48 replies to this topic

[edward]

AMPK activators (peripheral that is) are pretty cool in my opinion so I am interested in adding a few to see the effects on my endurance and other aspects of my fitness. If anyone needs a crash course just do some google searches on AMPK activation and throw in AICAR to the searches as it has had a lot of press recently and you should get some pertinent info.

Ok ill start off the list

natural activators:
Exercise
CR
Low Carb diet

supplements/drugs:
AICAR
Metformin
Guanidinopropionic acid (GPA)
Creatine
lipoic acid
resveratrol

Edited by edward, 28 September 2008 - 04:45 AM.

[niner]

supplements/drugs:
AICAR
...

Would this list also include the PPAR-delta agonist GW1516, a not terrifically complex thiazole? Seems like it might from a quick read, and it would be cheaper in principle, though possibly not in practice, than AICAR (aminoimidazole carboxamide ribonucleotide).

[edward]

supplements/drugs:
AICAR
...

Would this list also include the PPAR-delta agonist GW1516, a not terrifically complex thiazole? Seems like it might from a quick read, and it would be cheaper in principle, though possibly not in practice, than AICAR (aminoimidazole carboxamide ribonucleotide).

Yes, although GW1516/GSK-516 is coming at it from a different angle through PPAR-delta some of the effects would be the same.

PPAR-delta agonist + say Guanidinopropionic acid (GPA) (available and not that expensive) and we have a cheap exercise in a pill or at least when combined with aerobic exercise could make the weekend warrior capable of making tremendous gains (endurance and cardiovascular/over all health), however I think GSK will prevent GW1516 from being available anytime soon even though it is apparently a simple compound as they are developing it as a prescription drug.

PPAR delta agonist + AICAR would probably be better but yes it seems that AICAR is not cheap to produce.

So the ideal choice of AICAR+GW1516 seems to be out of reach.

As far as PPAR agonists readily available there are sesamin and Tetradecylthioacetic acid (TTA)... sesamin is mostly a PPAR-alpha agonist which is good but not as great as a selective PPAR-delta agonist would be. TTA supposedly has PPAR-delta activity but also has PPAR-alpha (good) and PPAR-gamma (not so good) activity.

GPA + TTA would be a currently available crude version of the AICAR +GW1516 combo touted to make a Tour de France champ out of Joe Couch Potato. The only big issue is TTA's effect on PPAR-gamma (if you agonize ppar-gamma you get fat cells gone wild, in a bad way), so a more selevetive PPAR-agonist would be needed. GPA is obviously not as good as AICAR and has its own problems.... (hence crude solution)

I admit I have only scratched the surface of this area as I have a lot of stuff going on in my life right now (so have not done the kind of research I would like on the subject) so anyone with more information than I please feel free to correct me and fill in the gaps.

Edited by edward, 30 September 2008 - 02:50 AM.

[niner]

Well, look at it this way: If GW1516 is relatively easy to make, I bet someone will make it, considering the stakes. I think that the doping agencies may already be on top of it, though.

[edward]

Well, look at it this way: If GW1516 is relatively easy to make, I bet someone will make it, considering the stakes. I think that the doping agencies may already be on top of it, though.

In so far as "doping" is concerned, the doping agencies are concerned more with whats in the athletes they have jurisdiction over not whats out there (caffeine, or sudafed used to be on the WADA list of banned substances, I think they are off it now except for very high blood levels). I no longer compete in athletics apart from the occasional race (your local 10k for some charity) or a club tennis tournament so "doping agencies" are of no concern to me, and in reality most consumers of performance enhancing substances are not professional athletes.

Edited by edward, 30 September 2008 - 03:55 PM.

[curious_sle]

Well, a test is arround now :-) reuters now i still wait for the supplement/drug to be available... would love to have more effect of the exercise i do. I kinda can't get a decent muscle mass so that would be welcome... (apart from the detail stuff)

[tunt01]

Add: Cucurbitane Triterpenoids - Chinese Bitter Melon

http://www.cell.com/...5521(08)00082-3


I've been looking for Bitter Melon around Chicago lately, if anyone knows where to purchase it locally (not in the pill form) let me know.

Or if anyone can find an equivalent product to Bitter Melon which produces these Cucurbitane Triterpenoids, please post it.

