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Thread: Effects of Stimulants on Metabolism

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    16 inches of pure passion Khar's Avatar
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    Effects of Stimulants on Metabolism

    When taking ephedrine/caffiene or any other stimulants that will increase your metabolism does your natural metabolism shut down or slow down to some degree as a result of the artificial boost in metabolism? Something similar to say taking creatine and while on creatine your liver stops or slows production of creatine. If it does slow down does it take time for it to rebound once you stop taking the stimulants or is it instantaneous?
    Last edited by Khar; 03-14-2004 at 07:00 PM.

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    Party of "No." Tryska's Avatar
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    Not quite, however, i do have a friend who is exploring the downgrade of b-2 receptors due to prolonged use of ephedrine, clenbuterol and albuterol. it was still in thesis stage as of a year ago - not sure whether he's made any progress.
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    16 inches of pure passion Khar's Avatar
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    if you find out anything let me know. I'm curious about this and I havn't been able to find **** on the net.

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    16 inches of pure passion Khar's Avatar
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    ttt

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    Wannabebig Member Podium Kreatin's Avatar
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    stimulants such as ephedrine and caffeine are "non-narcotic," b/c they do not create chemical dependency. Ephedrine is a beta-2 agonist which targets on a receptor, and its mechanism of action doesn't affect normal epinephrine/norepinephrine/thyroid production. Generally, the only chemicals which can make your glands atrophy are steroids (such as hydrocortisone or anabolic steroids).
    Caffeine is a phosphodiester inhibiter, whcih is an enzyme that breaks down cAMP (an intracellular messenger which tells the cell to do stuff). w/ more cAMP not breaking down, you have a buildup of cAMP, and hence, amplified effects (signal-> SIGNAL). Again, this doesn't target cAMP production, and wont' cause dependency.

    I heard myths of creatine causing dependency, but they are false. I don't think you can be dependent on supplementary creatine, cuz a lot of natural foods contain creatine (fruits, fish, meat). Creatine is stored in the muscles and recycled in the liver. Excess creatine is pissed out
    Last edited by Podium Kreatin; 03-17-2004 at 03:47 PM.
    "No one can completely believe that I am natural.
    The most important drug is to train like a madman
    -really like a madman
    The people who accuse me are those who have never trained once in their life as I train every day of my life."

    Alexandr Karelin
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    current stats (10/19/03): 20yrs, M, 5'4 @160lbs, ~11% body fat
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    16 inches of pure passion Khar's Avatar
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    Thanks Podium.
    Last edited by Khar; 03-17-2004 at 05:18 PM.

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    Steak and Eggs pusher's Avatar
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    Um, PK you may be half right, it may not cause 'chemical dependency' by affecting neurotransmitter production, but a stimulant like ephedrine can be addictive because chronic exposure of a receptor to an agonist can result in down-regulation => addiction.
    "The highest reward for man's toil is not what he gets for it, but what he becomes by it." -John Ruskin 1819-1900

    "He who fights monsters should see to it that in the process, he does not
    become a monster. And when you look into the abyss, the abyss also looks into
    you." - Nietzche

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    Wannabebig Member Podium Kreatin's Avatar
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    well, that's not always true. succinylcholine is an acetylcholine-analogue, and although it has a stronger effect than acetylcholine, it is broken down with the same enzymes that break down ACh. what happens w/ ephedrine is that it diffuses out of the receptors after it is "used." it doesn't really "damage" or change the receptor activity, and it doesn't down-regulate production of natural epinephrine.

    fight or flight:
    (CNS)---( Ach]-(adrenal medulla)--> Epi--> blood--> ]-beta-2Rc--> epi diffuses away and degrades
    ephedrine: intake->blood-->agonize beta Rc->ephedrine diffuses away and degrades

    according to this diagram, the only way to screw up our normal sympathetic system is if there is a way ephedrine causes a cell to release signals back into the kidney or brain, but that doesn't happen in nature. the brain pretty much makes the decisions. also, ephedrine is a polar molecule, and does not reach the brain, and hence, shoudl not affect the regularity of the brain
    Last edited by Podium Kreatin; 03-18-2004 at 01:01 AM.
    "No one can completely believe that I am natural.
    The most important drug is to train like a madman
    -really like a madman
    The people who accuse me are those who have never trained once in their life as I train every day of my life."

