Zacznijmy od tego,ze od roku widze przybytek na rynku dostepnosci ciekawych zabawek.Są informacje na ich temat,ale ogolem znikome.
Gh wiemy chyba wszyscy co to jest.
Ostatnio tez wiemy wiecej o IGF Lr3.
Panowie co z reszta,bo nie wiele wciaz o nich wiadomo,moze ktoś testował,albo ma jakis zaułek wiedzy.
CJC1295 (oczytałem sie jedynie,ze jest to rodzaj analagiczny ghrh 1-44)
GHRP-6 (hexapeptyd gh i tyle wiem)
MELANOTAN I i II (czorna magia)
PEGylated MGF (IGF-1Ec) (kombinacja nie z tej ziemi mgf obrobiony peg-iem,nie wiem po co)
HGH FRAGMENT (176-191)(wtf?)
DLys3 GHRP-6 (wtf2?)
HEXARELIN (ponoc kielich Graala wsrod analogów gh,ale malo nadal wiem)
SERMORELIN (2 rzecz,która chlubnie sie prezentuje obok hexa,rowniez malo znane)
GHRP-2 (kolejny peptyd)
MGF (nie wiele wiem,ponoc gorsze niz igf na bebechy)
Oto co znalazłem:
GHRH1-44, also known as Growth Hormone Releasing Hormone (other synonyms are GRF and GHRF), is a peptide that is produced in the hypothalamus and secreted to stimulate the release of growth hormone (GH). It consists of a 44 amino acid long sequence and is released in a pulsatile fashion similar to the pulsatile release of hGH. The active portion of this peptide can be found as a 29 amino acid long peptide and is appropriately named GHRH1-29. Despite the effectiveness of GHRH to stimulate growth hormone release there are a number of problems associated with using it in vivo. The most noteworthy problem is the half life of the peptide, which has been shown to be ~7 minutes using advanced HPLC technologies that have proven to be very accurate. The reason for this relatively short half life is due to an enzyme called dipeptidylaminopeptidase IV (DPP-IV), which has a high affinity for the amino acids Ala and Pro and in the case of GHRH it cleaves the 1 and 2 positions that consist of Tyr-Ala, creating GHRH3-29, an inactive form of the peptide.
This brings us to the introduction of a far more stable form of GHRH called CJC-1295. CJC-1295 is a tetrasubstituted peptide analogue of GHRH with D-Ala, Gln, Ala, and Leu substitutions at positions 2, 8, 15, and 27 respectively. These substitutions create a much more stable peptide with the substitution at position 2 to prevent DPP-IV cleavage, position 8 to reduce asparagine rearrangement or amide hydrolysis to aspartic acid, position 15 to enhance bioactivity, and position 27 to prevent methionine oxidation. These substitutions are key in increasing the overall half life of CJC-1295 but there lies an even greater reason as to why the half life has been extended from ~7 minutes to greater than 7 days! Bioconjugation is a relatively newer technology that takes a reactive group and attaches it to a peptide, which in turn reacts with a nucleophilic (usually a partially negative molecule) entity found in the blood to form a more stable bond. By combining the tetrasubstituted GHRH analogue with maleimodoproprionic acid using a Lys linker, you create a GHRH peptide with a high binding affinity for albumin. Once the CJC-1295 molecule has attached itself to albumin, it is given an extended half life and bioavailability thanks to the albumin preventing enzymatic degredation and kidney excretion. In fact, bioconjugation is so effective that there was less than 1% of CJC-1295 left unreacted in vivo and over 90% was stabilized after subcutaneous injection. This means that you get more of what you paid for working for you. There was no DPP-IV degredation observed on CJC-1295 in any of the various experiments conducted.
Melanotan and melanotan II are both analogs of the peptide hormone alpha-melanocyte stimulating hormone (α-MSH).
Hexarelin is a six-amino acid peptide. Studies have shown that hexarelin is actually more effective and longer lasting than growth hormone releasing hormone (GHRH). It is also known that GHRP-6 has a synergistic effect with GHRH, causing a far greater release than either of these substances alone. By combining GHRP-6 with Hexarelin, a more potent GH releasing peptide combination is created than ever heard of. The potential clinical usefulness of these GH releasing hexapeptides is also reinforced by observations that long-term administration produces elevations in circulating IGF-1 concentrations. Long term treatment with GHRP-6 similarly has been shown to elevate serum IGF-1 as well as IGF-binding protein-3 concentrations, alter body composition and promote linear growth.
