New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations.
Moulin. Aline A; Demange. Luc L; Ryan. Joanne J; Mousseaux. Delphine D; Sanchez. Pierre P; Bergé. Gilbert G; Gagne. Didier D; Perrissoud. Daniel D; Locatelli. Vittorio V; Torsello. Antonio A; Galleyrand. Jean-Claude JC; Fehrentz. Jean-Alain JA; Martinez. Jean J
Key Findings
- Compounds 5 and 34 are strong antagonists of hexarelin‑induced food intake in vivo
- The new antagonists do not trigger growth‑hormone release in rodents
- They do not interfere with growth‑hormone secretion caused by hexarelin
Practical Outcomes
- For biohackers, the study shows it’s possible to block hexarelin’s appetite effects without affecting growth hormone, but no ready‑to‑use product exists. It’s mainly a proof‑of‑concept for future drug development rather than an actionable protocol today.
Summary
Researchers made two new chemicals that can block the appetite‑boosting effect of the peptide hexarelin in animal tests, but they don’t change growth‑hormone levels. These compounds aren’t currently available as supplements or drugs for personal use.
Abstract
Ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure were synthesized and evaluated for their in vitro binding and biological activity. In this study, we explored the replacement of the alpha-aminoisobutyryl moiety by aromatic or heteroaromatic groups. Compounds 5 and 34 acted as potent in vivo antagonists of hexarelin-stimulated food intake. These two compounds did not stimulate growth hormone secretion in rodents and did not antagonize growth hormone secretion induced by hexarelin.
Study Information
pubmed
2008
2008-01-15T00:00:00.000Z
10.1021/jm701292s
71