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Xanthines as Adenosine Receptor Antagonists

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Methylxanthines

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 200))

Abstract

The natural plant alkaloids caffeine and theophylline were the first adenosine receptor (AR) antagonists described in the literature. They exhibit micromolar affinities and are non-selective. A large number of derivatives and analogues were subsequently synthesized and evaluated as AR antagonists. Very potent antagonists have thus been developed with selectivity for each of the four AR subtypes.

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Acknowledgements

CEM is grateful for support by BMBF (BioPharma - Neuroallianz), DFG, DAAD, European Commission (ERANET Neuron), and the State of North-Rhine Westfalia (NRW International Research Graduate Schools BIOTECH-PHARMA and Chemical Biology). KAJ acknowledges support from the Intramural Research Program of NIIDK, NIH.

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  1. PharmaCenter Bonn, Pharmaceutical Sciences Bonn (PSB), University of Bonn, Pharmaceutical Institute, An der Immenburg 4, 53121, Bonn, Germany

    Christa E. Müller

  2. Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Building. 8A, Room B1A-19, 8 center Dr. 2089-0810 NIH, NIDDK, LBC, Bethesda, MD, USA

    Kenneth A. Jacobson

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Müller, C.E., Jacobson, K.A. (2011). Xanthines as Adenosine Receptor Antagonists. In: Methylxanthines. Handbook of Experimental Pharmacology, vol 200. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-13443-2_6

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