7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors. |
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| Authors: | M Macchia F Salvetti S Bertini V Di Bussolo L Gattuso M Gesi M Hamdan K N Klotz T Laragione A Lucacchini F Minutolo S Nencetti C Papi D Tuscano C Martini |
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| Affiliation: | Dipartimento di Scienze Farmaceutiche, Università di Pisa, via Bonanno 6, 56126 Pisa, Italy. mmacchia@farm.unipi.it |
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| 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. |
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