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GHRP-6 and Hexarelin

By Anthony Roberts

 

Earlier this year, I was interviewed by a major online bodybuilding site (the interview was titled “Chemically Insane”), and in that interview, I predicted that various peptides would become the newest trend in performance enhancing drugs. For the most part, I was correct, and now they’re very popular and widely available, although still relatively new.

So, several months ago, I began my experimentation with various peptides, mostly with the goal of figuring out the best way to use them. My last major article examined my experiences with the two most popular peptides (IGF and MGF) currently on the market. This time around, I’m going to tell you about my experience with Hexarelin and GHRP-6, two lesser known peptides. With Lr3IGF-1, the use and goals of use is pretty straightforward…you pretty much use it to gain muscle and lose fat; on rare occasions, people use it to rehab an injury (I actually provided a full rehab protocol using IGF-1 in my first e-book). With MGF, it’s even simpler…you use it to increase muscle size, period.

Using the other peptides is a bit more complicated, and there are a couple of other reasons you might want to consider using them…but I’m getting a bit ahead of myself. The first thing I do when I’m researching a new anabolic is to jump on the internet and do some research in all of the available medical databases, and exhaust every search engine imaginable with keywords related to the new compound. The next thing I do is typically to get a couple of vials and try it for myself. I’m in a very unique position with regards to trying new compounds; in the case of several compounds (Esterless Boldenone, Masteron Enanthate, Stealth Injectables, etc…) I was actually able to try the products before they were released to the general public. In the case of Hexarelin and GHRP-6, I have had the opportunity to experiment with them for the past few months.

When I first received my vials of GHRP-6 and Hexarelin, I did what most people probably do…I reconstituted them, shot first, and asked questions later. I thought it would be a great idea to fire up 600mcs of GHRP-6 just before a heavy max effort deadlift session. Bad idea. I have a 45 minute drive to my gym (I happen to workout at a military academy, where I coach), and halfway there, I started to get a bit hungry. No problem, right? We’ve all worked out a bit hungry…well, that’s what I thought at first. Then when I hit about 400lbs into my deadlifts, I started getting dizzy…I broke into a cold sweat, and I had to sit down. I rushed to get some simple carbs into my body as quickly as possible, thinking that I was going hypoglycemic. Ok…I wasn’t going hypoglycemic, but it was pretty bad. That workout was shot. Still, I was wondering if I could actually slip into some kind of severe hypoglycemia from a shot of GHRP-6…it certainly felt like I could.

So, naturally, I was interested, and did some experimenting. I waited a day and invited a friend over to my place…then I did another shot of 600mcg (split bilaterally, 300mcg into each leg, as a subcutaneous shot). Then we sat around and waited, with a bunch of simple carbs ready. I got hungry, I was uncomfortable, and it wasn’t too much fun, but we sat there for a good couple of hours, and I didn’t pass out (in case you’re wondering, the friend was there to drive me to the hospital, in case I actually did pass out). Ok…so that settles that. Originally, I thought that maybe GHRP-6 operated by inducing some kind of mild hypoglycemia (hypoglycemia increases GH output). But that’s not how it actually works…

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Growth Hormone Releasing Peptide- 6 (GHRP-6) is a synthetic hexapeptide which stimulates the release of Growth Hormone. It accomplishes this by two totally separate mechanisms. On the one hand, it amplifies your body’s natural Growth Hormone Releasing Hormone (GHRH) signal transduction pathway, and on the other hand, acts as a functional antagonist of the hormone which causes inhibition of GH secretion (somatostatin) (1-3).

ghrp-6

GHRP-6 also has the benefit of being able to directly stimulate the anterior pituitary gland, resulting in increased GH release. So although my initial thoughts on the mechanism of action for this stuff was wrong, I was enthused when my research revealed that GHRP-6 induced GH secretion occurs by several mechanisms. Most importantly, those mechanisms are the induction of GHRH release from the hypothalamus,  stimulation of GH release from somatotrophs, joint actions of GHRH and antagonism of somatostatin, and finally by pronounced antagonism of somatostatin action on somatotrophs (1-4).  However, it bears clarification that GHRP-6 is not dependant on the GHRH pathway…it can boost your growth hormone levels without necessarily needing to elevate GHRH. This is important because if that pathway has been inhibited by long term GH use, GHRP-6 can still get your body producing and releasing GH.

Additionally, this peptide can also act on the central nervous system, (4) which can provide added benefits in neuroprotection as well as muscular strength increases for the user. Much of the strength increases we see with Anabolic Steroids in the Dihydrotestosterone family are suspected to be through a similar stimulation of the Central Nervous System. In my experience with GHRP-6 use, strength levels typically go up within the first week of starting out. 

