Cortistatin

Also known as: CORT, O00230

Cortistatin is a neuropeptide structurally related to somatostatin, encoded by the *CORT* gene (UniProt O00230). Its mechanism of action involves binding to all five somatostatin receptor subtypes (SSTR1–5) with high affinity, similar to somatostatin, but it also exhibits distinct properties, including binding to the ghrelin receptor (GHS-R1a) and the Mas-related G protein-coupled receptor MRGPRX2. This dual receptor interaction enables cortistatin to modulate neurotransmission, immune responses, and endocrine signaling, with effects on sleep regulation, inflammation, and cell proliferation. Key research findings indicate that cortistatin promotes slow-wave sleep, reduces inflammatory cytokine release (e.g., TNF-α, IL-6) in macrophages, and exhibits neuroprotective effects in models of neurodegeneration. Preclinical studies have shown its ability to inhibit tumor cell growth in certain cancers, though results vary by cell type. Its anti-inflammatory and immunomodulatory properties are distinct from somatostatin, suggesting unique therapeutic potential, but human data remain limited. Clinically, cortistatin is in the experimental stage, with no approved indications. Its potential applications include treating inflammatory disorders (e.g., rheumatoid arthritis, sepsis), sleep disturbances, and neurological conditions. However, challenges such as short half-life and lack of selective analogs hinder translation. Further research is needed to clarify its receptor-specific effects and safety profile. For research purposes only — not medical advice.

Key data

Mechanism of action

Precursor of neuropeptides that bind to all somatostatin receptor (SSTR) subtypes (PubMed:9125122). Inhibits cAMP production induced by forskolin through SSTRs (PubMed:9125122)

Research & studies

Frequently asked questions

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