cAMP. Since caffeine also functions as a PDEi, cAMP levels will be prolonged. This explains why ephedrine alone (a beta-3 agonist) is only a weak lipolytic-inducing agent, but extremely potent in concert with caffeine.

    Here's a good reveiw: http://www.sciencedirect.com/science...ca039e1e6c4368
    Should users of 1,3-dimethylamylamine be concerned about long-term cardiac effects?

    Second, I've always known that caffeine potentiates the effects of ephedrine. Is there anything else that can have such a profound effects on cAMP? (and not forskolin)
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    Great post and contribution.

    Reinforces why I hate Synephrine in fat loss products.
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    Originally Posted by Adjusting View Post
    Should users of 1,3-dimethylamylamine be concerned about long-term cardiac effects?
    1,3-DMAA appears to act mainly as a NE releasing agent via exchange-diffusion, so its effects on the heart would fall within the umbrella of norepinephrines effects. NE can act on cardiac beta-1 receptors, although this effect is negligable due to its systemic effects (alpha-1 agonism). Due to the baroreceptor reflex, cardiac output is actually diminished. I don't foresee any long-term cardiac effects even if one consumes 1-3-DMAA chronically due to the tolerance that develops after repeated administrations.

    Originally Posted by Adjusting View Post
    Second, I've always known that caffeine potentiates the effects of ephedrine. Is there anything else that can have such a profound effects on cAMP? (and not forskolin)
    More specific PDE isoform inhibition in adipose tissue, I suppose.

    http://www.ncbi.nlm.nih.gov/pubmed/18617377

    ANP & Lipolysis: http://www.ncbi.nlm.nih.gov/pubmed/18337116
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    Looks like a new product just came out with Methylsynephrine:

    3,3-diiodo-l-thyronine (T2) 150 mcg
    Methyl-Synephrine 30 mg
    Rauwolscine HCL 7 mcg
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    Thumbs up

    Great post.

    Just the info I needed.
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    Originally Posted by Madevilz View Post
    Looks like a new product just came out with Methylsynephrine:

    3,3-diiodo-l-thyronine (T2) 150 mcg
    Methyl-Synephrine 30 mg
    Rauwolscine HCL 7 mcg
    - IMO, thyroid metabolites are worthless unless one is supplementing with something like cytomel - and even then, the therapeutic index is very low (negative effects >> positive effects).

    - Methylsynephrine @30mg might be a decent dose combined with caffeine.

    - Rauwolscine is an alpha-2 antagonist and has nothing to do with lipolysis.
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    30mgs is way to low IMO even with caffeine. Ive used a lot of MS at various doses and it needs a higher dose then what would be used when dosing ephedrine.
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    Originally Posted by Sldge View Post
    30mgs is way to low IMO even with caffeine. Ive used a lot of MS at various doses and it needs a higher dose then what would be used when dosing ephedrine.
    In one of the studies I cited above, 60mg was sufficient to significantly effect hemodynamic values in adult males, which would indicate B1/B2 agonism. Co-supplementing with caffeine will promote this effect in a synergistic way, although one still has to account for caffeine tolerance, differential metabolism, body mass, exc.

    Is a methylsynephrine product on the horizon for DS? It would be nice for a company to produce a MS product with an efficient dose and without crap like yohimbine.
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    Five star thread. Will read again.
    Nutrition and Supp Science FAQ:
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    Originally Posted by neuron View Post
    In one of the studies I cited above, 60mg was sufficient to significantly effect hemodynamic values in adult males, which would indicate B1/B2 agonism. Co-supplementing with caffeine will promote this effect in a synergistic way, although one still has to account for caffeine tolerance, differential metabolism, body mass, exc.

    Is a methylsynephrine product on the horizon for DS? It would be nice for a company to produce a MS product with an efficient dose and without crap like yohimbine.
    IIRC a 40mg dose (may have been 50mg) felt like ~20mg ephedrine for me, but with a much shorter duration. Did not try it with caffeine, but Matt has tried it with probably everything from caffeine to oven cleaner.
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    Originally Posted by neuron View Post
    In one of the studies I cited above, 60mg was sufficient to significantly effect hemodynamic values in adult males, which would indicate B1/B2 agonism. Co-supplementing with caffeine will promote this effect in a synergistic way, although one still has to account for caffeine tolerance, differential metabolism, body mass, exc.