BUY RESEARCH GHRP-6


Increases in Growth Hormone levels in the body are typically accompanied by strength increases, muscle hypertrophy (growth), and lipolysis (fat loss). Other results experienced with increased GH levels are recuperative effects on joints and injuries; connective tissue strengthening and bone mineral density improvements are commonplace. Enhanced GH secretion also leads to the liver secreting more IGF-1 (Insulin-Like Growth Factor 1), which is thought to be the primary anabolic mechanism of action for Growth Hormone. In the case of GHRP-6, I gained quite a bit of weight when I was running it at the 600mcg/day level. I think that this was probably due to overfeeding that almost always accompanied my shot contributed to this weight gain. I gained about 12lbs in 2 weeks. I think that the same way people often throw EQ into bulking cycles to increase appetite stimulation, I would suggest using GHRP-6 instead. It’s not anywhere near as anabolic, but the appetite increase is far above anything I’ve ever experienced with any anabolics.

The women I know who have used GHRP-6 all had to discontinue its use because it was making them gain weight too quickly. But then again, most of the women who I know are national level (or professional) physique competitors, and at most need an additional 5-10lbs of muscle at most. GHRP-6 just put too much weight on them too quickly.

After experimenting with GHRP-6 for weight gain, I lowered the dose substantially and used it to help rehab a knee injury that had been bothering me for a couple of years. In this case, I lowered it to 100mcg/day, shot sub-q into the knee (ouch!). At this dose you won’t find the extreme hunger that a high dose of it usually causes, and a 5mg bottle of GHRP-6 is going to last for months, and I’m confidant that it’s going to be enough to rehab virtually any injury (in my case, I had done extensive damage to my knee over the years, culminating in a traumatic injury playing on turf…which resulted in my semi-retirement from competitive athletics). Anyway, I combined GHRP-6 with a knee rehab protocol designed by Eric Cressey, M.A. C.S.C.S., and advice from one of my research assistants, who has a degree in Sports Medicine. Taken this way, I used GHRP-6, and rehabbed my knee to almost where it was prior to my beginning my career in athletics. If you have an injury, find yourself a good rehab protocol, and try a low dose of GHRP-6. I bet you’ll be surprised.

Oh…and this brings me to another point. I’m sure most people subscribe to the theory that peptides only last for a couple of weeks in their reconstituted form. Well, after I had my GHRP-6 reconstituted for well over a month, I tried a shot at my old 600mcg dose, and guess what happened? Yeah, I got a huge increase in appetite within the hour. This tells me that we’re really underestimating the amount of time that a reconstituted peptide can retain its potency. I’m betting we have months, not weeks.

Since GHRP-6 acts directly on the feedback loop which signals the inhibition of GH release, it has been used immediately following either GH or IGF-1 cycles, to recover natural GH production by inhibiting somatostatin action. It has also been used concurrently with those compounds to negate some of the effects of those compounds on natural GH production. Most people who use IGF never actually realize that as IGF is part of the hormonal cascade that GH initiates, it is also part of the Negative feedback loop for it. 

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Typical doses of GHRP-6 range from 100mcg/day injected subcutaneously (for connective tissue strengthening) to 500mcg/day (for an anabolic effect). After experimentation with a wide variety of doses, and input from several people who have also used the product, I think that 500mcg/day is the upper limit of effective dosing for GHRP-6.

The most rapid side effect experienced with GHRP-6 is extreme hunger, which typically occurs within an hour of injection. This could be due to a possible effect on blood sugar lowering, or more likely (I suspect) due to its influence on Ghrelin (5), stimulated by the peptide influenced release of GH. Ghrelin, by the way, increases appetite and speeds gastric emptying. This means…even if you weren’t hungry a second ago, and your Ghrelin levels go up too much…you’ll be starving soon.

If I were looking to figure out the best way to use GHRP-6 in a bulking cycle, I would simply take my favorite bulking cycle, and run GHRP-6 with it at a daily dose of 600mcg/day, shot post-workout. The reason for the post-workout dosing is to take advantage of the appetite stimulating properties, at the same time as taking maximum advantage of the anabolic properties of the GH release that it will cause. And I’d probably consider using some insulin as well, because insulin is highly anabolic on its own, but also because the GH response to GHRP-6 is elevated with concurrent use of insulin (6). Again, this is only how I’d do it personally, and I’m sure people will experiment with things and find the optimal way to get the results they want on an individual basis. GHRP-6 and this is no exaggeration, will put as much weight on you as nearly any steroid. If you’re not careful, you’ll gain too much fat…my recommendation is to use this stuff on your off season bulking cycles.

