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Hexarelin

Examorelin, HEX

Quick Stats
Studies 233
Trials 61
Score 2
2003 pubmed

Absence of binding of targeted analogs of somatostatin carrying cytotoxic radicals or radionuclides to growth hormone secretagogue receptors on human myocardium.

Halmos. Gabor G; Schally. Andrew V AV; Comaru-Schally. Ana Maria AM; Nagy. Attila A; Irimpen. Anand A

Key Findings

  • Human heart tissue has a high density of growth‑hormone secretagogue (GHS) receptors.
  • OctreoScan and two cytotoxic somatostatin analogs (AN‑162 and AN‑238) showed no specific binding to human myocardium.
  • The lack of binding suggests these compounds should not increase cardiac side‑effects when used clinically.

Practical Outcomes

  • For biohackers using hexarelin, this research confirms that similar peptide‑drug conjugates are unlikely to cause extra heart toxicity. It doesn’t alter hexarelin dosing or protocols, but adds confidence that related targeted therapies are not a cardiac safety concern.

Summary

The study looked at whether certain cancer‑targeting drugs that are linked to a peptide similar to hexarelin would stick to the heart’s growth‑hormone secretagogue receptors. They found none of the tested drugs bound to the heart tissue, meaning they probably won’t add extra heart risk. This doesn’t change how you use hexarelin itself, but it reassures that related peptide‑drug combos aren’t likely to harm the heart.

Abstract

Various peripheral human tissues express receptors for growth hormone secretagogue (GHS), the highest density being in the myocardium. It was also reported that some octapeptide analogs of somatostatin (SRIH) can displace radiolabeled Tyr-Ala-hexarelin from GHS receptors on the human pituitary and heart. Thus, it is possible that radionuclide analogs of SRIH such as OctreoScan and recently developed cytotoxic SRIH analogs containing doxorubicin (DOX) intended for targeted tumor therapy, could bind to these GHS receptors, compromising the safety of compounds of this type. Therefore, we determined the binding of OctreoScan and two cytotoxic SRIH analogs consisting of octapeptide carrier RC-121 and DOX (AN-162) or 2-pyrrolino-DOX (AN-238) to human myocardium specimens. None of these compounds displayed specific binding to the human heart indicating that the clinical use of SRIH analogs linked to anthracyclines or radionuclides should not be associated with increased cardiac side effects.

Study Information

Provider

pubmed

Year

2003

Date

2003-04-25T00:00:00.000Z

DOI

10.1016/s0024-3205(03)00181-4