    Is a methylsynephrine product on the horizon for DS? It would be nice for a company to produce a MS product with an efficient dose and without crap like yohimbine.
    I may have not gotten that out correctly. I think 40-60 is probably fine but Im not someone who likes having their heart race, hands shake type feeling that most people seem to want just so they know "its working", hence all of the damn formulas with yohimbine in them. Even if people dont want to admit it they like feeling cracked out.

    In order to get that feeling (without yo, which I think is a great idea as well) you need a higher dose of the MS. Rob did find that the 50mg dose felt close to E for him but he doesnt use much caffeine or stims. Ive found that for the true E feel you need about 80mgs+ if you dont take it with any caffeine. With 200mgs of caffeine I find I only need 60mgs and the effects last around 3 hours (very similar to what i would get on EC). Now Im what I would call a super responder, I can take very small doses and get hit with the effects right away. Ive tested up to 150mgs alone and Ive tested 100-120mgs with caffeine and with a 50% mix of caffeine and caffeine that was time released. In a very close friend who I would call a non-responder (needs very high doses for min effects) he needed at least 100mgs.
    I also tried it with Dsade's alpha-yo to try to mimic the old ECY stack and that wasnt too bad. Ive tried it with a few others things that most people probably wouldnt try but I think best bang for the buck, down and dirty old school EC feel you want at least 50mgs and probably 60 of MS and at least 200mgs of caff but probably 225-250.

    I dont know if its something we would use in the future or not. I can say that we havent ruled it out that's for sure and there are really only a few issues as to why we wouldnt use it with cost being the biggest. All in all not a bad compound and IMO leaps and bounds better then MHA (geranamine).

    Originally Posted by Robboe View Post
    IIRC a 40mg dose (may have been 50mg) felt like ~20mg ephedrine for me, but with a much shorter duration. Did not try it with caffeine, but Matt has tried it with probably everything from caffeine to oven cleaner.
    That you did. Not oven cleaner yet but probably everything else, LOL.
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    Originally Posted by Sldge View Post
    I may have not gotten that out correctly. I think 40-60 is probably fine but Im not someone who likes having their heart race, hands shake type feeling that most people seem to want just so they know "its working"
    The good thing about methylsynephrine is that it does not possess a lot of the bad characteristics which stimulants have gotten a bad rap for. As discussed above, methylsynephrine has a very good hemodynamic pharmacodynamic profile.

    Ephedrine itself has a better hemodynamic profile as compared to its "legal" replacement, synephrine.

    Originally Posted by Sldge View Post
    hands shake type feeling that most people seem to want just so they know "its working", hence all of the damn formulas with yohimbine in them. Even if people dont want to admit it they like feeling cracked out.
    Yohimbine is frequently used in veterinary settings to reverse the effects of sedatives due to the fact that is easily crosses the BBB and increases central sympathetic tone. It also functions as a peripheral alpha-2 antagonist, which both function to increase synaptic norepinephrine levels. In humans, the former typically yields anxiety and/or other behavioral disturbances, whereas the latter can possibly result in lipolysis, although the concentration necessary to induce lipolysis is typically so high that it is unpleasant and potentially dangerous. Norepinpherine has a high affinity for B1, and alpha-1 receptors. As I mentioned in the article above, B1 receptors increase heart rate (chronotropy), and cardiac tension (inotropism), and alpha-1 receptors generally mediate peripheral vasoconstriction. The end result is that the heart is beating harder and faster, and against more peripheral vascular resistance, which can cause cardiac dysrhythmias (not a good thing). I think yohimbine's value for inducing fat loss would be greater if someone could figure out how to lessen its central effects/increase its hydrophilicity, since blocking alpha-2 receptors on fat cells has some merit in potentiating lipolysis.

    As far as people thinking they need the "cracked out" feeling for reassurance that the supplement they are taking is working, I would submit to you that they are not far off. Any drug that has high affinity for B2 receptors (albuterol, clenbuterol, isoproterenol), and therefore high affinity for B3, is known to cause fasciculations due to cAMP-enhanced calcium release within skeletal muscle. This subsides over time as beta-2 receptors are temporarily downregulated, although it is still a good marker for beta-receptor activity, and therefore a good litmus test for lipolytic-inducting capabilities.


