New fluorescent ligands for adenosine receptors (ARs), obtained by the insertion, in the N(6) position of NECA, of NBD-moieties with linear alkyl spacers of increasing length, proved to possess a high affinity and selectivity for the A(3) subtype expressed in CHO cells. In fluorescence microscopy assays, compound 2d, the most active and selective for human A(3)-AR, permitted visualization and localization of this human receptor subtype, showing its potential suitability for internalization and trafficking studies in living cells.
7-Nitrobenzofurazan (NBD)-Derivatives Of 5'-N-Ethylcarboxamidoadenosine (NECA) As New Fluorescent Probes For Human A3 Adenosine Receptors
MACCHIA, MARCO;BERTINI, SIMONE;DI BUSSOLO, VALERIA;GESI, MARCO;LUCACCHINI, ANTONIO;MINUTOLO, FILIPPO;NENCETTI, SUSANNA;MARTINI, CLAUDIA
2001-01-01
Abstract
New fluorescent ligands for adenosine receptors (ARs), obtained by the insertion, in the N(6) position of NECA, of NBD-moieties with linear alkyl spacers of increasing length, proved to possess a high affinity and selectivity for the A(3) subtype expressed in CHO cells. In fluorescence microscopy assays, compound 2d, the most active and selective for human A(3)-AR, permitted visualization and localization of this human receptor subtype, showing its potential suitability for internalization and trafficking studies in living cells.File in questo prodotto:
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