A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity in vivo
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Published Version
Date
2016-11-07
Authors
Pastor-Cavada, Elena
Pardo, Leticia M.
Kandil, Dalia
Torres-Fuentes, Cristina
Clarke, Sarah L.
Shaban, Hamdy
McGlacken, Gerard P.
Schellekens, Harriƫt
Journal Title
Journal ISSN
Volume Title
Publisher
Nature Publishing Group
Published Version
Abstract
Loss of appetite in the medically ill and ageing populations is a major health problem and a significant symptom in cachexia syndromes, which is the loss of muscle and fat mass. Ghrelin is a gut-derived hormone which can stimulate appetite. Herein we describe a novel, simple, non-peptidic, 2-pyridone which acts as a selective agonist for the ghrelin receptor (GHS-R1a). The small 2-pyridone demonstrated clear agonistic activity in both transfected human cells and mouse hypothalamic cells with endogenous GHS-R1a receptor expression. In vivo tests with the hit compound showed significant increased food intake following peripheral administration, which highlights the potent orexigenic effect of this novel GHS-R1a receptor ligand.
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Keywords
Growth hormone secretagogue , Food intake , Medicinal chemistry , Older adults , Mechanisms , Secretion , Fluorine , Peptide , Healthy , Anorexia-cachexia
Citation
Pastor-Cavada, E., Pardo, L. M., Kandil, D., Torres-Fuentes, C., Clarke, S. L., Shaban, H., McGlacken, G. P. and Schellekens, H. (2016) 'A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity in vivo', Scientific Reports, 6, 36456 (13pp). doi:10.1038/srep36456