    Alexandr Karelin
    Ten-time World Greco-Roman Champion
    1988, 1992, 1996 Olympic gold medalist

    current stats (10/19/03): 20yrs, M, 5'4 @160lbs, ~11% body fat
    lifted since march 2000
    occupation:MCB major @ uc berkeley

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    Steak and Eggs pusher's Avatar
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    You're right, but the expression of receptors, ie. number of receptors on a cell can be down regulated in response to constant exposure to exogenous stimulants, in order to normalize or approach homeostasis. Its like smoking, constant exogenous nicotine down regulates the expression of nicotinic receptors, so if you stop smoking, you are left with too few receptors on the cell which is why smoking is addictive because quitting smoking is so hard, at least until the number of receptors is up regulated back to normal levels.
    "The highest reward for man's toil is not what he gets for it, but what he becomes by it." -John Ruskin 1819-1900

    "He who fights monsters should see to it that in the process, he does not
    become a monster. And when you look into the abyss, the abyss also looks into
    you." - Nietzche

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    Party of "No." Tryska's Avatar
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    i think pusher's idea of down-regulation b-2 receptors, is exactly what my friend was talking about. he actually got the idea from his mother's albuterol inhaler and her consequent increase in weight.
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    16 inches of pure passion Khar's Avatar
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    can this down regulation be reversed after coming off the stimulant?

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    Steak and Eggs pusher's Avatar
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    I suppose so, it is possible. The question is whether you get back to initial numbers specially if they've been suppressed for a long time.
    "The highest reward for man's toil is not what he gets for it, but what he becomes by it." -John Ruskin 1819-1900

    "He who fights monsters should see to it that in the process, he does not
    become a monster. And when you look into the abyss, the abyss also looks into
    you." - Nietzche

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    16 inches of pure passion Khar's Avatar
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    Well then...I think I'm gonna stop taking so much damn EC...

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    Wannabebig Member Podium Kreatin's Avatar
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    Quote Originally Posted by pusher
    You're right, but the expression of receptors, ie. number of receptors on a cell can be down regulated in response to constant exposure to exogenous stimulants, in order to normalize or approach homeostasis. Its like smoking, constant exogenous nicotine down regulates the expression of nicotinic receptors, so if you stop smoking, you are left with too few receptors on the cell which is why smoking is addictive because quitting smoking is so hard, at least until the number of receptors is up regulated back to normal levels.
    i learned something different; nicotine's narcotic properties have little to do with the nicotinic receptors. its stimulatory properties, yes, it targets nicotinic receptors better than ACh, but this really doesn't do much damage (the mechanism is similar to succinylcholine), and does not contribute to addiction.
    the addiction of nicotine comes from the fact that the molecule it is lipophilic (whereas ephedrine is hydrophilic), and can go into the brain, and it does. it stimulates the reward center of the brain, which is why it can cause addiction. smoking is dangerous not from teh nicotine doing damage, but rather the carcinogens of burning tobacco, and that nicotine addiction makes you smoke in more carcinogens

    this is also why speed (a methamphetamine) is addictive. methamphetamine structures look like ephedrine, but it lacks the hydroxyl group. b/c it lacks the single hydroxy group that ephedrine has, it goes into the brain, and causes addiction. (this is why it is illegal to sell pure ephedrine; some simple reactions can turn ephedrine into speed or crystal "meth").

    summary: addiction/"downregulation"/hormonal negative feedback, in almost all cases, is caused by lipophilic molecules (like steroids, nicotine, and speed), b/c only lipophilic molecules can reach the brain and screw up your natural regulation of hormones
    "No one can completely believe that I am natural.
    The most important drug is to train like a madman
    -really like a madman
    The people who accuse me are those who have never trained once in their life as I train every day of my life."

