The present invention provides novel conformationally-defined macrocycliccompounds that have been demonstrated to be selective modulators of theghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes,isoforms and variants thereof). Methods of synthesizing the novel compoundsare also described herein. These compounds are useful as agonists of theghrelin receptor and as medicaments for treatment and prevention of a range ofmedical conditions including, but not limited to, metabolic and/or endocrinedisorders, gastrointestinal disorders, cardiovascular disorders, obesity andobesity-associated disorders, central nervous system disorders, geneticdisorders, hyperproliferative disorders and inflammatory disorders.
