Tesamorelin – 5MG/10MG

Tesamorelin

Tesamorelin is a synthetic polypeptide of 44 amino acids that is similar to human growth hormone-releasing hormone. Researchers argue that this modification in the N-terminus of the compound, an analogue growth hormone-releasing hormone might improve stability.

Mechanism: Tesamorelin has been evaluated for mechanism of action, and the posited is a GHRH receptor agonist functioning at the anterior pituitary gland resulting in enhanced synthesis as well as release of growth hormone. Growth hormones have a site of action in hepatocytes and on multiple cell types, such that growth hormone stimulates the synthesis of insulin-like growth factor-1 (IGF-1) at the systemic level. Furthermore, growth hormone can enhance the local and decentralized autocrine/paracrine action of IGF-1 by increasing its mRNA transcription rate within several tissues.

IGF-1 is thought to be the major anabolic mediator of growth hormone, released upon stimulation with the purpose of growth and anti-apoptosis. The Endocrine society reported that growth hormone is possibly lipolytic at different adipose depots, such as abdominal/visceral fat deposits. Tesamorelin is believed to promote the secretion of GH and, subsequently, IGF-1 by activity on the GHRH receptors of the anterior pituitary gland cells. Tesamorelin binding to the GHRH receptor in a manner that may reconfigure the structure of this receptor (see figure), possibly favoring additional cell communication pathways. Another theory for how Tesamorelin might work is that it increases the production of cAMP in some cells. This process could be performed by activating adenylate cyclase, which is that enzyme converts adenosine triphosphate (ATP) into cAMP. Elevated cAMP can trigger protein kinase A (PKA) activation, but the importance of the enzyme in cell signaling is not yet known. Upon activation, PKA can phosphorylate a range of target proteins, initiating a cascade of cellular responses. It is thought that Tesamorelin may stimulate the GHRH receptor which in turn activates cAMP-PKA signaling pathway causing secretion and production of growth hormone (hGH) from somatotroph cells located in the anterior pituitary. This could result in up to 69% increase in the total growth hormone levels (measured by area under the curve - AUC) and 55% increase in mean pulse area of growth hormone. But it does not appear to affect the pulse frequency or peak levels of growth hormone. Moreover, levels of IGF-1 supposedly increased by 122%.

Tesamorelin differs from human GHRH (TRH) inthat it has had every 5th amino acid taken outcausing once an increase to its half-life. With respect to the structural changes, an additional trans-3-hexenoic acid group is typically attached to the C-terminus of Tesamorelin. This change, called omega-amino acid modification, may help to more immovably secure the peptide within an anal in enzymes attacking it. This means that the N-terminus has CH₃CO- (acetyl ) group attached to it. By acetylating LmSUMO, stability of the molecule might increase and it could also improve biological activity. This makes Tesamorelin chemically N-(trans-3-hexenoyl)-[Tyr1]hGRF(1–44)NH2 acetate, detailing the specific modifications the peptide had undergone.

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