    Alexandr Karelin
    Ten-time World Greco-Roman Champion
    1988, 1992, 1996 Olympic gold medalist

    current stats (10/19/03): 20yrs, M, 5'4 @160lbs, ~11% body fat
    lifted since march 2000
    occupation:MCB major @ uc berkeley

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    Wannabebig Member Podium Kreatin's Avatar
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    meth (completely lipophilic, reaches brain, causes downregulation)
    http://chemfinder.cambridgesoft.com/...molid=537-46-2
    ephedrine (OH group makes the molecule impermeant to the brain, insignificant effect on regulation)
    http://chemfinder.cambridgesoft.com/...molid=299-42-3
    Last edited by Podium Kreatin; 03-18-2004 at 04:49 PM.
    "No one can completely believe that I am natural.
    The most important drug is to train like a madman
    -really like a madman
    The people who accuse me are those who have never trained once in their life as I train every day of my life."

    Alexandr Karelin
    Ten-time World Greco-Roman Champion
    1988, 1992, 1996 Olympic gold medalist

    current stats (10/19/03): 20yrs, M, 5'4 @160lbs, ~11% body fat
    lifted since march 2000
    occupation:MCB major @ uc berkeley

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    16 inches of pure passion Khar's Avatar
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    Thanks everyone for the info thus far. I was searching around for some other info on down regulation and so on and so forth. And I came across the Clen Handbook that zwarrior posted in the anabolic forum. Clen is a beta antagonist just like ephedrine, and here is a quote from the thread.

    Ketotifen is safe antihistamine used extensively some European countries to
    treat asthma and allergies. It can up regulate beta-2-receptors that Clen down
    regulates.
    IF ephedrine does down-regulate at all even if it is to a minute degree, would this Ketotifen regulate the receptors again? And where would one get Ketotifen?

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    Wannabebig Member Podium Kreatin's Avatar
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    Quote Originally Posted by Khar
    IF ephedrine does down-regulate at all even if it is to a minute degree, would this Ketotifen regulate the receptors again? And where would one get Ketotifen?
    lets relook at some concepts again:
    the mechanism of action of a drug is not the same as mechanism of the side effects of that drug. what this means is that clen and ephedrine are both beta-1,2 agonists, but the side effects they cause are not from their ability to agonize on these receptors.

    lets take a real, simpler example
    salicyclic acid was isolated from a tree, and was used to treat headaches. but, a side effect was upset stomach. it was also used for rheumatoid arthritis, but you needed tons of dosage to relieve the symptoms, which was really harsh on the stomach
    then, somebody decided that he can make a small change to the chemical, and maybe keep its analgesic property, but get rid of the side effects. he tried to add acetyl anhydride (a small compound) onto salicyclic acid, and then he invented aspirin (he also did the same thing to cocaine and invented heroin).
    both aspirin and salicyclic acid have the identical mechanism of action (it is a COX inhibitor) as a analgesic, but different side effects.

    so, "IF ephedrine does down-regulate at all even if it is to a minute degree, would this Ketotifen regulate the receptors again?" probably not, b/c they are different drugs, and they don't cause side effects the same, and to fix their side effects, you may need two different methods

    sorry for the long lecture, but i hope my explanation helps. i could be wrong tho about some things tho, b/c i haven't fully developed my knowledge of pharmacology (undergrad)
    Last edited by Podium Kreatin; 03-18-2004 at 07:58 PM.
    "No one can completely believe that I am natural.
    The most important drug is to train like a madman
    -really like a madman
    The people who accuse me are those who have never trained once in their life as I train every day of my life."

    Alexandr Karelin
    Ten-time World Greco-Roman Champion
    1988, 1992, 1996 Olympic gold medalist

    current stats (10/19/03): 20yrs, M, 5'4 @160lbs, ~11% body fat
    lifted since march 2000
    occupation:MCB major @ uc berkeley

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    16 inches of pure passion Khar's Avatar
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    I still am not quite grasping you fully. From what I *see* you are trying to equate to my ephedrine-ketotifen thoughts to something along the lines of coated vs un-coated tylenol. Or something to that effect. You are saying thatt acetyl anhydride and salicyclic acid form aspirin which does the same thing as salicyclic acid by itself, but because of the chemical combination the side effects of the lone salicyclic acid are nullified. Ephedrine is drug A and and Ketotifen is drug B. Drug A causes a reaction and drug B is used to counteract that reaction after drug A is no longer being administered. So I don't totally grasp why this wouldn't work. Sorry I'm probably just confusing anyone reading this thread but I still don't understand.

