PAR-2 AGONIST

摘要

A pharmaceutical composition for the prevention/treatment of a disease associated with PAR-2 which comprises a compound represented by the general formula (1) below or a salt thereof or a solvate thereof and a pharmaceutically acceptable carrier; a method for prevention or treatment of a disease associated with PAR-2 by using the compound or salt thereof or solvate thereof; and use of the compound or salt thereof or solvate thereof in the preparation of the pharmaceutical composition: Ar-CO-AA<SUB>1</SUB>-AA<SUB>2</SUB>-AA<SUB>3</SUB>-AA<SUB>4</SUB>-NH-X-Y (1) wherein: Ar represents a phenyl or aromatic heterocyclic group which may have a substituent; AA<SUB>1</SUB> represents a hydrophobic amino acid; AA<SUB>2</SUB> represents an amino acid which does not have a substituent carrying 2 or more carbon atoms; AA<SUB>3</SUB> represents an amino acid which does not have a substituent carrying 2 or more carbon atoms; AA<SUB>4</SUB> represents a basic amino acid; X represents a divalent, straight-chain or branched saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms; and Y represents a basic substituent, a straight-chain, branched or cyclic saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms, or an aromatic hydrocarbon group having 6 to 10 carbon atoms. The compound represented by the general formula (1) has a remarkably improved PAR-2 activating ability compared to a peptide composed of six amino acid residues (tethered receptor agonist peptide: TRAP) in spite of the fact that the compound has a fewer number of constituent amino acid residues than TRAP.