[Shepard]

The EGCG:

http://www.jbc.org/c...ll/282/41/30143

[Shepard]

I will say that some factions of the supplement community have been playing around in this area with GPA and fibrates/sesamin for a while and nothing groundbreaking seems to have happened.

[neogenic]

The EGCG:

http://www.jbc.org/c...ll/282/41/30143

A new study shows it raises aromotase levels, thereby increasing estrogen and lowering testosterone.

[tunt01]

anyone ever look at chromium picolinate? often used for type 2 diabetes... maybe activates ampk ?

http://www.ncbi.nlm....pubmed/19298540

[Shepard]

A new study shows it raises aromotase levels, thereby increasing estrogen and lowering testosterone.

Yeah, I've seen it. There is conflicting data, and of course, it's mostly murine and in vitro research. The study you reference was looking at adipose, and others have found inhibitory actions in prostatic and ovarian aromatase levels. So, it could be tissue specific actions, or it could be due to differing strains of mice used, or any number of things.

[tunt01]

anyone know where we can buy gw1516 or AICAR? even if overseas?

seems like the ideal solution to me, the more i look into this issue.

[lbarber4]

anyone know where we can buy gw1516 or AICAR? even if overseas?

seems like the ideal solution to me, the more i look into this issue.

http://www.tocris.co...php?ItemId=5334

This place sells AICAR, 50 mg 74$!

Edited by lbarber4, 25 March 2009 - 05:42 PM.

[tunt01]

anyone know where we can buy gw1516 or AICAR? even if overseas?

seems like the ideal solution to me, the more i look into this issue.

http://www.tocris.co...php?ItemId=5334

This place sells AICAR, 50 mg 74$!

looks like I need 480 mg per every 2-3 days. seems a little out of my price league...

[Shepard]

Sustanon is cheaper.

[tunt01]

what is the biological difference between the two? i didnt think that AICAR was considered a steroid.

[Shepard]

It's not. I was just joking around, as I don't see nearly the potential in these drugs for exercise performance as some people do. Only advanced endurance athletes can afford to inhibit mTOR with an exogenous drug, and they wouldn't want to do that unless they want a short career ending with muscle atrophy.

[tunt01]

do you know if gw1516 is the same as the old gw501516 that caused intestinal polyps/cancer to form?

what would you dot increase ampk besides exercise? seems like the ideal pathway to target, imo.

[Shepard]

Yeah, they are the same drug. I wouldn't do anything other than exercise to mess around with AMPK other than standard dietary manipulation for the goal. I want it released in a pulsatile fashion. If I wanted to ramp up AMPK beyond normal, then I'd look to low-carbing and multiple training sessions daily.

Why do you think it will be so great?

That's not to say that this area doesn't play a role for people that can't or won't exercise. I'm speaking strictly from an athletic perspective, with the small exceptions I noted above.

Edited by Shepard, 25 March 2009 - 10:05 PM.

[tunt01]

i think what you say makes sense, im probably looking at it along somewhat similar lines.

from my perspective, im super pressed for time/busy working white collar professional.

- the bitter melon-type stuff is really too low in power to be considered a true pulsatile burst of ampk, it's more like maintenance on the basal metabolism. kind of like the difference between standing while talking on the phone or sitting down at my desk.
- the AICAR would be used in a short pulsatile fashion, i would eat in the AM, wait like 30-45 mins then do the stuff. let it run its course for 60-120 mins before really eating again, just drink a bit of water/green tea as needed.
- rest of day --> lunch -> work, work work --> gym/real workout (run) -> dinner -> 1-2 hrs of reading for work -> bed

so AICAR would give me 1 more workout during the day w/o having to actually do it.... it is time saving, just very COSTLY time savings. i can't justify even considering to do it on a constant basis at these price levels, but a month or two? maybe... i dont know. time will tell.

i guess the other issue is really -- what are my alternatives to try to generate that extra workout w/o actually leaving the office and doing it? other than maintain a very good fatty acid lipid profile and mess around w/ the other things in this thread, it's very limited.

i don't care about aesthetics so much as i care about optimizing human performance, so to speak.

Edited by prophets, 25 March 2009 - 11:26 PM.