    About the cocaine and heroin though...heroin has nothing to do with cocaine. Heroin is synthesized from the opiate alkaloids codeine, papaverine, noscapine, and morphine. Whereas cocaine is synthesized from the coca plant. www.erowid.org for that info.

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    Steak and Eggs pusher's Avatar
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    If ketotifen increases the expression of b2 receptors independent of anything else, then it shouldn't matter why or what caused them to be in low abundance in the first place. But I believe clen is a selective b2 agonist, ephedrine is not (could be wrong).

    Clen basically results in a faster effect/response of b2 receptors than ephedrine, meaning: Because Your body doesn't like to be over or under its normal functional levels of anything, it reacts, trying to reach its equilibrium.It has many ways of doing this, as I've proposed in this case, reducing the number of receptors on its target cells Clen does this faster then ephedrine, you do develop a tolerance, and the stimulant becomes less effective.

    Review

    NOTE: the brain is not what you are targeting when you take ephedrine, it doesn't matter if it gets there or not. You want it to stimulate muscle and adipocites.

    Ephedrine stimulates agonist release/production and acts as an agonist itself.
    Ephedrine has ~40% of its stimulation on the beta-3 sites. Ephedra also additionally stimulates beta-1 and beta-2 receptors. Receptors bind b-agonists. When a b-agonist is bound to a b- receptor, the receptor initiates a series of chemical reactions that results in the production C-AMP inside the cell membrane. Ephedrine by itself is mildly effective because of the negative feedback system. Thats why CAFFEINE was added to the mix. And yet why do people develop a tolerance? Downregulation I'd say.

    OK, SO

    Clen quickly looses its thermogenic effects because your body reacts to the flood of agonists by trying to keep them from causing a response in the cell. The way it does this, is by reducing the number of gates where ligand receptor interaction take place.*** I shouldn't have refered to this as an addiction. GENE EXPRESSION IS VERY SENSITIVE.

    Sorry to be all over the place with the response, I'm having trouble explaining things clearly. What concerns me is the expression of these proteins, and the long term effects of suppressed normal function.

    Back to your original question, not sure. But your body is very smart and efficient and likes things a particular way. Logically, I would expect Long term effects of constant exposure. Its like people who stop consuming milk and develop lactose intolerance because they NO LONGER PRODUCE the enzyme required to digest lactose. It could happen.
    "The highest reward for man's toil is not what he gets for it, but what he becomes by it." -John Ruskin 1819-1900

    "He who fights monsters should see to it that in the process, he does not
    become a monster. And when you look into the abyss, the abyss also looks into
    you." - Nietzche

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    16 inches of pure passion Khar's Avatar
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    Ok I understand what you are saying now. But as it was worded in the Clen handbook ketotifen up regulates the receptors...Now I don't know anything about this chemical so maybe it was worded incorrectly, or maybe you can up-regulate without being down regulated first. I'm just a peon trying to understand But I DO understand what you were saying now. So I'm not a complete stooge.

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    Wannabebig Member Podium Kreatin's Avatar
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    Quote Originally Posted by Khar
    I still am not quite grasping you fully.
    what i'm saying is, each drug works on its own way. lets look at another example

    ppl think that you can counteract alcohol w/ coffee, b/c alcohol is a depressant and caffeine is a stimulant. they are functional antagonists, which means that their function may be opposite, but they are not antagonists of each others. coffee wil make you less drunk, it will also make you dehydrated. caffeine is a phosphodiester inhibitor, alcohol works by solubilizing into cells. this is why its not a good idea to counteract alcohol w/ caffeine; they don't antagonize on each others, but rather, two totally different pathways. also, alcohol and caffeine are both diuretics, but again, not via the same mech!
    so, int eh case of clen and ketotifen, yes, they are independent reactions. hence, using one drug to "solve" the side effects of anotehr is a bad idea imo, b/c it creates a "perceived" fix, but you're just making more problems. think of the alcohol/coffee example.
    About the cocaine and heroin though...heroin has nothing to do with cocaine.
    my mistake, i meant morphine and heroin
    http://chemfinder.cambridgesoft.com/...?molid=57-27-2
    http://chemfinder.cambridgesoft.com/...molid=561-27-3
    Last edited by Podium Kreatin; 03-19-2004 at 01:00 AM.
    "No one can completely believe that I am natural.
    The most important drug is to train like a madman
    -really like a madman
    The people who accuse me are those who have never trained once in their life as I train every day of my life."

