Background: Ghrelin is an endogenous ligand of the growth hormone secretagogue receptor (GHS-R) that functions as a short-term meal initiator and a long-term energy balance regulator. Antagonizing GHS-R could be a method to treat obesity. Objective: To review the published in vivo characterization of GHS-R antagonists between 2005 and 2008 and evaluate the validity of antagonizing GHS-R as a therapeutic strategy for obesity. Methods: Primary literature was searched using SciFinder and Google Scholar. Patents were searched using the European Patent Office and SciFinder. Results/conclusion: Several classes of small molecule GHS-R antagonists have been reported to be efficacious in rodent models for weight loss but none has advanced to human clinical trials. Antagonizing GHS-R as a therapy targeting the general obese population is a challenging strategy.
