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acyl-ghrelin
- Development stage
- Phase 1
- Modality
- Recombinant Proteins and Enzymes, Peptides
- Administration
- Intravenous, Subcutaneous, Intranasal
01
Overview
Acyl-ghrelin is the active, acylated form of the endogenous peptide hormone ghrelin. It is produced primarily in the stomach and requires an n-octanoylation at serine 3 for biological activity. Acyl-ghrelin acts as a potent agonist of the growth hormone secretagogue receptor 1a (GHSR1a), stimulating appetite and food intake via hypothalamic pathways. Beyond its orexigenic effects, synthetic human acyl-ghrelin has demonstrated cardiovascular benefits in clinical studies—most notably improving cardiac output and stroke volume in patients with heart failure with reduced ejection fraction (HFrEF) without causing hypotension or arrhythmias. Mechanistically, it increases myocardial contractility independently of calcium mobilization by reducing troponin I phosphorylation[1][5]. Acyl-ghrelin has also been studied for its roles in metabolic regulation and neuropsychiatric processes.
- Other names
- acylated ghrelinoctanoyl ghrelin
02
Targets
GHSR (Growth hormone secretagogue receptor)
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