Document Report Card

ID: ALA1145172

Journal: J Med Chem

Title: From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH.

Authors: Balboni G, Cocco MT, Salvadori S, Romagnoli R, Sasaki Y, Okada Y, Bryant SD, Jinsmaa Y, Lazarus LH.

Abstract: H-Dmt-d-Arg-Phe-Lys-NH(2) ([Dmt(1)]DALDA) binds with high affinity and selectivity to the mu opioid receptor and is a potent and long-acting analgesic. Substitution of d-Arg in position 2 with Tic and masking of the lysine amine side chain by Z protection and of the C-terminal carboxylic function instead of the amide function transform a potent and selective mu agonist into a potent and selective delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH. Such a delta antagonist could be used as a pharmacological tool.

CiteXplore: 16107162

DOI: 10.1021/jm0504959