    Originally Posted by Sldge View Post
    In order to get that feeling (without yo, which I think is a great idea as well) you need a higher dose of the MS. Rob did find that the 50mg dose felt close to E for him but he doesnt use much caffeine or stims. Ive found that for the true E feel you need about 80mgs+ if you dont take it with any caffeine. With 200mgs of caffeine I find I only need 60mgs and the effects last around 3 hours (very similar to what i would get on EC).
    Caffeine is definitely a must with methylsynephrine. Even ephedrine itself has demonstrated weak lipolytic inducing potential in the absence of caffeine. This makes sense as caffeine potentiates the transduction (Gs) mechanism involved in fat loss (inc. cAMP).


    Originally Posted by Sldge View Post
    All in all not a bad compound and IMO leaps and bounds better then MHA (geranamine).
    Based on its SAR, geranamine has no ability to directly induce fat loss, although it does have value in increasing energy, although tolerance seems to develop rapidly.
    Last edited by neuron; 03-25-2010 at 10:21 PM.
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    Great post. Had a question if anyone has the answer.

    (Ephedrine Sulfate vs. Ephedrine HCL) There are some OTC products available which contain sulfate (Bronkaid). The only data I have come across is that HCL is a stronger product. How significant is this difference? Are there other differences between the two?
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    Originally Posted by neuron View Post
    The good thing about methylsynephrine is that it does not possess a lot of the bad characteristics which stimulants have gotten a bad rap for. As discussed above, methylsynephrine has a very good hemodynamic pharmacodynamic profile.

    Ephedrine itself has a better hemodynamic profile as compared to its "legal" replacement, synephrine.



    Yohimbine is frequently used in veterinary settings to reverse the effects of sedatives due to the fact that is easily crosses the BBB and increases central sympathetic tone. It also functions as a peripheral alpha-2 antagonist, which both function to increase synaptic norepinephrine levels. In humans, the former typically yields anxiety and/or other behavioral disturbances, whereas the latter can possibly result in lipolysis, although the concentration necessary to induce lipolysis is typically so high that it is unpleasant and potentially dangerous. Norepinpherine has a high affinity for B1, and alpha-1 receptors. As I mentioned in the article above, B1 receptors increase heart rate (chronotropy), and cardiac tension (inotropism), and alpha-1 receptors generally mediate peripheral vasoconstriction. The end result is that the heart is beating harder and faster, and against more peripheral vascular resistance, which can cause cardiac dysrhythmias (not a good thing). I think yohimbine's value for inducing fat loss would be greater if someone could figure out how to lessen its central effects/increase its hydrophilicity, since blocking alpha-2 receptors on fat cells has some merit in potentiating lipolysis.

    As far as people thinking they need the "cracked out" feeling for reassurance that the supplement they are taking is working, I would submit to you that they are not far off. Any drug that has high affinity for B2 receptors (albuterol, clenbuterol, isoproterenol), and therefore high affinity for B3, is known to cause fasciculations due to cAMP-enhanced calcium release within skeletal muscle. This subsides over time as beta-2 receptors are temporarily downregulated, although it is still a good marker for beta-receptor activity, and therefore a good litmus test for lipolytic-inducting capabilities.




    Caffeine is definitely a must with methylsynephrine. Even ephedrine itself has demonstrated weak lipolytic inducing potential in the absence of caffeine. This makes sense as caffeine potentiates the transduction (Gs) mechanism involved in fat loss (inc. cAMP).




    Based on its SAR, geranamine has no ability to directly induce fat loss, although it does have value in increasing energy, although tolerance seems to develop rapidly.
    I agree with a lot of what you said. I do think caffeine is a must, especially with this. You need it with ephedrine so there is no reason to not add it to this. At the right dose of both it had a very similar feel to the EC stack it just didnt last as long for me. Normally I can get 4 good hours out of EC and I was only around half of that with MSC.

    I think you need to use YO with Tyramine and without carbs. That combo was the best for me for fat loss when I played with that combo 10 years ago or so. Its not that being cracked out might not be a good litmus test when talking about some of these compounds. But you could induce the cracked out feeling with compounds you normally wouldnt think would boost weight loss. I feel like its a bad idea for people who dont have experience with these compounds or with supplements to think they need to feel all these sides to think they have a product that works. You could put a serious dose of YO in any product but not enough to actually produce weight loss or any other benefit but it gives the sheeple the thought that it must be working. Its like the tingle in shampoo.

