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Ghrelin receptor modulators and their therapeutic potential.
Luca Costantino1, Daniela Barlocco
1Università di Modena e Reggio Emilia, Dipartimento di Scienze Farmaceutiche, Via Campi 183, 41100 Modena, Italy. luca.costantino@unimore.it
Future Medicinal Chemistry
|March 24, 2011
Summary
New nonpeptidic compounds targeting the ghrelin receptor show promise for metabolic and growth disorders. These compounds include agonists that increase fat-free mass and antagonists that reduce food intake, offering potential therapeutic applications.
Area of Science:
- Medicinal Chemistry
- Endocrinology
- Pharmacology
Background:
- Ghrelin, a peptide hormone primarily from the stomach, regulates growth hormone (GH) release and plays a role in nutrition, body composition, and organ function.
- Initial drug discovery efforts focused on GH secretagogues (ghrelin-receptor agonists) as anabolic agents, but faced market entry challenges.
Purpose of the Study:
- To explore novel nonpeptidic compounds modulating the ghrelin receptor for therapeutic potential.
- To investigate the effects of ghrelin receptor agonists and antagonists on body composition, food intake, and GH secretion.
Main Methods:
- Discovery and characterization of novel nonpeptidic oxindole agonists, triazole/2,4-diaminopyrimidine-based antagonists, and quinazolinone antagonists.
- Evaluation of compound efficacy in preclinical models related to metabolic and growth regulation.
Main Results:
- Oxindole agonists demonstrated an increase in fat-free mass.
- Ghrelin receptor antagonists effectively reduced food intake without inhibiting agonist-stimulated GH secretion.
- Other antagonists (quinazolinones) showed potential as antiobesity and antidiabetic agents, while inverse agonists reduced weight gain.
Conclusions:
- Novel nonpeptidic compounds targeting the ghrelin receptor offer diverse therapeutic possibilities.
- These findings highlight the significant and increasing importance of ghrelin receptor modulators in medicinal chemistry research for various pathological conditions.
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