PEGylated Mechano Growth Factor is a new and innovative form of MGF that outperforms natural MGF many times over. PEG stands for polyethylene glycol, a unique polymer that is non-ionic and soluble in water. By covalently bonding a PEG chain to a peptide you can expand the physical radius of the overall molecule, which creates a “shield" around the peptide and prevents proteases and antibodies from cleaving it and rendering it inactive. PEGylation also has various lengths (weights) and using a chain that is too large can block the binding of the peptide to its receptor. This, and the fact that MGF is a smaller peptide, is why we decided to use a smaller PEG chain and since d-arg MGF is insoluble in water the addition of a PEG chain is a positive feature to this peptide.
Commentary highlighted in green is to further explain the statements from the article and key points from the article are highlighted in red.......
The FASEB Journal express article 10.1096/fj.05-3786fje. Published online September 6, 2005
A strong neuroprotective effect of the autonomous Cterminal peptide of IGF-1 Ec (MGF) in brain ischemia
Joanna Dłużniewska,* Anna Sarnowska,† Małgorzata Beręsewicz,* Ian Johnson,‡Surjit K. S. Srai,§ Bala Ramesh,§ Geoffrey Goldspink,// Dariusz C. Górecki,¶ and Barbara Zabłocka*
The 24 amino acid peptide amide (NH2-YQPPSTNKNTKSQ(d)R(d)RKGSTFEEHK-NH2 corresponding to the shorter consensus mammalian sequence for the C-terminal MGF peptide was synthesized using the Fmoc protection strategy. The D-form of arginine was used for the synthesis instead of the naturally occurring L-form. The N terminus was modified by a PEG derivative (O’O-bis(2-aminopropyl)polyethylene glycol 1900) (Jeffamine) via a succinic acid bridge.................
Comments: Goldspink is the scientist that actually discovered MGF and for purposes specific to this study he uses MGF but instead of the human sequence which contains 3 arginines, they use the shorter consensus mamalian sequence containing 2 arginines. They removed the arginine at the 23rd position. Human form MGF has a third arginine at the 23rd position. They are also using the D-form of arginine to keep them from cleaving and makes it more stable.
Based on these analyses and taking into account the high degree of homology, we have generated a consensus sequence for the mammalian 24aa C-terminal peptides of the IGF-1 splice variant IGF-1Eb/Ec or MGF (Fig. 1B). This consensus sequence was used to prepare a synthetic, 24 amino acid long MGF C-terminal peptide. Based on the human sequence, this peptide contained two rather than three arginines (Fig. 1B). To increase the stability of the MGF peptide, which was found to be rapidly degraded in the serum or tissue fluids (Yang and Goldspink, unpublished), the D-form of arginine was used for synthesis instead of the naturally occurring Lform. Moreover, the N terminus of the peptide was PEGylated...................
Comments: As you can see proof here that plain MGF is not stable and must be PEGylated to stabilize.....from the mouth of Goldspink himself.
Such a small and biologically active molecule is a good candidate for development into a therapeutic modality. Indeed, we have shown here that C-terminal MGF peptide can be modified into a more stable and potentially targetable moiety by specific chemical modifications. In contrast, the recombinant full-length IGF-1, although neuroprotective in vitro, was found ineffective when delivered by intracarotid injection. It remains to be elucidated whether this disparity was due to different biological activities or resulted from the increased stability of the modified C-terminal MGF molecule. The difference in permeability through the blood-brain (BBB) barrier could also be a factor, but it has to be stressed that the PEGylated C-terminal MGF and recombinant IGF-1 have similar molecular size.
We demonstrate here the efficacy of the modified C-terminal MGF peptide administered as a single bolus injection intra-arterially. This suggests that the stabilized, pegylated peptide molecule was able to cross the BBB and penetrate into the neurones…………………..
Comments: As you can see clearly in red that PEGylation made the MGF peptide more stable and more targetable for development of a therapeutic modality for the pharmaceutical world.
The HGH Fragment is a modified form (Figure 1) of amino acids 176-191 at the C-terminal region of growth hormone.
Investigators at Monash University discovered that the fat-reducing effects of GH appear to be controlled by a small region near one end of the GH molecule. This region, which consists of amino acids 176-191, is less than 10% of the total size of the GH molecule and appears to have no effect on growth or insulin resistance. It works by mimicking the way natural hGH regulates fat metabolism but without the adverse effects on blood sugar or growth that is seen with unmodified hGH. Like unmodified GH, the HGH fragment 176-191 stimulates lipolysis and inhibits lipogenesis both in laboratory testing and in animals and humans. The HGH fragment does not appear to affect appetite.
In laboratory tests on fat cells from rodents, pigs, dogs, and humans, the HGH fragment released fat specifically from obese fat cells but not from lean ones, reduced new fat accumulation in all fat cells, enhanced the burning of fat. In rodents (rats and mice), HGH fragment reduced body fat in obese animals but, enhanced fat burning without changing food consumption or inducing growth (as it does not increase IGF levels) or any other unwanted hGH effect.