    Overall I like MS and MSC. I did add Dsades alpha-yo to it during testing and it was pretty good. I like the idea of having a stim that works really well, hits pretty hard but lasts no longer then 2 hours. Its perfect to use precardio or workout but not be amped up late at night.
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    Originally Posted by M1keD View Post
    Great post. Had a question if anyone has the answer.

    (Ephedrine Sulfate vs. Ephedrine HCL) There are some OTC products available which contain sulfate (Bronkaid). The only data I have come across is that HCL is a stronger product. How significant is this difference? Are there other differences between the two?
    Although your post is completely off-topic, the sulfate constituent is heavier than HCl, so ephedrine HCl possesses slightly more ephedrine by weight.

    25 mg ephedrine HCl = 20.5 mg ephedrine

    25 mg ephedrine sulfate = 19.25 mg ephedrine

    Originally Posted by Sldge View Post
    Its not that being cracked out might not be a good litmus test when talking about some of these compounds. But you could induce the cracked out feeling with compounds you normally wouldnt think would boost weight loss. I feel like its a bad idea for people who dont have experience with these compounds or with supplements to think they need to feel all these sides to think they have a product that works. You could put a serious dose of YO in any product but not enough to actually produce weight loss or any other benefit but it gives the sheeple the thought that it must be working. Its like the tingle in shampoo.
    Agreed.
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    Originally Posted by neuron View Post
    Although your post is completely off-topic, the sulfate constituent is heavier than HCl, so ephedrine HCl possesses slightly more ephedrine by weight.

    25 mg ephedrine HCl = 20.5 mg ephedrine

    25 mg ephedrine sulfate = 19.25 mg ephedrine



    Agreed.
    Sorry, and thanks for the reply.
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    I just ordered a stack of LX and the new Alpha-T2 mentioned above with MS @ 30.

    This is a great thread and I had a question regarding the caffeine component. Since I will be taking the Alpha in the AM, would my 1-2 cups of morning coffee at the office be a succifient synergist, or would a direct caffeine pill in the ~200 range be a better option, in terms of bioavailibility?

    I hope that question makes sense.
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    If you have coffee anyway then don't take the caffeine pill. I don't think you'll need 280+mgs of caff with the Alpha-T2, at least not fir the first week.
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    As a supplement consumer, I don't understand why someone would take MS when they can take E. Obviously supplement producers can't use E anymore, but I can walk down the street to CVS and pick up a box of Bronkaid for less than the latest & "greatest" fat-loss supplement. Is there any reason to use MS over E?
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    Originally Posted by DriverDan View Post
    Is there any reason to use MS over E?
    No.
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    Originally Posted by neuron View Post
    I think yohimbine's value for inducing fat loss would be greater if someone could figure out how to lessen its central effects/increase its hydrophilicity, since blocking alpha-2 receptors on fat cells has some merit in potentiating lipolysis.
    This may sound stupid (to you), but I'm still inclined to ask:

    Do you thinking that people with higher peripheral A2 number/density may suffer less from the negative central effects of yohimbine? For instance, I have a number of issues with stubborn fat that is cold to the touch (peri-gyno fat, lower back/love handles, glutes...) and have taken 20mg Y/200mg Caff (on an empty stomach) on multiple occasions and have had zero feelings of anxiety or whatnot. Conversely, many people that talk about Y cracking them out (even in a few mg doses), from what I have seen, have fairly even BF distributions and are already pretty lean anyway.
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    Originally Posted by papagunz View Post
    This may sound stupid (to you), but I'm still inclined to ask:

    Do you thinking that people with higher peripheral A2 number/density may suffer less from the negative central effects of yohimbine? For instance, I have a number of issues with stubborn fat that is cold to the touch (peri-gyno fat, lower back/love handles, glutes...) and have taken 20mg Y/200mg Caff (on an empty stomach) on multiple occasions and have had zero feelings of anxiety or whatnot. Conversely, many people that talk about Y cracking them out (even in a few mg doses), from what I have seen, have fairly even BF distributions and are already pretty lean anyway.
    Interesting question. The anxiogenic property of yohimbine is due to its ability to cross the blood-brain-barrier and increase sympathetic tone in various brain regions - specifically the lateral hypothalamus circuit to the amygdala. The influence of this drug produces tachycardia, mydriasis, paleness, hypertension, and other manifestations of anxiety.

