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Tanning drug for skin cancer prevention


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#1 goku

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Posted 05 October 2005 - 07:06 AM


Has no one on this forum heard of Melanotan? It's a peptide in the third phase of testing from a pharmaceutical company in Australia called Epitan. It's being designed as a preventive for skin cancer -- Australia has the worst skin-cancer prevalence in the world which is why it's being developed there. It gives you an even, REAL tan by stimulating the melanocorticoids with synthetic melanin. It is also a very powerful aphrodiasiac, although it works much differently than something like viagra. It is also a thermogenic and a very powerful antioxidant. Check out the scientific literature on this peptide. Billions are floating around it's impending and tentative release scheduled in 2007 where you'll be able to get it by prescription. They'll have it in a transdermal and subligual form by then, as well as a very tiny subcutaneous implant for more serious requirements.

BTW, if you know people in the scientific R&D community, you can get your hands on lyophilized Melanotan right now. It has to be reconsituted with bacteriostatic water and injected subcutaneously, but it's painless, safe, and you can use BD-Ultrafine needles like the ones used by diabetics. The injection is only into fatty tissue immeidately under skin -- no blood injecting.

I use and believe me, this stuff works.

#2 goku

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Posted 05 October 2005 - 09:32 AM

In terms of the science behind MT-II, I feel an obligation to provide some direct source for easy viewing.

So for starters, here's a scientific abstract from Pub Med database. But first, here's the link to validate it:

http://www.ncbi.nlm....2693&query_hl=2


Effects of a superpotent melanotropic peptide in combination with solar UV radiation on tanning of the skin in human volunteers.

Dorr RT, Ertl G, Levine N, Brooks C, Bangert JL, Powell MB, Humphrey S, Alberts DS.

Department of Medicine, Cancer Center Division, University of Arizona, Tucson, AZ, USA. bdorr@azcc.arizona.edu

OBJECTIVE: Three phase 1 clinical trials of a superpotent melanotropic peptide, melanotan-1 (MT-1, or [Nle(4)-D-Phe(7)]alpha-melanocyte-stimulating hormone) were performed to demonstrate safety for MT-1 therapy combined with UV-B light or sunlight. DESIGN: Open-label studies at 2 dose levels of MT-1 combined with small doses of UV-B to the neck or buttock or full sunlight to half of the back. SETTING: Dermatology clinics at the Arizona Health Sciences Center, Tucson. INTERVENTIONS: The first study randomized 4 subjects to MT-1 (0.08 mg/kg per day subcutaneously) and 4 subjects to injections of isotonic sodium chloride (9%) solution for 10 days, followed by neck irradiation with 3 times the minimal erythema dose (MED) of UV-B light. In the next study (n = 12), the MT-1 dosage was increased to 0.16 mg/kg per day for 10 days, with UV-B radiation (0.25-0.75 MED) given to a buttock site for 5 days during (n = 7) or after (n = 5) MT-1 administration. A final study randomized 8 subjects to 3 to 5 days of sunlight to half of the back or to sunlight plus 0.16 mg/kg of MT-1 for 5 days per week for 4 weeks. RESULTS: Tanning in the first study was achieved in 3 of 4 subjects receiving MT-1, and these subjects also had 47% fewer sunburn cells at the irradiated neck site. More skin sites darkened with the higher dose of MT-1 in the second study. In the third study, there was significantly enhanced tanning of the back in the MT-1 group, and this was maintained at least 3 weeks longer than the tanning in the sunlight-only controls, who required 50% more sun-exposure time for equivalent tanning. MAIN OUTCOME MEASURE: There were no pathologic findings at any UV-B or sun-exposed sites in any subject. Toxic effects due to MT-1 were minor, consisting of nausea and transient facial flushing. CONCLUSION: Melanotan-1 can be safely combined with UV-B light or sunlight and appears to act synergistically in the tanning response to light.

Publication Types:
Clinical Trial
Clinical Trial, Phase I
Randomized Controlled Trial

PMID: 15262693 [PubMed - indexed for MEDLINE]

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#3 goku

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Posted 05 October 2005 - 10:19 AM

Here's yet another abstract on the neuroprotective attributes of Melanotan:

Here's the link, where you can read the full text article if you like:

http://www.ncbi.nlm....1111&query_hl=2

1: Eur J Pharmacol. 2003 Feb 21;462(1-3):179-83. Related Articles, Links


The potent melanocortin receptor agonist melanotan-II promotes peripheral nerve regeneration and has neuroprotective properties in the rat.

Ter Laak MP, Brakkee JH, Adan RA, Hamers FP, Gispen WH.

