7-nitrobenzofurazan (NBD) derivatives of 5 '-N-ethylearboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors

Authors
Macchia, M Salvetti, F Bertini, S Di Bussolo, V Gattuso, L Gesi, M Hamdan, M Klotz, KN Laragione, T Lucacchini, A Minutolo, F Nencetti, S Papi, C Tuscano, D Martini, C
Citation
M. Macchia et al., 7-nitrobenzofurazan (NBD) derivatives of 5 '-N-ethylearboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors, BIOORG MED, 11(23), 2001, pp. 3023-3026
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
23
Year of publication
2001
Pages
3023 - 3026
Database
ISI
SICI code
0960-894X(200112)11:23<3023:7(DO5'>2.0.ZU;2-Z
Abstract
New fluorescent ligands for adenosine receptors (ARs), obtained by the inse rtion, in the N-6 position of NECA, of NBD-moieties with linear alkyl space rs of increasing length, proved to possess a high affinity and selectivity for the A(3) subtype expressed in CHO cells. In fluorescence microscopy ass ays, compound 2d, the most active and selective for human A(3)-AR, permitte d visualization and localization of this human receptor subtype, showing it s potential suitability for internalization and trafficking studies in livi ng cells. (C) 2001 Elsevier Science Ltd. All rights reserved.