Ipamorelin

Ipamorelin

Ipamorelin is a growth hormone releasing peptide. It stimulates the body to release more human growth hormone and igf-1. Increases in gh and igf-1 can result in many benefits including:

- Builds Lean Tissue
- Lowers Body Fat
- Improved Recovery from training
- anti aging
- Improves Mood and Sleep Patterns

Ipamorelin is similar to other GHRP's such as GHRP-2 and GHRP-6. However Ipamorelin does not cause sudden spikes in prolactin or cortisol like GHRP-2 and GHRP-6 can do. Both of those hormones when elevated can cause negative side effects. Cortisol is a steroid hormone that is released when stressed and can be very catabolic. Prolactin counteracts the effect of dopamine, which is responsible for sexual arousal. Elevated prolactin can cause a variety of unwanted physical and psychological effects.

Raun K et al. (1998) highlighted ipamorelin's beneficial effects over the other ghrp's. In pentobarbital anaesthetised rats, ipamorelin released GH with a potency and efficacy comparable to GHRP-6. In conscious swine, gh release after ipamorelin injection was high and again vey similar to GHRP6. In the same study GHRP-2 displayed higher potency but lower efficacy. The specificity for GH release was studied in swine. They found 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 when extremely high doses of were used. Ipamorelin was the first GHRP-receptor agonist with a selectivity for GH release similar to that displayed by GHRH.

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. However ipameolin is slow in its delivery unlike GHRP’s which spike GH levels at a faster rate. This another notable difference when researching ghrp's. Moreover it has been shown that Ipamorelin is able to exert a dynamic control effect on the somatotroph population and on GH hormone content (Jiménez-Reina L et al. 2002).

A variety of promising effects have been displayed when ipamorelin has been studied. Adeghate E et al. (2004) examined the effect ipamorelin had on insulin secretion from pancreatic tissue fragments of normal and diabetic rats. Ipamorelin evoked significant (p<0.04) increases in insulin secretion from the pancreas of normal and diabetic rats. It was shown that ipamorelin stimulates insulin release through the calcium channel and the adrenergic receptor pathways.

Nitrogen balance is very important in humans. A positive value is often found during periods of growth, tissue repair or pregnancy. This means that the intake of nitrogen into the body is greater than the loss of nitrogen from the body, so there is an increase in the total body pool of protein. A negative value can be associated with burns, fevers, wasting diseases and other serious injuries and during periods of fasting. This means that the amount of nitrogen excreted from the body is greater than the amount of nitrogen ingested. Aagaard NK et al. (2009) studied the metabolic effects of Ipamorelin on selected hepatic measures of alpha-amino-nitrogen conversion during steroid-induced catabolism. Prednisolone was the steroid used to induce this catabolism. In prednisolone treated rats ipamorelin reduced CUNS by 20% (p<0.05), decreased the expression of urea cycle enzymes, neutralised N-balance, and normalized or improved organ N-contents. Therefore accelerated nitrogen wasting in the liver and other organs caused by prednisolone treatment was counteracted by treatment with Ipamorelin.

Ipamorelin is ideal for pre bed dosing due to it's long active life and minimal effect on hunger levels. When other GHRP's are used such as GHRP 2/6 they can cause a sudden increase in appetite which can be awkward pre bed. Doses as little as 200mcg are highly effective but I feel Ipamorelin truly shines when you boom dose it. I have gone up to as much as 1mg pre bed and that was incredible. Although for most a dose of 500mcg would be more than enough when combined with a GHRH. My favourite peptide cycle to date has been CJC-1295 DAC with GHRP-2 through the day. Then a high dose of Ipam used pre bed.

Finally just want to list what I feel is a key advantage ipamorelin has over GH injections in a research environment. Unlike GH injections it does not shut down the body’s natural production of this hormone, it just enhances it. In the long run this is a huge factor and I feel future studies will highlight the importance of this in relation to health.

References

1. Aagaard NK, Gr&oslash;fte T, Greisen J, Malml&ouml;f K, Johansen PB, Gr&oslash;nbaek H, &Oslash;rskov H, Tygstrup N, Vilstrup H (2009) Growth hormone and growth hormone secretagogue effects on nitrogen balance and urea synthesis in steroid treated rats. PMID: 19231263 [PubMed - indexed for MEDLINE]
2. Adeghate E, Ponery AS (2004) Mechanism of ipamorelin-evoked insulin release from the pancreas of normal and diabetic rats. PMID: 15665799 [PubMed - indexed for MEDLINE]
3. Raun K, Hansen BS, Johansen NL, Th&oslash;gersen H, Madsen K, Ankersen M, Andersen PH (1998) Ipamorelin, the first selective growth hormone secretagogue. PMID: 9849822 [PubMed - indexed for MEDLINE]
4. Jim&eacute;nez-Reina L, Ca&ntilde;ete R, de la Torre MJ, Bernal G (2002) Influence of chronic treatment with the growth hormone secretagogue Ipamorelin, in young female rats: somatotroph response in vitro. PMID: 12168778 [PubMed - indexed for MEDLINE]

Growth hormone and growth hormone secretagogue effects on nitrogen balance and urea synthesis in steroid treated rats.