Department of Medical Pharmacology, Rudolf Magnus Institute of Neuroscience, University Medical Center Utrecht, Universiteitsweg 100, 3584 CG, Utrecht, The Netherlands.

The neurotrophic and neuroprotective potential of the alpha-melanocyte-stimulating hormone (alpha-MSH) analog cyclo-[Ac-Nle(4),Asp(5),D-Phe(7),Lys(10)]alpha-MSH-(4-10) amide (melanotan-II), a potent melanocortin receptor agonist, was investigated. The sciatic nerve crush model was used as a paradigm to investigate the neurotrophic properties of melanotan-II. Melanotan-II significantly enhanced the recovery of sensory function following a crush lesion of the sciatic nerve in the rat at a dose of 20 microg kg(-1) per 48 h, s.c., but not at a dose of 2 or 50 microg kg(-1). In addition, we observed that melanotan-II also possesses neuroprotective properties, as it partially protected the nerve from a toxic neuropathy induced by cisplatin. Thus, the present data for the first time demonstrate the effectiveness of the potent alpha-MSH analog melanotan-II in nerve regeneration and neuroprotection.

PMID: 12591111 [PubMed - indexed for MEDLINE]

#4 goku

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Posted 05 October 2005 - 10:20 AM

Here's another abstract from medline on the thermogenic (fatloss) effect of Melanotan. First, here's the link:

http://www.ncbi.nlm....5137&query_hl=2


J Endocrinol. 2004 Jul;182(1):123-32. Related Articles, Links

Unabated anorexic and enhanced thermogenic responses to melanotan II in diet-induced obese rats despite reduced melanocortin 3 and 4 receptor expression.

Li G, Zhang Y, Wilsey JT, Scarpace PJ.

Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville, Florida 32610, USA.

The effects of the chronic activation of the central melanocortin (MC) system by melanotan II (MTII) were assessed in chow-fed (CH) and high-fat (HF) diet-induced obese (DIO) Sprague-Dawley rats. Six-day central infusion of MTII (1 nmol/day) reduced body weight and visceral adiposity compared with ad libitum-fed control and pair-fed groups and markedly suppressed caloric intake in both CH and DIO rats. The anorexic response to MTII was similar in DIO relative to CH rats. MTII induced a sustained increase in oxygen consumption in DIO but a delayed response in CH rats. In both diet groups, MTII reduced serum insulin and cholesterol levels compared with controls. HF feeding increased brown adipose tissue (BAT) uncoupling protein 1 (UCP1) by over twofold, and UCP1 levels were further elevated in MTII-treated CH and DIO rats. MTII lowered acetyl-CoA carboxylase expression and prevented the reduction in muscle-type carnitine palmitoyltransferase I mRNA by pair-feeding in the muscle of DIO rats. Compared with CH controls, hypothalamic MC3 and MC4 receptor expression levels were reduced in DIO controls. This study has demonstrated that, despite reduced hypothalamic MC3/MC4 receptor expression, anorexic and thermogenic responses to MTII are unabated with an initial augmentation of energy expenditure in DIO versus CH rats. The HF-induced up-regulation of UCP1 in BAT may contribute to the immediate increase in MTII-stimulated thermogenesis in DIO rats. MTII also increased fat catabolism in the muscle of DIO rats and improved glucose and cholesterol metabolism in both groups.

PMID: 15225137 [PubMed - indexed for MEDLINE]

#5 mnosal

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Posted 05 October 2005 - 12:26 PM

Goku, I'm curious if you're currently using "Mus***-Res*****" product ?
If so, what dose & what kind of dosing schedule ED, EOD

#6 canz

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Posted 05 October 2005 - 01:14 PM

I'm interested in this as well. I remember seeing this somewhere else, but the information was choppy and unreliable.

#7 xanadu

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Posted 06 October 2005 - 12:15 AM

At first I thought you were talking about melatonin until I took a second look at the word. Sounds interesting but I'm not going to try anything that has to be injected, even subcutaneously. Besides, this is in early testing phase. Goku, what were your experiences with this?

#8 iambhall

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Posted 06 October 2005 - 01:54 AM

Goku, where are you getting your lyophilized Melanotan?

#9 eternaltraveler

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Posted 06 October 2005 - 01:58 AM

I wouldn't trust most of the sources I have seen for this substance. As it is an injectable contamination is a MUCH larger concern.