Overall, I was pretty impressed with GHRP-6, in my experience with it. Its ability to put weight on me was actually too potent, although the strength gains were nice. Now, I’ll mostly use GHRP-6 for post cycle therapy from IGF use, or when I need to get rid of an injury.

 I’ve never used Growth Hormone (let’s face it…it’s expensive, and Lr3IGF-1 + MGF is a much better buy), but when I used Hexarelin, I experienced most of the results that GH users report, but in much less time.  Out of the two GH secretagogues that I tried (Hexarelin and GHRP-6), Hexarelin is definitely my favorite. In my own personal case, I’m 28 years old right now, and not looking to add any more mass. I can comfortably maintain my bodyweight with my doctor-prescribed anabolics (I’m on permanent Hormone Replacement Therapy), and now I mostly focus on athletic-oriented goals. So strength gains without much weight, and maybe a bit of bodyfat loss, are my primary concerns. If I were in my early 20’s and still looking to gain weight, I’d probably be in love with GHRP-6, but for this stage of the game, I prefer the effects I’ve found with Hexarelin.

Hexarelin is a GH secretagogue, specifically a  hexapeptide which stimulates the release of growth hormone (GH) in both GH deficient as well as normal humans. When given by injection, plasma growth hormone concentrations increased (with a dose-dependent response curve). Growth Hormone levels peak at the half-hour mark after injection, then decreasing to baseline values within roughly four hours (half-life is about 55 minutes). (7)

ghrp-6

 

Of course, as we know from other peptides like GHRP-6, this type of surge in Growth Hormone levels has been positively correlated with increases in strength, muscle hypertrophy, and fat loss. Therefore, the many advantages of having GH secreted in larger amounts via administration of Hexarelin are comparable to the effects of injectable growth hormone administration. In my own case, I found that Hexarelin increased my strength and even aided with fat-loss a bit, but didn’t put much weight on me at all. This makes it very different from GHRP-6, which piles tons of weight on me.

BUY RESEARCH GHRP-6

Although my knee injury was, for the most part, totally healed from my use o GHRP-6, I suspect that Hexarelin would have produced very similar results or that purpose. That’s because, as we already know, increasing GH levels elicits a favorable increase in bone mineral density. When I used Hexarelin, however, I was mostly interested in the increase in GH which would provide me with both increased mitosis and meiosis (each of which leads to hypertrophy, i.e. increased muscle size), triglyceride hydrolysis which helps aid in fat loss. And since there are GH receptors (though no IGF-1 receptors) in adipose tissue, I decided to use my Hexarelin subcutaneously in my abdomen. Even though the GH response is systemic (whole-body), it couldn’t hurt to concentrate the shots where fat is more highly concentrated (which in males is the abdomen). I used 200mcg/day of Hexarelin, shot sub-q (in my case, being under 100kgs, this is just slightly over the maximum response dose...as I later found out).

Hexarelin enhanced GH secretion also leads to the liver secreting more IGF-1 (Insulin-Like Growth Factor 1). IGF-1 is thought to be the primary causative factor in the anabolic effects of Growth Hormone. It needs to be noted at this point that data on this is actually conflicting, and I’ve seen studies where (somehow?) Hexarelin elicits a release in GH without a commensurate increase in IGF-1 levels. In my own experience with Hexarelin, I found it to be reasonably anabolic on its own, and think that the
But lets be realistic here; it’s important to realize that Hexarelin is not going to produce results similar to high dose GH cycles, in the normal person. This is because Hexarelin only stimulates the increase of GH, and has been found to be effective up to 2mg/kg, but after that dose does not really produce more results in terms of GH secretion (7). Thus, a dose of 2mgs/kg is the upper limit for Hexarelin use, while GH users in the professional ranks of athletics and bodybuilding have gone as high as 10iu/day. Hexarelin, at 2mg/kg of bodyweight has been compared by most users to the type of results seen with 1-2iu/day of GH. At the price, though, Hexarelin is a much better alternative. If you need the type of results that 3iu+/day of GH are going to give you, then that’s an impossibility with Hexarelin use. Still, for the price and for the effects, this stuff is a steal when compared with using 2iu of GH every day.

