International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors.
By B. Fredholm, Adriaan P. IJzerman, Kenneth A. Jacobson, Karl Norbert Klotz, J. Linden. Pharmacological Reviews, 2001
2,677 citations recorded by the source corpus.
Four adenosine receptors have been cloned and characterized from several mammalian species. The receptors are named adenosine A(1), A(2A), A(2B), and A(3). The A(2A) and A(2B) receptors preferably interact with members of the G(s) family of G proteins and the A(1) and A(3) receptors with G(i/o) proteins. However, other G protein interactions have also been described. Adenosine is the preferred endogenous agonist at all these receptors, but inosine can also activate the A(3) receptor. The levels of adenosine seen under basal conditions are sufficient to cause some activation of all the receptors, at least where they are abundantly expressed. Adenosine levels during, e.g., ischemia can activate all receptors even when expressed in low abundance. Accordingly, experiments with receptor antagonists and mice with targeted disruption of adenosine A(1), A(2A), and A(3) expression reveal roles for these receptors under physiological and particularly pathophysiological conditions. There are pharmacological tools that can be used to classify A(1), A(2A), and A(3) receptors but few drugs that interact selectively with A(2B) receptors. Testable models of the interaction of these drugs with their receptors have been generated by site-directed mutagenesis and homology-based modelling. Both agonists and antagonists are being developed as potential drugs.
Subfields: Cellular and Molecular Neuroscience, Molecular Biology, Physiology
View Paper: https://www.semanticscholar.org/paper/3aa930ed2eb42ccb104b17c42667a8ff6abac4a8
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Citations in the corpus
- Adenosine, an endogenous distress signal, modulates tissue damage and repair (2007, background): “Adenosine acts on four G-protein coupled receptors that are well conserved among vertebrates.(14) Their characteristics are”
- Physiology of Astroglia. (2018, neutral): “Adenosine receptors, represented by four subtypes (A1, A2A, A2B, and A3) with distinct pharmacological and functional properties (525), are classical G protein-coupled seven-transmembrane-spanning metabotropic receptors.”
- International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update (2011, background): “…of adenosine receptors for more than 20 years, and two reports from the committee have previously been published in this journal—the first one dealing with receptors for both adenosine and nucleotides (Fredholm et al., 1994), the second with adenosine receptors only (Fredholm et al., 2001a).”