    There is definitely genetic variability to the density of NE receptors in this region, as well as environmental impacts which can play a role in yohimbines ability to produce anxiety. As an example: monkeys subjected to emotional trauma as perinates demonstrated increased aptitude for cortisol dysregulation, hippocampal atrophy, and overt manifestations of anxiety throughout their lives. This has been hypothesized to translate to humans with poor upbringings who also experience similar symptoms. The consequences are of such an event/sequence are extremely pleiotrophic (metabolic syndrome, type II diabetes, exc).

    There are also differences between the sexes. Females have much lower response to sympathetic stimulation (less fight or flight). This is likely the reason why yohimbine is typically better tolerated in women than men.

    The densities of catecholamine receptors (alpha1/2-bete1/2/3) peripherally is not related to its anxiogenic properties. I think that if yohimbine is working for you, not producing anxiety, and not effecting heart rate & blood pressure, then feel free to use it.
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    Originally Posted by papagunz View Post
    This may sound stupid (to you), but I'm still inclined to ask:

    Do you thinking that people with higher peripheral A2 number/density may suffer less from the negative central effects of yohimbine? For instance, I have a number of issues with stubborn fat that is cold to the touch (peri-gyno fat, lower back/love handles, glutes...) and have taken 20mg Y/200mg Caff (on an empty stomach) on multiple occasions and have had zero feelings of anxiety or whatnot. Conversely, many people that talk about Y cracking them out (even in a few mg doses), from what I have seen, have fairly even BF distributions and are already pretty lean anyway.
    I have similar fat storage, and also do not react unfavorably to yohimbine. Maybe we are just more feminine.
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    Originally Posted by DriverDan View Post
    As a supplement consumer, I don't understand why someone would take MS when they can take E. Obviously supplement producers can't use E anymore, but I can walk down the street to CVS and pick up a box of Bronkaid for less than the latest & "greatest" fat-loss supplement. Is there any reason to use MS over E?
    I think a lot of it is convenience. People dont want to actually go to CVS, sign their name on a piece of paper saying they buy E every month. No one uses benzedrex and you can get that just as easy.
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    Originally Posted by neuron View Post
    Interesting question. The anxiogenic property of yohimbine is due to its ability to cross the blood-brain-barrier and increase sympathetic tone in various brain regions - specifically the lateral hypothalamus circuit to the amygdala. The influence of this drug produces tachycardia, mydriasis, paleness, hypertension, and other manifestations of anxiety.

    There is definitely genetic variability to the density of NE receptors in this region, as well as environmental impacts which can play a role in yohimbines ability to produce anxiety. As an example: monkeys subjected to emotional trauma as perinates demonstrated increased aptitude for cortisol dysregulation, hippocampal atrophy, and overt manifestations of anxiety throughout their lives. This has been hypothesized to translate to humans with poor upbringings who also experience similar symptoms. The consequences are of such an event/sequence are extremely pleiotrophic (metabolic syndrome, type II diabetes, exc).

    There are also differences between the sexes. Females have much lower response to sympathetic stimulation (less fight or flight). This is likely the reason why yohimbine is typically better tolerated in women than men.

    The densities of catecholamine receptors (alpha1/2-bete1/2/3) peripherally is not related to its anxiogenic properties. I think that if yohimbine is working for you, not producing anxiety, and not effecting heart rate & blood pressure, then feel free to use it.
    Thank you very much for the detailed response. Guess I'm fairly womanly, woo. Makes sense, considering the gyno and preference for fat storage on my ass.

    I would have thought that the ratio of peripheral to neuronal catecholamine receptors would have some impact. (my simple lines of thinking were leaning towards less substrate (Y) available centrally if the bulk of the Y was already bound to peripheral catecholamine receptors) Thanks again for clearing all of this up.

    Another quick (possibly) question. Does higher BF percentage upregulate aromatase expression? The reason I ask is because both my father and I have gyno, and we were both significantly obese throughout our pubescent years. I think it may somewhat explain my patterns in fat deposition, and to a much lesser degree, my mannerisms.
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  30. #30
    Anna Ball Lick papagunz's Avatar
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    Originally Posted by Robboe View Post
    I have similar fat storage, and also do not react unfavorably to yohimbine. Maybe we are just more feminine.
    Exciting prospect. We can take that, turn it in our favor, and just say we're "sensitive."
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