Ipamorelin

[Semin]

Introduction about Ipamorelin

Ipamorelin is a small-molecule ghrelin mimetic, the first in a class of growth hormone-releasing peptides (GHRP), synthetic growth hormone secretagogues (GHS) that bind to key control points for growth, appetite and gastric motility. Research with GHRPs led to the isolation of the first naturally occurring GHS, ghrelin, a "hunger hormone" secreted by stomach cells.

Exploratory studies in humans demonstrated that ghrelin infusions increased gastric emptying in normal volunteers and in patients with idiopathic or diabetic gastroparesis. However, ghrelin is an unstable lipid-peptide molecule with a pharmacokinetic half-life of about ten minutes, and thus is not an optimal drug candidate.

In contrast, ipamorelin demonstrates a more sustained half-life in humans. Ipamorelin has been shown to be both highly potent and very selective in vivo, and has also demonstrated good safety and tolerability in human clinical studies.

[Semin]

Ipamorelin or NNC 26-0161, a polypeptide hormone, is a growth hormone secretagogue and ghrelin mimetic and analog developed by Novo Nordisk[3]. Ipamorelin belongs to the most recent generation of GHRPs from the mid 1990s and causes significant release of growth hormone by itself, due both to its suppression of somatostatin (an antagonist to GHRH) and stimulation of release of GH from the anterior pituitary, similar to GHRP-2 and GHRP-6 which are compounds from the same class (growth hormone releasing peptides).[1] The cells that produce and release GH are known as somatotropes.[2] Like GHRP-2 and GHRP-6, ipamorelin does not have ghrelin’s lipogenic properties. Like GHRP-2 and unlike GHRP-6 ipamorelin never induces hunger in mammals. Ipamorelin acts synergistically when applied during a native GHRH (growth-hormone releasing hormone) pulse or when coadministered with GHRH or a GHRH analog such as Sermorelin or GRF 1-29 (growth releasing factor, aminos 1-29).[1] The synergy comes both due to the suppression of somatostatin and the fact that ipamorelin increases GH release per-somatotrope, while GHRH increases the number of somatotropes releasing GH.[1,2]

There is also a secondary effect of neuronal excitation in the hypothalamus caused by ipamorelin, which lasts for approximately 3 hours after application, similar to GHRP-2 and GHRP-6.

Ipamorelin has a unique property among the GHRP class of peptides. That property is known as selectiveness. Raun et al demonstrated the selectiveness of ipamorelin for GH release only in a study]
The development and pharmacology of a new potent growth hormone (GH) secretagogue, ipamorelin, is described. Ipamorelin is a pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2), which displays high GH releasing potency and efficacy in vitro and in vivo. As an outcome of a major chemistry programme, ipamorelin was identified within a series of compounds lacking the central dipeptide Ala-Trp of growth hormone-releasing peptide (GHRP)-1. In vitro, ipamorelin released GH from primary rat pituitary cells with a potency and efficacy similar to GHRP-6 (ECs) = 1.3+/-0.4nmol/l and Emax = 85+/-5% vs 2.2+/-0.3nmol/l and 100%). A pharmacological profiling using GHRP and growth hormone-releasing hormone (GHRH) antagonists clearly demonstrated that ipamorelin, like GHRP-6, stimulates GH release via a GHRP-like receptor. In pentobarbital anaesthetised rats, ipamorelin released GH with a potency and efficacy comparable to GHRP-6 (ED50 = 80+/-42nmol/kg and Emax = 1545+/-250ng GH/ml vs 115+/-36nmol/kg and 1167+/-120ng GH/ml). In conscious swine, ipamorelin released GH with an ED50 = 2.3+/-0.03 nmol/kg and an Emax = 65+/-0.2 ng GH/ml plasma. Again, this was very similar to GHRP-6 (ED50 = 3.9+/-1.4 nmol/kg and Emax = 74+/-7ng GH/ml plasma). GHRP-2 displayed higher potency but lower efficacy (ED50 = 0.6 nmol/kg and Emax = 56+/-6 ng GH/ml plasma). The specificity for GH release was studied in swine. None of the GH secretagogues tested affected FSH, LH, PRL or TSH plasma levels. Administration of both GHRP-6 and GHRP-2 resulted in increased plasma levels of ACTH and cortisol. Very surprisingly, ipamorelin did not release ACTH or cortisol in levels significantly different from those observed following GHRH stimulation. This lack of effect on ACTH and cortisol plasma levels was evident even at doses more than 200-fold higher than the ED50 for GH release. In conclusion, ipamorelin is the first GHRP-receptor agonist with a selectivity for GH release similar to that displayed by GHRH. The specificity of ipamorelin makes this compound a very interesting candidate for future clinical development.[3]

