Metabolic modulation of the growth hormone-releasing activity of hexarelin in man.
Maccario. M M; Arvat. E E; Procopio. M M; Gianotti. L L; Grottoli. S S; Imbimbo. B P BP; Lenaerts. V V; Deghenghi. R R; Camanni. F F; Ghigo. E E
Key Findings
- Hexarelin produces a much larger GH spike than GHRH (â62âŻÂ”g/L vs â20âŻÂ”g/L).
- Oral glucose or lipid infusion almost completely blocks GH release from GHRH but only reduces hexarelinâinduced GH by ~30â40%.
- Hexarelinâs GHâreleasing action is relatively resistant to metabolic inhibition by glucose and free fatty acids.
Practical Outcomes
- For biohackers aiming to boost GH for muscle, fat loss, or antiâaging, hexarelin can be effective without needing to fast. It may allow GH spikes even in a fed state, simplifying timing around meals. Start with low, subâcutaneous doses (e.g., 2âŻÂ”g/kg IV equivalent) and monitor IGFâ1 and side effects, as safety data are limited.
Summary
Hexarelin is a synthetic peptide that triggers a strong growth hormone (GH) surge, and unlike the natural hormone-releasing factor (GHRH), its effect isnât knocked down much by eating carbs or having high blood fats. In simple terms, you can still get a big GH boost from hexarelin even after a meal or when your blood is full of fatty acids.
Abstract
Hexarelin (His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2) is a new potent synthetic growth hormone (GH)-releasing hexapeptide. The mechanism of action of hexarelin in man has never been evaluated. Hexarelin may act directly on specific pituitary receptors and indirectly on the hypothalamus. To elucidate its mechanism of action in man, we studied the interaction of hexarelin with glucose and free fatty acids (FFA), two metabolic factors known to inhibit both basal and GH-releasing hormone (GHRH) stimulated GH secretion. Glucose is thought to inhibit GH secretion via stimulation of endogenous somatostatin release, whereas FFA could also act directly on somatotrope cells. Therefore, we investigated the effect of oral glucose (100 g) and lipid-heparin infusion (250 mL of a 10% lipid solution + 2,500 U heparin) on the GH response to a maximal dose (2 micrograms/kg intravenously [IV]) of hexarelin or GHRH in six normal men. Hexarelin elicited a clear-cut GH response (mean +/- SEM; peak, 62.6 +/- 8.0 micrograms/L) that was higher (P < .01) than that observed after GHRH (peak, 19.8 +/- 2.4 micrograms/L). Although similar increases in plasma glucose were observed with the two peptides, oral glucose almost abolished the GH response to GHRH (peak, 5.6 +/- 0.9 micrograms/L, P < .01) while only blunting the somatotrope response to hexarelin (peak, 38.4 +/- 7.9 micrograms/L, P < .05). Similarly, lipid-heparin infusion nearly abolished the GH response to GHRH (peak, 4.9 +/- 1.0 micrograms/L, P < .01) while only blunting the somatotrope response to hexarelin (peak, 34.2 +/- 4.5 micrograms/L, P < .05).(ABSTRACT TRUNCATED AT 250 WORDS)
Study Information
pubmed
1995
10.1016/0026-0495(95)90300-3
58
39