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Literature DB >> 11714602

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

M Macchia¹, 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.

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.

Entities: Chemical Gene Species

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Year: 2001 PMID： 11714602 DOI： 10.1016/s0960-894x(01)00610-2

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

7 in total

Review 1. Fluorescent approaches for understanding interactions of ligands with G protein coupled receptors.

Authors: Rajashri Sridharan; Jeffrey Zuber; Sara M Connelly; Elizabeth Mathew; Mark E Dumont
Journal: Biochim Biophys Acta Date: 2013-09-18

2. Synthesis of BODIPY derivatives substituted with various bioconjugatable linker groups: a construction kit for fluorescent labeling of receptor ligands.

Authors: Fabian Heisig; Sabrina Gollos; Sven J Freudenthal; Ali El-Tayeb; Jamshed Iqbal; Christa E Müller
Journal: J Fluoresc Date: 2013-09-20 Impact factor: 2.217

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

Review 1. Fluorescent approaches for understanding interactions of ligands with G protein coupled receptors.

2. Synthesis of BODIPY derivatives substituted with various bioconjugatable linker groups: a construction kit for fluorescent labeling of receptor ligands.

Review 3. Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands.

4. Design, Synthesis, and Pharmacological Evaluation of Fluorescent and Biotinylated Antagonists of ρ1 GABAC Receptors.

Review 5. Fluorescent ligands for adenosine receptors.

Review 6. Chemical Probes for the Adenosine Receptors.

7. An Affinity-Based Probe for the Human Adenosine A_2A Receptor.

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

Review 1. Fluorescent approaches for understanding interactions of ligands with G protein coupled receptors.

2. Synthesis of BODIPY derivatives substituted with various bioconjugatable linker groups: a construction kit for fluorescent labeling of receptor ligands.

Review 3. Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands.

4. Design, Synthesis, and Pharmacological Evaluation of Fluorescent and Biotinylated Antagonists of ρ1 GABAC Receptors.

Review 5. Fluorescent ligands for adenosine receptors.

Review 6. Chemical Probes for the Adenosine Receptors.

7. An Affinity-Based Probe for the Human Adenosine A2A Receptor.

7. An Affinity-Based Probe for the Human Adenosine A_2A Receptor.