[D-Lys³] GHRP-6 is a Ghrelin and GHRP-6 antagonist (anti-Ghrelin). An antagonist is an opposing or resistant structure in relation and tends to neutralize or impede some action or effect. In this case, the [D-Lys³] GHRP-6 is actually a selective antagonist of the cognate ghrelin receptor, i.e. the GH-secretagogue receptor (GSR).
Moze komus sie przyda taka krótka opisowośc.Dla mnie za mało.Jesli ktos zechciałby sie podzielić swoją wiedzą byłoby ciekawiej.
edit:znalazłem coś jeszcze o ghrp-2
The products that exist on the market today that produce the same results are with injection. This new product, HGH Strips, is taken orally through strips that are placed on the back of the toungue. HGH Strips is scientifically developed with GHRP-2 (Growth Hormone Releasing Peptide-2), L-Lysine, L-Argenin and L-Valine which amino acids are specifics for increasing the natural production of GH (Growth Hormone) by the anterior pituitary deep inside the brain; also called Somatotropin, it influences in growth of cells, bones, muscles and organs throughout the body. HGH Strips helps to increasing the levels of IGF-1 (Insulin like Growth Factor-1 is a metabolite of human growth hormone) rise; a natural anabolic growth factor molecule. Studies have found that IGF-1 has increased lean body mass, reduced fat, built up bone and muscle tissue, it may even regenerate nerve tissues and boost the immune system.
Growth Hormone Releasing Peptide - 2 (GHRP2)
Is a synthetic six amino acid peptide that has robustly potent properties.
GHRPs are a small family of peptides acting at the pituitary and the hypothalamus to release Growth hormone (GH) through the activation of a specific, G protein-coupled receptor.
They were discovered 20 years ago as synthetic metenkephalin- derived oligopeptides (Synthetic tissue derived amino acids). Although it has no structural homology with Growth Hormone Releasing Hormone (GHRH), in clinical studies GHRP-2 demonstrated action on the pituitary to release Human Growth Hormone (HGH). Similar results were effective when GHRP-2 was administered sublingual. Clinical studies showed the most potent GHRP being the hexapeptide GHRP-2.
Growth Hormone Releasing Peptide 2(GHRP2) substantially stimulates the pituitary gland's increased natural production of the body's own endogenous human growth hormone (HGH). This therapy consists of daily periodic sub-lingual dosing. Growth Hormone releasing peptide 2, GHRP2 has shown on it's own to robustly increase IGF-1 levels, and even greater results occurred when used with Growth Hormone Releasing Hormone (GHRH) to which also stimulates the pituitary gland to produce increased natural secretion of human growth hormone. This also boosts the hypothalamus function as well.
The results of the clinical studies published in the Journal of Endocrinology and Metabolism in 1997 for GHRP2 - showed that a medically supervised, prescribed and administered therapy increased growth hormone levels in adults and children, who have growth hormone deficiency.
The increase in the body's growth hormone via elevated IGF-1 levels produced by the pituitary gland in response to GHRP2 therapy -- has an anabolic effect on the tissues of the body and other benefits identified below.
Frequently asked Questions
Q: Why use GHRP2 instead of Growth Hormone?
A: This can be used alone or as an adjunct to HGH therapy. Both methods will yield robust results. The synergy of using GHRP2 with injectable growth hormone is that it allows your own natural production to remain and rebuild along with the use of injectable growth hormone. GHRP2 works greatly on it's own as well.
Q: I have heard of using growth hormone orally and don't have much faith in this manner of its application. Can you explain about this?
A: Growth hormone has a brief half life and is rendered ineffective when orally applied, swallowed and passed into the gastric tract. Then it must pass through the liver when applied orally. This is why HGH is effectively administered through subcutaneous injections. Conversely, GHRP2 oral mucosal medicine delivery i.e.: sublingual/ intranasal as demonstrated in clinical studies, is an effective alternative method of systemic medicine /supplement delivery that offers not only impressive results -- but several advantages over both injectable and enteral methods.
Because the oral mucosa is highly vascularised, medi-suppliments that are absorbed through the oral mucosa directly enter the systemic circulation, bypassing the gastrointestinal tract and first pass metabolism in the liver. For some supplements and drugs, this results in rapid onset of action via a more comfortable and convenient delivery route than the intravenous route. Not all medications, however, can be administered through the oral mucosa because of the characteristics of the oral mucosa and the physicochemical properties of the supplement.
GHRP2 can be delivered sublingual and is the preferred method of application -- and in a peer reviewed clinical study from the Department of Pediatrics at the University of Arkansas for Medical Sciences, published in the Journal of Endocrinology and Metabolism in 1995, "All 15 children had a significant GH response to 15 pg/kg dose. The intranasal /mucosa delivery was well tolerated."
Zmieniony przez - SaMuRai-N w dniu 2009-01-24 02:21:09