    Alexandr Karelin
    Ten-time World Greco-Roman Champion
    1988, 1992, 1996 Olympic gold medalist

    current stats (10/19/03): 20yrs, M, 5'4 @160lbs, ~11% body fat
    lifted since march 2000
    occupation:MCB major @ uc berkeley

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    Wannabebig Member Podium Kreatin's Avatar
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    ok, i looked at some other posts here, and i think there is soem confusion

    let me repeat
    mechanism of a drug is NOT the same mechanism which causes the side effects! clen's mech is that it is a beta-agonist. BUT, if it downregulates the beta receptors, it is NOT from the fact that it agonized on the receptor! this is a very important concept in pharmacology, and this is why i brought up the aspirin/salicyclate example. they relieve pain b/c they both inhibit COX, but salicyclic acid causes side effects (stomach upset) by an UNRELATED mechanism.
    just b/c ephedrine and clen are both beta-agonists doesn't mean they have the same side effects. if side effects were the same in different classes of drugs, tehn there would be no business for pharmaceuticals. the purpose of pharmacology research is developing new versions of current drugs, but w/ more specificity and less side effects. there have been patents involving only one constituent change in two drugs, b/c sometimes, a small change in a molecule will keep the same drug effects, but will have different side effects (eg. Bayer patented aspirin with their very simple one-step reaction with salicyclate)

    btw, can u guys see the chemical links i posted? i dunno if u need to sign up (its free from my knowledge)
    "No one can completely believe that I am natural.
    The most important drug is to train like a madman
    -really like a madman
    The people who accuse me are those who have never trained once in their life as I train every day of my life."

    Alexandr Karelin
    Ten-time World Greco-Roman Champion
    1988, 1992, 1996 Olympic gold medalist

    current stats (10/19/03): 20yrs, M, 5'4 @160lbs, ~11% body fat
    lifted since march 2000
    occupation:MCB major @ uc berkeley

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    Party of "No." Tryska's Avatar
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    no ones talking about side effects tho podium. they are talking about down -regulation of the very receptors that are being affected.
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    16 inches of pure passion Khar's Avatar
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    I can see the posts. I understand what you are getting at the with mechanisms of the drugs now.

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    Wannabebig Member Podium Kreatin's Avatar
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    Quote Originally Posted by Tryska
    no ones talking about side effects tho podium. they are talking about down -regulation of the very receptors that are being affected.
    well, a side effect is any other additional drug effects that are not its main purpose. im just saying that downregulation of clen may be a side effect of that drug, and shouldn't imply that ephedrine wil downregulate as well. its possible to stimulate the adrenergic receptors w/o resulting in the decrease of the number of receptors available. look at our body's natural neurotransmitters like epinephrine. if we lift heavy weights, our epinephrine goes up to allow us to push the weights. but does lifting on a daily basis mean that our adrenaline rush will decrease through time, b/c high blood epinephrine results in a decrease of beta receptors? no. epinephdrine, clen, and ephedrine all work the same way in its ability to work on the beta receptors, but have different downregulation activity.

    lets look at another example: aspirin is used to prevent heart attacks. if somebody takes like 2 aspirin a day, then skips one day, will he have a sudden increase in his chance of heart attack b/c his body became dependent on aspirin's ability to prevent heart attack? well no, b/c aspirin's ability to downregulate COX doesn't cause our body to upregulate production of COX enzymes to counteract aspirin. same thing for ephedrine; i dont' think our body resists it. as for clen, i believe the downregulation is a side effect not related to its beta-agonist ability
    "No one can completely believe that I am natural.
    The most important drug is to train like a madman
    -really like a madman
    The people who accuse me are those who have never trained once in their life as I train every day of my life."

    Alexandr Karelin
    Ten-time World Greco-Roman Champion
    1988, 1992, 1996 Olympic gold medalist

    current stats (10/19/03): 20yrs, M, 5'4 @160lbs, ~11% body fat
    lifted since march 2000
    occupation:MCB major @ uc berkeley

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