Ipamorelin: Mechanism of Action
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Comprar peptídeo Ipamorelin 10mgMecanismo de Acao
Ipamorelin ativa the GHS-R1a (ghrelin receptor) on pituitary somatotroph cells with an in vitro EC₅₀ of 1.3 ± 0.4 nmol/L e em vivo ED₅₀ of 2.3 nmol/kg (swine). Binding desencadeia phospholipase C (PLC) ativacao via Gα₁₁/q → IP3 → intracellular Ca²⁺ release → GH vesicle exocytosis — a pathway distinto(a) de GHRH's cAMP signaling.[1][2]
Receptor & Signaling Profile
| Target | Action | Downstream Effect |
|---|---|---|
| GHS-R1a (Ghrelin Receptor) | Selective agonist | PLC → IP3 → Ca²⁺ → GH vesicle exocytosis |
| cAMP (co-stimulation) | Enhances pre-estimulou adenylyl cyclase | Co-stimulation of GHS-R1a and GHRH-R has been studied in pituitary-cell and rodent models |
| Enteric Cholinergic Neurons | Activates excitatory neurons (atropine/TTX-sensitive) | Accelerates gastric motility and emptying |
Ipamorelin's selectivity is exceptional: it does NOT stimulate ACTH, cortisol, FSH, LH, prolactin, or TSH — even at 200× the ED₅₀. Adicionalmente, cronico(a) administration nao desensitize somatotrophs, diferentemente de GHRH que induz homologous down-regulacao.[1][7]
Half-life ~2 h (published PK).[2]
vs. Related Compounds
| Caracteristica | Ipamorelin | GHRP-6 / GHRP-2 | GHRH |
|---|---|---|---|
| Selectivity | HIGH — GH only | LOW — GH + ACTH + cortisol + prolactin | Selective for GH |
| Desensibilizacao | NO | Partial | YES (homologous) |
| Primary Signaling | PLC / Ca²⁺ | PLC / Ca²⁺ | cAMP |
| Half-Life (Human) | ~2 hours | Shorter (5× faster depuracao) | Minutes |
“Resumo da Pesquisa Pre-clinica Key Preclinical Studies EstudoModeloPrincipais AchadosRef Raun et al.”
Referencias
- Raun K, Hansen BS, Johansen NL, et al. Ipamorelin, the primeiro(a) selective hormonio do crescimento secretagogue. European Journal of Endocrinology. 1998;139(5):552-561.
- Gobburu JVS, Agersø H, Jusko WJ, Ynddal L. Pharmaceutical Research. 1999;16(9):1412-1416.
- Johansen PB, Nowak J, Skjaerbaek C, et al. Ipamorelin, a novo(a) growth-hormone-releasing peptide, induz longitudinal bone growth in rats. Growth Hormone & IGF Research. 1999;9(2):106-113.
- Venkova K, Mann W, Nelson R, Greenwood-Van Meerveld B. JPET. 2009;329(3):1110-1116.
- Greenwood-Van Meerveld B, Tyler K, Mohammadi E, Pietra C. Journal of Experimental Pharmacology. 2012;4:149-155.
- Beck DE, Sweeney WB, McCarter MD. Int J Colorectal Dis. 2014;29(12):1527-1534.
- Jiménez-Reina L, Cañete R, de la Torre MJ, Bernal G. European Journal of Anatomy. 2002;6(1):37-45.
- Svensson J, Lall S, Dickson SL, Jansson JO. Journal of Endocrinology. 2000;165:569-577.
- Lall S, Tung LY, Ohlsson C, Jansson JO, Dickson SL. Growth hormone (GH)-independent estimulacao of adiposity by GH secretagogues. BBRC. 2001;280(1):132-138.
- Adeghate E, Ponery AS. Mechanism of ipamorelin-evoked insulin release do(a) pancreas of normal and ratos diabeticos. Neuro Endocrinology Letters. 2004;25(6):403-406.
- Johansen PB, Hansen KT, Andersen JV, Johansen NL. Xenobiotica. 1998;28(11):1083-1092.
- Andersen NB, Malmlöf K, Johansen PB, Oxlund H. Growth Hormone & IGF Research. 2001;11(5):266-272.
- Hansen TK, Ankersen M, Raun K, Hansen BS. Highly Potent Growth Hormone Secretagogues: Hybrids of NN703 and Ipamorelin. Bioorganic & Medicinal Chemistry Letters. 2001;11(14):1915-1918.
- Lu Z, Ngan MP, Liu JYH, Rudd JA. Physiology & Behavior. 2024.
- Sinha DK, Balasubramanian A, Tatem AJ, et al. Translational Andrology and Urology. 2020;9(Suppl 2):S149-S159.
- Thøgersen H, Johansen NL, Lau J, et al. A New Series of Highly Potent Growth Hormone-Releasing Peptides Derived from Ipamorelin. Journal of Medicinal Chemistry. 1998;41.
- Mohammadi E, Bhatt V, Bhatt AB, Pietra C, Greenwood-Van Meerveld B. Ipamorelin atenua visceral and somatic nociception through periferico(a) ghrelin receptor mechanisms. 2020.
- U.S. Food & Drug Administration. FDA Evaluation of Ipamorelin-Related Substancia Farmaceutica a Granels. FDA Pharmacy Compounding Advisory Committee. 2024.
- World Anti-Doping Agency. WADA Lista de Substancias Proibidas — S2: Hormonios Peptidicos, Fatores de Crescimento, Substancias Relacionadas e Mimeticos. 2024.
- Polvino WJ. US Patent 8,039,456 B2.
- Thøger Nielsen K, et al. Validated screening method for GH-releasing peptides using UHPLC-HRMS on dried blood spots. Drug Testing and Analysis. 2021.
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