A fluorescent tripeptide probe derived by coupling fluorescein to H-Dmt-Tic-Glu-NH2 was developed to interact with ä-opioid receptors with high affinity (Ki ) 0.035 nM) and selectivity (Kií/Kiä ) 4371). It acts as an irreversible ä-opioid receptor antagonist, and binding to NG108-15 cells is blocked by the standard nonpeptidic ä-opioid receptor antagonist naltrindole. This probe should prove useful in the study of the distribution of ä-opioid receptors in tissues and the internalization of opioid peptides during signal transduction.

Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic

SALVADORI, Severo;DALPIAZ, Alessandro;ARGAZZI, Roberto;
2004

Abstract

A fluorescent tripeptide probe derived by coupling fluorescein to H-Dmt-Tic-Glu-NH2 was developed to interact with ä-opioid receptors with high affinity (Ki ) 0.035 nM) and selectivity (Kií/Kiä ) 4371). It acts as an irreversible ä-opioid receptor antagonist, and binding to NG108-15 cells is blocked by the standard nonpeptidic ä-opioid receptor antagonist naltrindole. This probe should prove useful in the study of the distribution of ä-opioid receptors in tissues and the internalization of opioid peptides during signal transduction.
2004
Balboni, G; Salvadori, Severo; Dalpiaz, Alessandro; Bortolotti, F; Argazzi, Roberto; Negri, L; Lattanzi, R; Bryant, Sd; Jinsmaa, Y; Lazarus, Lh...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/1209158
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