Tesamorelin: Mechanism of Action
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Comprar peptídeo Tesamorelin - todos os tamanhos1. Receptor Target — GHRH Receptor
Tesamorelin acts como um(a) specific agonist para o(a) GHRH receptor (GHRHr), a seven-transmembrane G protein-coupled receptor (GPCR) located on somatotroph cells no(a) anterior pituitary gland. Binding potency is comparable to endogenous GHRH. [7]
2. DPP-4 Resistance
The trans-3-hexenoic acid modification no(a) N-terminal Tyr1 acts como um(a) chemical shield against DPP-4 cleavage. Native GHRH is rapidamente degradado(a) (T½ ~5 min); Tesamorelin's modification extends stability to ~26–38 min. [3]
3. Sinalizacao a Jusante Cascade
Gₛ → Adenylyl Cyclase → cAMP → PKA → Ca²⁺ Influx → GH Exocytosis:
- Receptor ativacao desencadeia the Gₛα subunit
- Gₛα estimula adenylyl cyclase, converting ATP to cAMP
- Elevated cAMP ativa Protein Kinase A (PKA)
- PKA opens voltage-gated Ca²⁺ channels → calcium influx
- Ca²⁺ desencadeia exocytosis of pre-stored GH vesicles
- Simultaneamente, cAMP promove GH gene transcricao (new GH synthesis) [7]
🔑 Pulsatility Preserved: Diferentemente de exogenous rhGH (which creates constant supraphysiological levels), Tesamorelin estimula natural pulsatile GH release. The IGF-1 negativo(a) feedback loop remains intact, preventing runaway GH production. [8]
The product supplied here is for uso em pesquisa apenas independentemente de regulatory status of related formulations.
4. Selectivity
Tesamorelin is highly selective para o(a) GHRH receptor. It does not significantly alter TSH, LH, ACTH, or Prolactin levels. Diferentemente de GHRPs (e.g., Ipamorelin), it nao bind the ghrelin receptor. [9]
5. Receptor-Level Summary
Receptor-level: GHRH-receptor agonist at anterior-pituitary somatotrophs (cAMP/PKA signalling). [7]
6. Comparison with Related Molecules
| Compound | Structure | Key Difference |
|---|---|---|
| Endogenous GHRH | Native 44 aa | Rapidly degraded by DPP-4 (T½ ~5 min) |
| Tesamorelin | 44 aa + hexenoyl cap | DPP-4 resistant (T½ ~30 min); pulsatile GH |
| Sermorelin | 29 aa fragment | Shorter T½ (~5–10 min); menos potent |
| CJC-1295 + DAC | GHRH analog + DAC | Days-long T½; continuous “GH bleed” (not pulsatile) |
| Somatropin (rhGH) | Exogenous GH | Bypasses pituitary; suprime natural production |
7. Pharmacokinetics
| Parameter | Value |
|---|---|
| Half-Life (T½) | ~26–38 min |
| GH Pulsatility | Preserved (natural pulses, IGF-1 feedback intact) |
| Metabolism | Proteolytic cleavage; no formal human metabolismo studies |
| Animal T½ | 21–45 min (dogs) |
“Aviso sobre Estudos In Vitro / Pré-clínicos: Os achados de pesquisa descritos acima foram observados em estudos laboratoriais (in vitro) e/ou em modelos animais.”
Referencias
- Falutz J, Allas S, Kotler D, et al. AIDS, 19(12), 1279-87, 2005.
- Ferdinandi ES, Brazeau P, High K, et al. Basic Clin Pharmacol Toxicol, 100(1), 49-58, 2007.
- Falutz J, Allas S, Blot K, et al. N Engl J Med, 357(23), 2359-70, 2007.
- Falutz J, Mamputu JC, Potvin D, et al. J Clin Endocrinol Metab, 95(9), 4291-304, 2010.
- Wang Y, Tomlinson B. Expert Opin Investig Drugs, 18(3), 303-10, 2009.
- Grunfeld C, Dritselis A, Kirkpatrick P. Tesamorelin. Nat Rev compound Discov, 10(2), 95-6, 2011.
- Stanley TL, Chen CY, Branch KL, Makimura H, Grinspoon SK. J Clin Endocrinol Metab, 96(1), 150-8, 2011.
- Dhillon S. Drugs, 71(8), 1071-91, 2011.
- Spooner LM, Olin JL. Ann Pharmacother, 46(2), 240-7, 2012.
- Stanley TL, Falutz J, Marsolais C, et al. Clin Infect Dis, 54(11), 1642-51, 2012.
- Stanley TL, Fourman LT, Feldpausch MN, et al. Lancet HIV, 6(12), e821-e830, 2019.
- Adrian S, Scherzinger A, Sanyal A, et al. J Frailty Aging, 8(3), 154-159, 2019.
- Baker LD, Barsness SM, Borson S, et al. Arch Neurol, 69(11), 1420-9, 2012.
- Lopez J, Quan A, Budihardjo J, et al. Growth Hormone Improves Nerve Regeneration, Muscle Re-innervation, and Functional Outcomes After Chronic Denervation Injury. Sci Rep, 9(1), 3117, 2019.
- Grinspoon SK, Fourman L, Stanley T, et al. Impact of Tesamorelin on Cardiovascular Disease Risk Prediction Scores: Subanalysis. Open Forum Infect Dis, 12(Suppl 1), 2025.
- Clemmons DR, Miller S, Mamputu JC. PLoS One, 12(6), e0179538, 2017.
- Makimura H, Feldpausch MN, Rope AM, et al. J Clin Endocrinol Metab, 97(12), 4769-79, 2012.
- Fourman LT, Czerwonka N, Feldpausch MN, et al. AIDS, 31(16), 2253-9, 2017.
- Mangili A, Falutz J, Mamputu JC, et al. PLoS One, 10(10), e0140358, 2015.
- Lake JE, La K, Erlandson KM, et al. AIDS, 35(9), 1395-1402, 2021.
- Makimura H, Murphy CA, Feldpausch MN, Grinspoon SK. J Clin Endocrinol Metab, 99(1), 338-343, 2014.
- Stanley TL, Feldpausch MN, Oh J, et al. JAMA, 312(4), 380-9, 2014.
- Ellis RJ, Vaida F, Hu K, et al. J Infect Dis, 231(5), 1230-1238, 2025.
- Falutz J, Potvin D, Mamputu JC, et al. J Acquir Immune Defic Syndr, 53(3), 311-22, 2010.
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