Whereas GHRP-6 and GHRP-2 cause a release and increase in cortisol and prolactin levels, ipamorelin only selectively releases GH at any dose. Further, a mega-dose of ipamorelin results in a concomitant mega-release of GH (up to the entire amount present in the pituitary), whereas GHRP-2 and GHRP-6 have limits of approximately 1mcg/kg in humans for their maximal GH release.[4,5]

References]
[1] Bowers CY, Momany F, Reynolds GA. In vitro and in vivo activity of a small synthetic peptide with potent GH releasing activity. 64th Annual Meeting of the Endocrine Society, San Francisco, 1982, p. 205. [2]Bowers CY, Momany F, Reynolds GA, Sartor O. Multiple receptors mediate GH release. 7th International Congress of Endocrinology, Quebec, Canada, 1984, p. 464.

[3] Raun K, Hansen BS, Johansen NL, Thøgersen H, Madsen K, Ankersen M, Andersen PH. Ipamorelin, the first selective growth hormone secretagogue. Eur J Endocrinol. 1998 Nov;139(5)]
[4] Brosnan-Cook, M. et al. (1998) Iontophoretic delivery of ipamorelin, a growth hormone secretagogue. Proceedings of 80th Annual Meeting Endocrine Society, New Orleans, USA. Abstract Pp1-186.

[5] Jogarao V S Gobburu; Henrik Agerso; William J Jusko . Pharmacokinetic-Pharmacodynamic Modeling of Ipamorelin, a Growth Hormone Releasing Peptide in Human Volunteers. Lars Ynddal Pharmaceutical Research: Sep 1999; 16, 9; ProQuest Nursing & Allied Health Source p. 1412.

[Semin]

Ipamorelin is an interesting peptide taken 300mcg twice daily or you could lower the dose for 3 times daily, side effects are head rushs, I would recommend taking this 30 minutes before workout ,with gear, Ipamorelin is a new and potent synthetic pentapeptide which has distinct and specific growth hormone (GH)-releasing properties. With the objective of investigating the effects on longitudinal bone growth rate , body weight , and GH release, Ipamorelin in different doses (0, 18, 90 and 450 ?g/day) was injected three times daily for 15 days to test subjects, After intravital Tetracycline labelling on days 0, 6, and 13, LGR was determined by measuring the distance between the respective fluorescent bands in the proximal tibia metaphysis. Ipamorelin dose-dependently increased LGR from 42 ?m/day in the vehicle group to 44, 50, and 52 ?m/day in the treatment groups . There was also a pronounced and dose-dependent effect on body weight gain. The treatment did not affect total IGF-I levels, or serum markers of bone formation and resorption. The number of tartrate-resistant acid phosphatase-positive multinuclear cells in the metaphysis of the tibia did not change significantly with treatment. The responsiveness of the pituitary to a provocative i.v. dose of Ipamorelin or GHRH showed that the plasma GH response was marginally reduced , after Ipamorelin, but unchanged after GHRH. The pituitary GH content was unchanged by Ipamorelin treatment. Whether Ipamorelin or other GH secretagogues may have a place in the treatment of children with growth retardation requires demonstration in future clinical studies.before closing Ipamorelin is the most selective GH releaser you can get.

Ipa doesn't create bumps in either prolactin or cortisol like GHRP-2 and -6. Ipa is a rifle bullet, not a shotgun blast like other GHRP's. Also it's great for those on relatively calorie restricted diets because it doesn't stimulate appetite

[DecaDoesABodyGood]

what does gastric emptying mean? Are there any peptides that do not cause that?* Thank You!

[Semin]

"
what does gastric emptying mean? Are there any peptides that do not cause that?* Thank You!
"

I have not felt and GI feelings w/ Ipamorelin usage.* Believe it refers to increasing peristalsis, etc - GHRP-6 and MT-2 might have these characteristics - they are not bad however

[DecaDoesABodyGood]

Have you or anyone you know that used Ipamorelin experienced negative side effects, if so..what were they?

