7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors.
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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ABSTRACT: The design, development and use of small molecule fluorescent ligands to directly or indirectly study receptors, enzymes and other targets in the central nervous system (CNS) have in recent years become an intense area of investigation, especially for use in quantitative, sensitive and direct binding assays to study target proteins, both intra- and extra-cellularly and as prodromal diagnostic tools. The rapid development of ultra sensitive fluorescent spectroscopic approaches, such as fluorescence correlation spectroscopy, flow cytometry, confocal laser scanning microscopy, fluorescence polarization and multi-photon fluorescence microscopy, is opening new scenarios for the use of small molecule fluorescent ligands in the study of CNS pharmacology. In combination with effective and efficient labeling protocols, these techniques offer enormous possibilities at both micro- and nanometer level to develop parallel multifaceted tools in pharmacological and related sciences. This review covers small molecule fluorescent ligands that have been applied to study proteins and other targets in the CNS through visualisation by means of fluorescent imaging technologies.Mini Reviews in Medicinal Chemistry 06/2012; · 2.53 Impact Factor