#10 goku

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Posted 06 October 2005 - 01:59 AM

I'm lucky enough not to have to go through a middleman like Mus*** Res*****. I have geneticists in my family, and they can order direct from peptide manufacturers for cheap. There are a handful of dealers online with mixed results with people ordering from most of them. Melanotan only comes in a lyophilized (freeze-dried) powder right now which is extremely temperature sensitive. You have to know how to handle the peptide. It's also difficult to manufactur in the synthesizer compared to most peptides and there are several versions -- some only cure erectile dysfunction.

To answer another post, yes, Melanotan often gets confused with Melatonin -- NOT AT ALL the same thing, just similar spelling.

My experience with Melanotan is excellent. After two weeks of a loading phase of 2 mg ED (every day) reconstituted in bacteriostatic water I was starting to tan, and I'm very fair (type I skin) and have never really tanned before. Now I'm dark all the time and only require a maintenance dose of about 2 mg every 4 days or so. I didn't burn once this summer. That's what Melanotan is being designed for by Epitan in Australia -- to protect fair-skinned people from skin cancer. I haven't noticed any fat loss effect that is supposed to occur, but I'm very lean so that's probably why. I definitely also notice the enhanced libido. I've experimented wth viagra before, and this is stronger -- also works in a very different way if you read the scientific literature -- some American pharm companies who got on the Melanotan bandwagon a little late ar developing a version of the peptide that doesn't tan but still has the libido enhancing effect to market it as that and not infringe on Epitan's patent. There's currently a lot of competition with this peptide. And even some analogues in the works.

By 2007 or perhaps 2008 a transdermal or sublingual or pill version (probably all three actually) will hit the market, although you'll likely need a prescription for any version. Right now, you indeed have to inject, but subcutaneous is a very superficial injection. Diabetics do subcutaneous injections constantly. You don't even feel them and there's no blood if you do it right. You're going JUST under the skin into the adipose tissue (fatty tissue). It's truly no big deal at all. It's not intramuscular inj. or intravenous which is what most people think of when they think injection. The needles are so small and fine you don't even feel anything and they go in like half a centimeter.

Injection is actually far safer than swallowing pills which the liver has to process. If anyone here knows anything about anabolic steroids for instance, you'll know that it's the pill versions that are by far the most dangerous; the 17 AA's wreak havoc on your liver and kidneys. Injection is always used throughout the medical industry -- not pills -- think when you go to the hospital. Injection is actually what IS safe once you know how to do it b/c you're not infering with your digestive system nor putting strain on your liver. It's a far more efficient vector no matter what you're taking. And in terms of danger -- the peptide is lyophilized (meaning very, very, very frozen when you get it) and you reconstitute with bacteriostatic water (like saline -- if you wear contacts you'll know what I'm talking about -- but much stronger antispetic) -- it's extremely clean. Besides, I get mine right out of a standardized synthesizer, so there's no concern for me anyway. But in general, when people express paranoia about injection, it's groundless. Unless you're buying something in a ready state for actual injection from some middleman -- yes, that would scare me too.

#11 goku

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Posted 06 October 2005 - 02:00 AM

No contamination is not an issue for me. And if you mean bacterial contamination of any kind, you don't even understand what Melanotan is.

#12 goku

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Posted 06 October 2005 - 02:04 AM

No contamination is not an issue for anyone who uses melanotan unless you buy it already reconstituted -- which you never should, nor does any supplier I have ever heard of do that -- b/c once reconstituted Melanotan degrades rapidly. So if you mean bacterial contamination of any kind, you don't even understand what Melanotan is, b/c bacterial infection would be impossible unless YOU, in actually handling melanotan, were to contaminate it -- which again, you'd have to be incredibly careless to do so. If you mean toxic metal contaminants in parts per billion, that again is a non-issue with peptides. That doesn't happen in peptide synthesizers.

#13 goku

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Posted 06 October 2005 - 02:14 AM

For the earlier question, as concerns dosing, it depends on your body weight to some degree, but you're looking at a loading phase like i earlier mentioned to build up the substance in your system and while you acclimate to it. You need about 30 mg to do a small cycle and get properly tanned at first if you're quite pale genetically.

