Hexarelin — Growth hormone secretagogue — synthetic hexapeptide GHRP class / GHS-R1a agonist with cardioprotective properties
Hexarelin is a synthetic hexapeptide (His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2) that acts as a potent GHS-R1a agonist with the strongest GH-releasing potency among the GHRP class (more potent than GHRP-6 and GHRP-2). Unlike GHRP-6, it does not significantly stimulate appetite (lower ghrelin-pathway activity at the hypothalamic level). Key mechanism: GHS-R1a activation in the pituitary and hypothalamus triggers pulsatile GH release; additionally, GHS-R1a is expressed in cardiac tissue where hexarelin exerts direct cardioprotective effects independent of GH secretion — reduces ischemia-reperfusion injury, improves cardiac contractility, and activates PAI-1 (protective anti-apoptotic pathway in cardiomyocytes). Notably, hexarelin's GH-releasing effect undergoes rapid tachyphylaxis with continuous dosing — cycling is essential.
نظرة عامة
هذه الصفحة جزء من مكتبة المركّبات المُصنَّفة بالأدلة في Hormonaly. جميع الادعاءات السريرية مرتبطة بمصادر علمية مُحكَّمة عبر خط أنابيب التحقق المزدوج للاستشهادات.
فئة المركّب
Growth hormone secretagogue — synthetic hexapeptide GHRP class / GHS-R1a agonist with cardioprotective properties
آلية العمل
Hexarelin is a synthetic hexapeptide (His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2) that acts as a potent GHS-R1a agonist with the strongest GH-releasing potency among the GHRP class (more potent than GHRP-6 and GHRP-2). Unlike GHRP-6, it does not significantly stimulate appetite (lower ghrelin-pathway activity at the hypothalamic level). Key mechanism: GHS-R1a activation in the pituitary and hypothalamus triggers pulsatile GH release; additionally, GHS-R1a is expressed in cardiac tissue where hexarelin exerts direct cardioprotective effects independent of GH secretion — reduces ischemia-reperfusion injury, improves cardiac contractility, and activates PAI-1 (protective anti-apoptotic pathway in cardiomyocytes). Notably, hexarelin's GH-releasing effect undergoes rapid tachyphylaxis with continuous dosing — cycling is essential.
الوضع التنظيمي
NOT FDA approved. NOT EMA approved. Investigational peptide. No approved indication in any jurisdiction.
مستوى الأدلة
C — Human pharmacological studies confirm potent GH-releasing effect (PMID: 7490562, 7883661); Phase 2 cardiac data in humans is limited; no Phase 3 RCTs completed for any indication; not FDA/EMA approved.