Aagaard NK1, Grøfte T, Greisen J, Malmlöf K, Johansen PB, Grønbaek H, Ørskov H, Tygstrup N, Vilstrup H.


Abstract

OBJECTIVES:

Growth hormone (GH) reduces the catabolic side effects of steroid treatment via effects on the amino-nitrogen metabolism. Ipamorelin is a synthetic peptide with GH releasing properties. We wished to study the metabolic effects of Ipamorelin and GH on selected hepatic measures of alpha-amino-nitrogen conversion during steroid-induced catabolism.

DESIGN:

Five groups of rats were included: (1) free-fed controls (2) pair-fed controls (3) prednisolone (delcortol, 4 mg x kg(-1) x day(-1)) (4) prednisolone and GH (1 mg x kg(-1) x day(-1)) (5) prednisolone and Ipamorelin (0.5 mg x kg(-1) x day(-1)). After seven days the hepatic capacity of urea-N synthesis (CUNS) was determined in parallel with measurements of liver mRNA levels of urea cycle enzymes, whole-body N-balance, and N-contents of various organs.

RESULTS:

Compared to pair-fed controls, prednisolone increased CUNS (p<0.01) as well as the expression of urea cycle genes (p<0.01), and decreased N-balance (p<0.01) as well as organ N-contents (p<0.05). Compared to prednisolone treated animals, co-administration of GH reduced CUNS by 33% (p<0.01), normalized urea cycle gene expression, improved N-balance 2.5-fold, and normalized or improved organ N-contents. In prednisolone treated rats Ipamorelin reduced CUNS by 20% (p<0.05), decreased the expression of urea cycle enzymes, neutralised N-balance, and normalized or improved organ N-contents.

CONCLUSION:

Accelerated nitrogen wasting in the liver and other organs caused by prednisolone treatment was counteracted by treatment with either GH or its secretagogue Ipamorelin, though at the doses given less efficiently by the latter. This functional study of animals confirms that the GH secretagogue exerts GH related metabolic effects and may be useful in the treatment of steroid-induced catabolism.


PMID: 19231263 [PubMed - indexed for MEDLINE]

I am putting my gf (Barbie) on cjc no dac (50-100mcg) and ipam (100-200mcg) twice daily. That is an extremely safe stack with minimal side effects and should just give great results

Influence of chronic treatment with the growth hormone secretagogue Ipamorelin, in young female rats: somatotroph response in vitro.

Jiménez-Reina L1, Cañete R, de la Torre MJ, Bernal G.

Abstract

Growth hormone (GH) is secreted in the anterior pituitary gland by the somatotroph cells. Secretion is regulated by growth hormone releasing hormone (GHRH) and somatostatin. Morever, GH secretagogues (GHS) can exert a considerable effect on GH secretion. In order to determine the effects of chronic treatment with the GHS Ipamorelin on the composition of the somatotroph cell population and on somatotroph GH content, an in vitro analysis was performed of the percentage of somatotroph cells (% of total), the ratio of different GH cell types (strongly/weakly-staining) and individual GH content, in pituitary cell cultures obtained from young female rats receiving Ipamorelin over 21 days (Ipamorelin group) and the effects were compared with those of GHRH (GHRH group) or saline (saline group). The ultrastructure of somatotroph cells did not change, but the volume density of secretion granules was increased (P<0.05) by previous in vivo Ipamorelin or GHRH treatment. In 3-day basal pituitary cell monolayer cultures, the percentage of somatotroph cells showed no modifications between groups, nor was there any change in the ratio of strongly/weakly immunostaining GH cells. In the Ipamorelin group alone, in vitro treatment with Ipamorelin (10(-8) M), or GHRP 6 (10(-8) M), or GHRH (10(-8) M) for 4 hours, increased the percentage of somatotroph cells, without modifying the ratio of strongly/weakly immunostained GH cells. Basal intracellular GH content in somatotroph cells over 4 hours was lower in the Ipamorelin group and the GHRH group than in the saline group. Only in the Ipamorelin group did Ipamorelin (10(-8) M), GHRP 6 (10(-8) M) and GHRH (10(-8) M) prompt increased intracellular GH content. These data suggest that, at least in the young female rat, the GHS Ipamorelin is able to exert a dynamic control effect on the somatotroph population and on GH hormone content.


PMID: 12168778 [PubMed - indexed for MEDLINE]

Ipamorelin, the first selective growth hormone secretagogue.

Raun K1, Hansen BS, Johansen NL, Thøgersen H, Madsen K, Ankersen M, Andersen PH.

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.

PMID: 9849822 [PubMed - indexed for MEDLINE]

I am loving my cycle. I am only dosing it once daily but will start doing it twice soon. For the first 2 days I used 1mg sermorelin and 500mcg pre bed. The following 2 nights I used 1mg tesamorelin and 500mcg ipamorelin. I have noticed an increase in fatigue though which is a good sign (even if I don't like it). The hand numbness has been so bad and my sleep amazing. I hadn't been sleeping well over the last 2 months but these peps and made a huge difference and fast.

500mcg ipamorelin with 100mcg cjc no DAC is a great pre-bed stack. It knocks you out!