[Shepard]

If people won't be dosing it round-the-clock, my concerns might be for nothing, anyway. It's not having much of an effect on AMPK levels in skeletal muscle in people:

http://diabetes.diab...db06-1716v1.pdf

Edited by Shepard, 25 March 2009 - 11:38 PM.

[Shepard]

what are my alternatives to try to generate that extra workout w/o actually leaving the office and doing it?

Such is the problem with focusing on endurance work. It takes a lot of time.

[Happy Gringo]

I use ECGC and forskolin together, then take I3C with meals to hopefully offset the increased estrogen.

[tunt01]

I use ECGC and forskolin together, then take I3C with meals to hopefully offset the increased estrogen.

forskolin seems like an interesting molecule. i had never looked at it previously.

it seems like it might be a decent alternative to melanotan, though transdermal application is more prone to human error than taking an injection or popping a pill.

i take I3C with meals and drink green tea all day already. might give forskolin a shot at some point.

Edited by prophets, 27 March 2009 - 04:34 PM.

[IronFanatic]

Hi guys, interesting discussion going on here. I've been lookin for logs of individuals already using these compounds, as they've been out for a while now, but alas to no prevail.

TLR is selling GW1516 and tocris and some others are selling AICAr at ridiculously inflated prices. Although, tocris doesn't sell to the general publc.

You guys mention pulsing the compound to limit sides. If i would say pulse aicar or GW, could i still expect some muscle atrophy as a trade off? Meaning will my anaerobic performance and muscular strength go down? and the aerobic performance go up?

Is it only GW 1516 that converts Fast twitch fibers to slow twitch fibers or does Aicar do this as well? since gw is through the ppar delta...

Upon cessation of said compound, will the ratio of slow twitch and fast twitch fibers revert back to baseline or will they remain permanently altered?

Finally, Is there any endurance benefit to pulsing small amounts of Aicar or GW.. say 5-10 mg per day? As liver toxicity may be an issue?

[tunt01]

I'm not an expert on this subject, but here are my thoughts:

1. GW1516 definitely triggers cancer in the intestinal tract and was abandoned by its lead drug sponsor for that reason. All the PPAR targeting drugs have serious cancer risks, you have to be ultra careful.
2. AICAR is inflated for a reason. It likely doesn't cause cancer and works.
3. Pulsing makes sense because that's how your circadian rhythm works. Who the hell runs for 16 hrs a day and sleeps for 8 hrs? You work out, you eat/rest, that's how life works.
4. AICAR should convert as well.
5. It will revert back if you never exercise and sit on your fat ass, then you are reprogramming your muscles back to laziness.
6. Pulsing small amounts, probably helpful, but I've no idea how much. I'm not clear on dose, the dose #s I've seen are all over the map. I'm not even entirely sure what an ideal dose is for someone even if they did take the optimal amount. If you are dose in small amounts, then I would probably guess it is more cost effective to use the other items in this thread, like eating bitter melon.

[IronFanatic]

Yeah, that makes sense. But i think shepard has it nailed down. For the sedentary sloth, this indeed may be a Godsend. But for an athlete, this may end up being more destructive than useful, unless used extremely wisely and with proper protocol. As the risk of atrophy seems quite great. And one needs to always maintain a proper balance of muscular strength to endurance. Sacrificing one for the other is certainly not an option. Converting too many fast twitch to slow twitch will negatively impact speed and stength. Which is a no no. You're essentially sacrificing athleticism for sustained endurance. I hope this isn't the case but it definitely appears that way. which is really a shame, since if you could keep the strength and speed and add that amount of endurance as well--- Wow!
yeah, you can't have your cake and eat too. I guess its no alternative to EPO.

[motomatt]

do you know if gw1516 is the same as the old gw501516 that caused intestinal polyps/cancer to form?

Peroxisome proliferator-activated receptor-b/d (PPARb/d) ligands do not potentiate growth of human cancer cell lines

[carlosuseche]

It's not. I was just joking around, as I don't see nearly the potential in these drugs for exercise performance as some people do. Only advanced endurance athletes can afford to inhibit mTOR with an exogenous drug, and they wouldn't want to do that unless they want a short career ending with muscle atrophy.

Inhibit mTOR? (rapamycin, a drug known to alleviate the effects of a faulty AKT pathway..... and immunosuppressant drug that turn off mTOR)

Could AICAR be used instead of rapamycin (maybe in autism!)?