Synthesis and biological evaluation of an orally active ghrelin agonist that stimulates food consumption and adiposity in rats

LY444711 is an orally active ghrelin agonist that binds with good affinity and is a potent activator of the growth hormone secretagogue receptor 1a (GHS-R1a) receptor. In rat models of feeding behavior and pharmacology, LY444711 creates a positive energy balance and induces adiposity by stimulating...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-12, Vol.14 (23), p.5873-5876
Main Authors: Lugar, Charles W., Clay, Michael P., Lindstrom, Terry D., Woodson, Andrea L., Smiley, David, Heiman, Mark L., Dodge, Jeffrey A.
Format: Article
Language:English
Subjects:
Adipose Tissue - drug effects
Adipose Tissue - physiology
Administration, Oral
Animals
Biological and medical sciences
Drug Evaluation, Preclinical
Eating - drug effects
Eating - physiology
Energy expenditure
Feeding. Feeding behavior
Food consumption
Fundamental and applied biological sciences. Psychology
Ghrelin
Growth hormone secretagogues
Male
Medical sciences
Miscellaneous
Peptide Hormones - chemistry
Peptide Hormones - pharmacology
Pharmacology. Drug treatments
Rats
Rats, Long-Evans
Receptors, G-Protein-Coupled - agonists
Receptors, G-Protein-Coupled - physiology
Receptors, Ghrelin
Vertebrates: anatomy and physiology, studies on body, several organs or systems
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Summary:LY444711 is an orally active ghrelin agonist that binds with good affinity and is a potent activator of the growth hormone secretagogue receptor 1a (GHS-R1a) receptor. In rat models of feeding behavior and pharmacology, LY444711 creates a positive energy balance and induces adiposity by stimulating food consumption and sparing fat utilization. 2-(2-Amino-2-methyl-propionylamino)-5-phenyl-pentanoic acid {1-[1-(4-methoxy-phenyl)-1-methyl-2-oxo-2-pyrrolidin-1-yl-ethyl]-1 H-imidazol-4-yl}-amide (LY444711, 6) is an orally active ghrelin agonist that binds with high affinity to and is a potent activator of the growth hormone secretagogue receptor 1a (GHS-R1a) receptor. In rat models of feeding behavior and pharmacology, 6 creates a positive energy balance and induces adiposity by stimulating food consumption and sparing fat utilization. As an orally active ghrelin agonist, 6 represents a new pharmacological tool to investigate the orexigenic role of ghrelin in regulating energy homeostasis.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.09.027