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Review
. 2011:(200):151-99.
doi: 10.1007/978-3-642-13443-2_6.

Xanthines as adenosine receptor antagonists

Christa E Müller  1 , Kenneth A Jacobson
Affiliations
Review

Xanthines as adenosine receptor antagonists

Christa E Müller et al. Handb Exp Pharmacol. 2011.

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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Figures

Fig. 1
Fig. 1
8-Unsubstituted xanthine derivatives
Fig. 2
Fig. 2
8-Phenyl- and 8-phenylalkyl-substituted xanthines and heteroaromatically substituted derivatives
Fig. 2
Fig. 2
8-Phenyl- and 8-phenylalkyl-substituted xanthines and heteroaromatically substituted derivatives
Fig. 3
Fig. 3
8-Cycloalkylxanthines
Fig. 4
Fig. 4
8-Styrylxanthines and configurationally stable analogs
Fig. 5
Fig. 5
Deazaxanthines and azaxanthines
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Fig. 6
Tricyclic xanthine derivatives
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Fig. 7
Functionalized xanthines as molecular probes
Fig. 7
Fig. 7
Functionalized xanthines as molecular probes
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References

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