Article

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

Dipartimento di Scienze Farmaceutiche, Università di Pisa, via Bonanno 6, 56126 Pisa, Italy.
Bioorganic & Medicinal Chemistry Letters (impact factor: 2.55). 01/2002; 11(23):3023-6. pp.3023-6
Source: PubMed

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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Keywords

adenosine receptors
 
affinity
 
CHO cells
 
compound 2d
 
human A(3)-AR
 
human receptor subtype
 
linear alkyl spacers
 
NBD-moieties
 
New fluorescent ligands
 
potential suitability
 
trafficking studies