A fluorescent tripeptide probe derived by coupling fluorescein to H-Dmt-Tic-Glu-NH2 was developed to interact with delta-opioid receptors with high affinity (K-i = 0.035 nM) and selectivity (K-i(mu)/K-i(delta) = 4371). It acts as an irreversible delta-opioid receptor antagonist, and binding to NG108-15 cells is blocked by the standard nonpeptidic delta-opioid receptor antagonist naltrindole. This probe should prove useful in the study of the distribution of delta-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 / Balboni, G.; Salvadori, S.; DAL PIAZ, A.; Bortolotti, F.; Argazzi, R.; Negri, Lucia; Lattanzi, Roberta; Bryant, S. D.; Jinsmaa, Y.; Lazarus, L. H.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 47:(2004), pp. 6541-6546. [10.1021/jm040128h]
Highly Selective Fluorescent Analogue of the Potent delta-Opioid Receptor Antagonist Dmt-Tic
NEGRI, Lucia;LATTANZI, Roberta;
2004
Abstract
A fluorescent tripeptide probe derived by coupling fluorescein to H-Dmt-Tic-Glu-NH2 was developed to interact with delta-opioid receptors with high affinity (K-i = 0.035 nM) and selectivity (K-i(mu)/K-i(delta) = 4371). It acts as an irreversible delta-opioid receptor antagonist, and binding to NG108-15 cells is blocked by the standard nonpeptidic delta-opioid receptor antagonist naltrindole. This probe should prove useful in the study of the distribution of delta-opioid receptors in tissues and the internalization of opioid peptides during signal transduction.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
