Synthesis and pharmacological evaluation of indolinone derivatives as novel ghrelin receptor antagonists

…, P Marini, R Avallone, M Zanchet, S Bandiera…

Index: Puleo, Letizia; Marini, Pietro; Avallone, Roberta; Zanchet, Marco; Bandiera, Silvio; Baroni, Marco; Croci, Tiziano Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 18 p. 5623 - 5636

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Citation Number: 16

Abstract

The ghrelin receptor is a G-protein-coupled receptor (GPCR) widely expressed in the brain, stomach and the intestine. It was firstly identified during studies aimed to find synthetic modulators of growth hormone (GH) secretion. GHSR and its endogenous ligand ghrelin were found to be involved in hunger response. Through food intake regulation, they could affect body weight and adiposity. Thus GHSR antagonists rapidly became an attractive ...