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A Novel Non-Peptidic Agonist of the Ghrelin Receptor with Orexigenic Activity In vivo.

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.

SUBMITTER: Pastor-Cavada E

PROVIDER: S-EPMC5098229 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature

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A Novel Non-Peptidic Agonist of the Ghrelin Receptor with Orexigenic Activity In vivo.

Pastor-Cavada Elena E Pardo Leticia M LM Kandil Dalia D Torres-Fuentes Cristina C Clarke Sarah L SL Shaban Hamdy H McGlacken Gerard P GP Schellekens Harriet H

Scientific reports 20161107

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 end ...[more]

PMID: 27819353

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