Literature DB >> 11277527

Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool.

J E van Muijlwijk-Koezen1, H Timmerman, R P van der Sluis, A C van de Stolpe, W M Menge, M W Beukers, P H van der Graaf, M de Groote, A P IJzerman.   

Abstract

A new preparative synthetic route for the irreversible adenosine A1 antagonist 8-cyclopentyl-3-N-[3-((3-(4-fluorosulphonyl)benzoyl)-oxy)-propyl]-1-N-propyl-xanthine (FSCPX, 1) is described. The availability of ample amounts of the irreversible antagonist FSCPX allowed us to use FSCPX as a research tool for adenosine A1 receptors in in vivo experiments. After verification of the irreversible antagonistic function of FSCPX in in vitro experiments, FSCPX was used successfully as a 'receptor knock-down' tool in in vivo experiments on conscious rats.

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Year:  2001        PMID： 11277527     DOI： 10.1016/s0960-894x(01)00069-5

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


  10 in total

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3.  Mass spectrometry-based ligand binding assays on adenosine A1 and A2A receptors.

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4.  A Non-imaging High Throughput Approach to Chemical Library Screening at the Unmodified Adenosine-A3 Receptor in Living Cells.

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Journal:  Front Pharmacol       Date:  2017-12-13       Impact factor: 5.810

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Review 6.  Chemical Probes for the Adenosine Receptors.

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Review 8.  International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update.

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Journal:  Pharmacol Rev       Date:  2022-04       Impact factor: 25.468

9.  Scintillation proximity assay (SPA) as a new approach to determine a ligand's kinetic profile. A case in point for the adenosine A1 receptor.

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Journal:  Purinergic Signal       Date:  2015-12-09       Impact factor: 3.765

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

Authors:  Xue Yang; Thomas J M Michiels; Coen de Jong; Marjolein Soethoudt; Niek Dekker; Euan Gordon; Mario van der Stelt; Laura H Heitman; Daan van der Es; Adriaan P IJzerman
Journal:  J Med Chem       Date:  2018-08-21       Impact factor: 7.446
  10 in total

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