[Semin]

I have never heard or had experienced any negative side effects - will keep my eyes out for any others however

[DecaDoesABodyGood]

Does Ipamorelin cause increased hunger?

[Semin]

"
Does Ipamorelin cause increased hunger?
"

Not really, no

[Semin]

"
Have you or anyone you know that used Ipamorelin experienced negative side effects, if so..what were they?
"

One side effect can come alongside boom or mega-dosing Ipmorelin - when the researchers injects half or whole vials...can experience a head rush/flushing (doses of 1-2mg)

Ipamorelin dosage range should be 100-500mcg

[nrvous]

Bumping this thread to see if there are any new findings while pinning 100mcgs twice daily sub'q (am/pm post workout). Really looking for synergy and joint repair at this dosage. Any comments or suggestions before I place my order?

[Semin]

"
Bumping this thread to see if there are any new findings while pinning 100mcgs twice daily sub'q (am/pm post workout). Really looking for synergy and joint repair at this dosage. Any comments or suggestions before I place my order?
"

I like adding a 100mcg touch of Ipamorelin to random melanotan, hcg, tb-500, mod grf 1-29 and/or ghrp injections often

Very low dosage (popular and approved by mainstream) - my comments/suggestion would be to not look for anything dramatic - should be hardly noticeable & w/o side effect(s) on ipamorelin at a reasonable dosage (100mcg administrations) - best of luck!

[nrvous]

Ok. What's a moderate dosage to where I will notice the effects without sides?* I have also considered pinning 200mcgs twice daily. In don't think I read that many people were having sides with that dosage either.

[bigboy22]

How much do we expect to spend every month for ipamorelin? What is the recommended dose to achieve great results as soon as possible? I am leaning toward ipamorelin, but I am still not so sure with my decision.

[mrfitness]

Wow. You had definitely discussed a lot about ipamorelin. I know a lot of people are satisfied and interested in ipamoreling. However, I think it would be best if you would discuss about other kinds of peptides as well. There are also those who are interested in DSIP, GHRP-2, GHRP-3, MOD GRF and the others,

[IzzyPretty]

So much information about ipamorelin. I guess I just suffered from information overload. Lol. Ipamorelin is not bad at all. In fact, it is also great, but not as great as what others claim.

[cassey]

One side effect can come alongside boom or mega-dosing Ipmorelin - when the researchers injects half or whole vials...can experience a head rush/flushing (doses of 1-2mg)

Ipamorelin dosage range should be 100-500mcg

I also get head flushing even when I am just taking a low dose of ghrp 6. However, I am not bothered by it as it easily goes away in a few minutes or hours.

[marielle]

Introduction about Ipamorelin

Ipamorelin is a small-molecule ghrelin mimetic, the first in a class of growth hormone-releasing peptides (GHRP), synthetic growth hormone secretagogues (GHS) that bind to key control points for growth, appetite and gastric motility. Research with GHRPs led to the isolation of the first naturally occurring GHS, ghrelin, a "hunger hormone" secreted by stomach cells.

Exploratory studies in humans demonstrated that ghrelin infusions increased gastric emptying in normal volunteers and in patients with idiopathic or diabetic gastroparesis. However, ghrelin is an unstable lipid-peptide molecule with a pharmacokinetic half-life of about ten minutes, and thus is not an optimal drug candidate.

In contrast, ipamorelin demonstrates a more sustained half-life in humans. Ipamorelin has been shown to be both highly potent and very selective in vivo, and has also demonstrated good safety and tolerability in human clinical studies.

Ipamorelin showing safety and tolerability in human clinical studies is among the reason why this peptides is so popular. It is also among the more expensive peptides. Well, it is worth the price after all.

[queen_B]

Not really, no

Really? It still makes me hungry. However, the hunger is not as bad as when I was still using GHRP-2. I am not sure if it was the ipamorelin or MOD GRF that is causing the hunger, but I do still get hungry with my ipamorelin + MOD GRF intake.

[Burmann]

Ok. What's a moderate dosage to where I will notice the effects without sides?* I have also considered pinning 200mcgs twice daily. In don't think I read that many people were having sides with that dosage either.

Try to lower your dose to 100mcgs twice daily. It is enough to help you achieve whatever your body goal is. I am not fond of taking high dose of peptides or the likes as I think it is just a waste of money.