One of my powerlifter friends (read: Lab Rats), who assists me in some of my research used Hexarelin while training for a meet. He had the dual purpose of rehabbing a shoulder as well as trying to increase his bench press. As you probably could have guessed, his bench went up, and his shoulder seemed to have healed. He was using roughly half the dose of Hexarelin I recommend for hypertrophy and fat loss, which worked out to about 50mcg/day shot 2x a day in the injured shoulder. His shoulder healed up nicely, and his strength went up a bit. Neither myself nor my friend had any increased appetite on Hexarelin, and I suspect that this is because it has a much less profound effect on Ghrelin levels. The strength gains we both received from its use were very similar to those experienced with GHRP-6, but with very little weight gain, and negligible fat loss. Hexarelin is a nice addition to a cutting cycle, to make maximum use of the GH response to both anabolic steroids as well as the GH induced response from training. And, it never hurts to include something that’s going to help your joints on a cutting cycle, since we know that the typical compounds used in a cutting cycle (Winstrol, etc…) often cause joint problems. We can use the added GH from the Hexarelin to help protect our otherwise compromised joints on a cycle, without spending tons of money on GH.

BUY RESEARCH GHRP-6

Unlike GH, however, some attenuation to Hexarelin occurs by week 4, and continues on up to 16 weeks of use. By separating Hexarelin cycles by 4 week off periods, this attenuation can be totally reset, (9) and the next cycle of Hexarelin will produce the same level of results as the first cycle. During a cutting cycle, I recommend using Hexarelin for the weeks where compounds such as Winstrol are used, and continuing its use for the duration of the cycle. If you’re using Lr3IGF-1 on your cutting cycle, then I recommend saving the Hexarelin for after the IGF use is over.

Although, many athletes use Hexarelin alone, others have used it after a Growth Hormone or Insulin-Like Growth Factor one cycle, to as a form of Post-Cycle Therapy for the recovery of their own natural GH and IGF-1 production. Again, for this purpose, 2mg/kg, injected subcutaneously is the proper dose per day. 

Although they’re new, and haven’t been experimented with too extensively in the bodybuilding community, I think that both GHRP-6 and Hexarelin will be used more commonly in the coming months and years. It took me far too long to jump on the bandwagon with IGF, and I was far too slow to begin my personal experimentation with MGF, so when these two peptides became available to me, I didn’t want to let the opportunity go for too long. Now, after some pretty extensive personal experimentation with these two peptides, I think that Hexarelin is a great anabolic addition to a cutting cycle, and GHRP-6 is probably the most potent (non-steroid) weight gainer that I’ve ever used. Considering the price, legal status, and availability, these two are probably going to find their way into quite a few cycles over the next few years.




References:
1.    Cheng K, Chan WW-S, Butler BS, Barreto A, Smith RG 1989 The synergistic effects of His-D-Trp-Ala-Trp-D-Phe-Lys-NH2 on GRF stimulated growth hormone release and intracellular cAMP accumulation in rat primary pituitary cell cultures. Endocrinology 124:2791–2797
2.    Smith RG, Pong S-S, Hickey GJ, Jacks TM, Cheng K, Leonard RJ, Cohen CJ, Arena JP, Chang CH, Drisko JE, Wyvratt Jr MJ, Fisher MH, Nargund RP, Patchett AA 1996 Modulation of pulsatile GH release through a novel receptor in hypothalamus and pituitary gland. Recent Prog Horm Res 51:261–286
3.    Leonard RJ, Chaung L-YP, Pong S-S 1991 Ionic conductances of identified rat somatotroph cells studies by perforated patch recording are modulated by growth hormone secretagogues. Biophys J 59:254
4.    Smith, Development of Growth Hormone Secretaogues, Endocrine Reviews, 26(3) 346-360
5.    Ghrelin: structure and function. Physiol Rev. 2005 Apr;85(2):495-522. Review.
6.    Penlava, A, et. al. Effect of growth hormone (GH)-releasing hormone (GHRH), atropine, pyridostigmine, or hypoglycemia on GHRP-6-induced GH secretion in man.J Clin Endocrinol Metab. 1993 Jan;76(1):168-71.
7.    Imbimbo, B.P., et. al Growth hormone-releasing activity of hexarelin in humans. A dose-response study.Eur J Clin Pharmacol. 1994;46(5):421-5.
PMID: 7957536 [PubMed - indexed for MEDLINE]
8.    Kinetics and Disposition of Hexarelin, A Peptidic Growth Hormone Secretagogue, in Rats
Marie Roumi, Sylvie Marleau, Patrick du Souich, Tony Maggi, Romano Deghenghi, and Huy Ong
Drug Metab. Dispos., Jan 2000; 28: 44.
9.    Rahim, A., Shalet, SM Does desensitization to hexarelin occur?
Growth Horm IGF Res. 1998 Apr;8 Suppl B:141-3.

 
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