A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity in vivo

dc.contributor.authorPastor-Cavada, Elena
dc.contributor.authorPardo, Leticia M.
dc.contributor.authorKandil, Dalia
dc.contributor.authorTorres-Fuentes, Cristina
dc.contributor.authorClarke, Sarah L.
dc.contributor.authorShaban, Hamdy
dc.contributor.authorMcGlacken, Gerard P.
dc.contributor.authorSchellekens, Harriët
dc.contributor.funderScience Foundation Irelanden
dc.contributor.funderIrish Research Council for Science, Engineering and Technologyen
dc.contributor.funderUniversidad de Sevillaen
dc.contributor.funderPfizer Process Development Centre, Cork
dc.date.accessioned2016-12-12T17:24:16Z
dc.date.available2016-12-12T17:24:16Z
dc.date.issued2016-11-07
dc.date.updated2016-12-09T12:52:42Z
dc.description.abstractLoss 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.en
dc.description.sponsorshipScience Foundation Ireland (SFI/12/IP/1315 and SFI/12/RC/2275); Irish Research Council for Science and Technology and Pfizer Process Development Centre, Cork (Enterprise Partnership Scheme)en
dc.description.statusPeer revieweden
dc.description.versionPublished Versionen
dc.format.mimetypeapplication/pdfen
dc.identifier.articleid36456
dc.identifier.citationPastor-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/srep36456en
dc.identifier.doi10.1038/srep36456
dc.identifier.endpage13en
dc.identifier.issn2045-2322
dc.identifier.journaltitleScientific Reportsen
dc.identifier.startpage1en
dc.identifier.urihttps://hdl.handle.net/10468/3370
dc.identifier.volume6en
dc.language.isoenen
dc.publisherNature Publishing Groupen
dc.rights© 2016, the Authors. This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/en
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.subjectGrowth hormone secretagogueen
dc.subjectFood intakeen
dc.subjectMedicinal chemistryen
dc.subjectOlder adultsen
dc.subjectMechanismsen
dc.subjectSecretionen
dc.subjectFluorineen
dc.subjectPeptideen
dc.subjectHealthyen
dc.subjectAnorexia-cachexiaen
dc.titleA novel non-peptidic agonist of the ghrelin receptor with orexigenic activity in vivoen
dc.typeArticle (peer-reviewed)en
Files
Original bundle
Now showing 1 - 1 of 1
Loading...
Thumbnail Image
Name:
1737.pdf
Size:
1.47 MB
Format:
Adobe Portable Document Format
Description:
Published Version
License bundle
Now showing 1 - 1 of 1
Loading...
Thumbnail Image
Name:
license.txt
Size:
2.71 KB
Format:
Item-specific license agreed upon to submission
Description: