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EnglishA fluorescent tripeptide probe derived by coupling fluorescein to H-Dmt-Tic-Glu-NH2 was developed to interact with delta-opioid receptors with high affinity (Ki = 0.035 nM) and selectivity (Ki(mu)/Ki(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 L.; LATTANZI R.; BRYANT S.D.; JINSMAA Y.; LAZARUS L.H.. - 47(2004), pp. 6541-6546.
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| Titolo: | Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic |
| Autori: | |
| Data di pubblicazione: | 2004 |
| Rivista: | |
| Citazione: | 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 L.; LATTANZI R.; BRYANT S.D.; JINSMAA Y.; LAZARUS L.H.. - 47(2004), pp. 6541-6546. |
| 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 (Ki = 0.035 nM) and selectivity (Ki(mu)/Ki(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. |
| Handle: | http://hdl.handle.net/11584/12954 |
| Tipologia: | 1.1 Articolo in rivista |
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