In terms of some people being worried about after effects of Melanotan b/c it's so new, that's understandable. But, like I said, I have two family members who are geneticists who use, and they've read all the literature on this -- not just skimming abstracts on some database. And I've read dozens of reports. Also, Epitan has been in phase IIIb testing for quite a while. Thousands of people have used for the company in experiments with safe and good results across the board. In fact, the more studies done, the more excited people are getting about the surprising new effect of melanotan like it's antioxidant activity, its thermogenic effect, and it's very powerful effect at curing ED. I'm young, so maybe it's partly that, but I get remarkable erections with this stuff. I'm in social circles where lots of people use all sorts of stuff, and frankly, many nootropics scare me more than melanotan, especially when people mix different noops for the synergistic effect. Not that it's toxic per se, it's just the random way you're tampering w/ the complicated interactions of neurotranmitters. However, I'd be hypocritical to preach against Noops -- i love noops -- so do about half the biologists who are in the know out there -- many still think they're way too primitive right now. When he CREB drugs hit the market it'll be a different story. Helicon and NeuroLogic have some really cool stuff that might make it through the long and arduous road to actual release.

Anyway, melanotan has been a good experience for me and the people I know who've used it.

#14 goku

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Posted 06 October 2005 - 02:16 AM

BTW, the earlier post about muscle research, I've heard mixed reports about their MT-II if you're curious -- some satisfied customers, some not. I know better sources for sure.

#15 eternaltraveler

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Posted 06 October 2005 - 02:25 AM

b/c bacterial infection would be impossible unless YOU, in actually handling melanotan, were to contaminate it


Peptide gets made by some likely less than legitimate source. Gets shipped out to distributors, distributors repackage, and send to you.

You're telling me that it's not just unlikely, but impossible for bacteria to enter the mix at any point in this process?

All I'm saying, is that if you are going to inject something, into your body, past all external lines of defense you should be sure of exactly what is in it.

I've seen assays of this substance from several sources. Non of them that I saw was above 80% of the desired peptide. There was 20% or more of something else in all of them. Now it's been awhile since I've looked into this at all, perhaps things have changed.

If you have an infallible source, that's great. Are you a source?

#16 eternaltraveler

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Posted 06 October 2005 - 02:29 AM

melanotan II also has the side effect of acting as a sexual stimulant

#17 goku

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Posted 06 October 2005 - 03:29 AM

No, like I said, I get mine direct. And even the suppliers on the web (there's only a handful who can get this) have HPCL and other pertinent documentation to attest to a purity of >95%. I have never seen less than this much and I've ordered from a few of these sources before I found my current source. And yes, I am telling people that if they get it lyophilized, you can't get infected b/c again, you have to reconstitute with bacteriostatic water and the fact that it's lyophilized and in an aerobic environment means safety. But if you order from a sketchy source or someone who only offers 80 % purity (which I've never heard of b/c that is terrible) I'd be worried -- not for bacteria but b/c the MT-II was not made in a standardized synthesizer of it's below 90% pure (90% is even low), b/c 80% is way too impure and I doubt it would be stable and survive. It's a very sensitive peptide to temperature.

As to whether I am a source, I could be, although I'm not really looking to become a dealer at all. I have a lot of the peptide right now, but there's no way I could supply dozens of people right now. As I said, I get mine from my geneticist family members, and they are not going to order tons of the stuff for me to redistribute -- they would be aghast if they found out. They use it, and they got me into it, but they're certainly not suppliers.

If a few people (10 or <) needed some, I could supply that, but that would be it. I could also recommend decent sources. They'd be more expensive though b/c most people selling sell 10 mg for about 150 USD or more. When you order it from the actual manufacturer it's much cheaper.

#18 eternaltraveler

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Posted 06 October 2005 - 09:23 PM

I may have been misunderstood. The assays I've seen were not posted by the sources themselves, but were tested independently (the reason for this is secondary sources bought them and had them tested because their customers complained that it wasn’t working).

This discrepancy is most likely due to the fact that the peptide IS unstable, and the other 20% is probably mostly the breakdown products of it (therefore the original >95% purity could be quite accurate).

I am merely urging those on this forum to be very careful of what they inject into their bodies of something not made by a pharmaceutical company.

#19 goku

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Posted 07 October 2005 - 08:57 AM

Yeah, I understand the concern for people if they're ordering from email address sources -- who knows how or where they're getting their melanotan from.

#20 goku

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Posted 07 October 2005 - 10:08 AM

Melanotan works. And it's the only substance icurrently in existence that will actually induce a tan in a person until analogues are developed which is many years away cuz those new drugs will have to go through the long and arduous journey of drug clearance -- usually 10 years -- although some analogues are currently in the works to compete with Epitan's cornering of the market in 2007-8. I'm just glad to be tanned now, cuz I can never wait for this stuff to hit market once I know about it. BTW, kinda off topic, but they got this really article just came out in the online Scientific American Minds about new notropics in the works.

#21 xanadu

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Posted 07 October 2005 - 08:22 PM

You know what might be interesting? I was just thinking that since you only need a small amount, like 2mg, why not do your own transdermal system? You could do it with that solvent, whose name escapes me at the moment, the one that reduces joint pain and is used to deliver some other substances. Just mix up your stuff and let it sit on your skin. Dosage might be a little tricky at first until you got the hang of it. Other solvents might be usable. Aren't some skin creams sold that contain transdermal substances in them? Just mix a little of this in with a cream like they are trying with idebenone.

#22 wannafulfill

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Posted 07 October 2005 - 10:06 PM

$$$ is why

#23 goku

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Posted 07 October 2005 - 11:38 PM

MT-II is expensive. The analogue MT-I -- which is a bit more potent for tanning, is even more expensive -- that's why everyone uses MT-II instead -- more economical. But yeah, Melanotan is expensive. Just check out the main underground suppliers in the world @ Melanotan.org. Very few suppliers below 150 USD per 10 mg. But I get it so cheap I can part with it for 90-100 USD per 10 mg to make a resonable profit to make the hassle and risk worth my while -- but that's still too much for most people. However, after loading phase, using MT-II becomes way cheaper to simply maintain your tan. But you gotta build up the peptide in your system, which for very fair people means about 30 mg to get a solid tan -- that's just the reality of using MT-II. If you can't afford at least 25 mg all at once, you're wasting your money -- you won't be tan before 25 mg, even with conjuncting usuage with a solarium or just getting lots of sun (which is recommended to expedite intial tan -- after your tan administering the drug alone will maintain tan).

I don't know about being able to simply mix something into the peptide to make it transdermal. I really doubt it's that easy, but I'm not well versed in that kinda molecular modification for a different vector. Frankly, it can't be that easy or other suppliers would have done that or advised that method cuz they could sell a lot more peptid b/c people are so paranoid about needles -- even the tiny BD Ultrafine II needles used for subcutaneous inj.

Anyway, I got lots of people telling me they WILL (but not now) order after they save up. So who knows. I've only got two people who actually buy off me that aren't my local friends.

#24 xanadu

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Posted 08 October 2005 - 07:47 PM

goku, it has nothing to do with molecular modification. I was talking about using a solvent such as dmso or perhaps something even better. These substances will go right through the skin and carrying into the body anything that is dissolved in them. There are transdermal creams that use something else to do the same thing.

Good luck with your business.

#25 goku

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Posted 08 October 2005 - 10:51 PM

Ok, but by mixing the MT-II peptide with a solvent like dmso, even using something like sonification I'm not sure the peptide would dissolve -- also, dmso might very well affect the molecular structure of the peptide -- it degrades extremely rapidly in warm temperatures. I think a more stable form of the peptide needs to be made before it could be mixed with a solvent and survive the process.

Again, I might be wrong, but it's unlikely b/c I know biocemists who use, and they would have propisitioned something like that if it was that easy. Believe me, people have considered this possibility before. Others have suggested enteric coatings a capsule form for oral administration. But even getting the peptide through the stomach acids, it would never make it through the liver. Someone else mentioned sublingual administration, but the peptide won't pass the membrane under the tongue.

But hey, if you figure out how to modify the peptide to use one of these routes, you could be the most successful underground dealer out there. Even Epitan has had to use an implant that gradually releases the peptide direct into the bloodstream for experimentation instead of a transdermal cream. If they can't do it yet -- god knows why -- I'm not sure who can.

#26 bossplaya

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Posted 17 October 2005 - 11:08 PM

I've read that MT-II is also being considered as a replacement for Viagra, because it induces spontaneous erections. Not that I am interested in that kind of effect; it would be more annoying than anything else, to suddenly 'crack a fat', 'get a stiffy' (As the Aussies say), or get a spontaneous erection in public, at work, or in some other awkward type of situation. I've never had any trouble getting it up in the first place.

But for its tanning effects, yeah, that sounds desirable. So either way it is marketed, if as an impotence drug, the side effect will be a tan. If marketed as a tanning drug, the side effect will be sexual stimulation.

#27 goku

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Posted 21 October 2005 - 03:14 AM

They actually have analogues in the works to isolate the impotence alleviating element without inducing a tan in order not to infringe on Epitan's patent.

I don't mind the erections at all, even though I'm young. But yes, they are pretty random. I just like being tanned year round which is why I use and Melanotan is also highly neuroprotective which is the main reason I mentioned it on this forum. I don't know how it compares to the other noops exactly, but the neuroprotective effects are substantial according to the scientific literature.

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#28 liorrh

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Posted 03 February 2006 - 11:15 PM

what about body compositon effects (effects on lean mass, fat mass)?




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