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When Ipamorelin binds to GHS-R1a, it triggers an intracellular signaling cascade: Receptor activation Ipamorelin binds the GHS-R1a receptor on pituitary somatotrophs Phospholipase C pathway Gq/11 protein coupling activates PLC, generating IP3 and DAG Calcium mobilization IP3-mediated calcium release from intracellular stores triggers GH vesicle exocytosis Pulsatile GH release Growth hormone is released in a physiological pulsatile pattern, preserving hypothalamic feedback A critical distinction in Ipamorelin's mechanism is that it preserves the hypothalamic-pituitary feedback axis

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Furthermore, besides regulating circulating IGF-I levels via its impact on the hepatic GH sensitivity, insulin also inhibits hepatic synthesis and secretion of IGF-binding protein-1 (IGFBP-1)