Title |
A Novel Non-Peptidic Agonist of the Ghrelin Receptor with Orexigenic Activity In vivo
|
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Published in |
Scientific Reports, November 2016
|
DOI | 10.1038/srep36456 |
Pubmed ID | |
Authors |
Elena Pastor-Cavada, Leticia M. Pardo, Dalia Kandil, Cristina Torres-Fuentes, Sarah L. Clarke, Hamdy Shaban, Gerard P. McGlacken, Harriet Schellekens |
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. |
X Demographics
Geographical breakdown
Country | Count | As % |
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United States | 1 | 33% |
Unknown | 2 | 67% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 3 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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Unknown | 27 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
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Student > Master | 5 | 19% |
Student > Bachelor | 4 | 15% |
Student > Ph. D. Student | 4 | 15% |
Researcher | 3 | 11% |
Student > Doctoral Student | 2 | 7% |
Other | 4 | 15% |
Unknown | 5 | 19% |
Readers by discipline | Count | As % |
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Chemistry | 5 | 19% |
Neuroscience | 3 | 11% |
Nursing and Health Professions | 3 | 11% |
Agricultural and Biological Sciences | 2 | 7% |
Pharmacology, Toxicology and Pharmaceutical Science | 2 | 7% |
Other | 6 | 22% |
Unknown | 6 | 22% |