POTENT LIGANDS OF THE GHRELIN RECEPTOR

摘要

The present invention relates to highly potent ligands at the ghrelin receptor to influence food intake or other conditions.

主权项

1. A peptide comprising the amino acid sequence
X1—X2—X3—X4—X5—NR1R2, wherein
X1 represents an amino acid selected from the group consisting of Lys and Arg;X2 and X4 each independently represents an aromatic amino acid, with the proviso that at least one of X2 and X4 is not D- or L-tryptophane;X3 represents a hydrophobic amino acid;X5 represents Leu-Leu; andR1 and R2 are each independently hydrogen or an optionally substituted hydrocarbon group; or, alternatively, R1 and R2 together with the nitrogen atom to which they are attached form a 5- or 6-membered ring; further wherein said peptide is capable of increasing or decreasing the constitutive activity of a ghrelin receptor by at least 10%, when contacted with said ghrelin receptor at a concentration of 10−7 M in an inositol turnover assay in COS-7 cells expressing the ghrelin receptor.