H-Dmt-D-Arg-Phe-Lys-NH2 ([Dmt1]DALDA) binds with high affinity and selectivity to the í 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 í agonist into a potent and selective ä antagonist H-Dmt-Tic-Phe-Lys(Z)-OH. Such a ä antagonist could be used as a pharmacological tool.

From the potent and selective mu opioid receptor agonist H-Dmt-D-Arg-Phe-Lys-NH2 to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH

SALVADORI, Severo;ROMAGNOLI, Romeo;
2005

Abstract

H-Dmt-D-Arg-Phe-Lys-NH2 ([Dmt1]DALDA) binds with high affinity and selectivity to the í 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 í agonist into a potent and selective ä antagonist H-Dmt-Tic-Phe-Lys(Z)-OH. Such a ä antagonist could be used as a pharmacological tool.
2005
Balboni, G; Cocco, Mt; Salvadori, Severo; Romagnoli, Romeo; Sasaki, Y; Okada, Y; Bryant, Sd; Jinsmaa, Y; Lazarus, Lh
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/516938
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