title: International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.
abstract: In the 10 years since our previous International Union of Basic and Clinical Pharmacology report on the nomenclature and classification of adenosine receptors, no developments have led to major changes in the recommendations. However, there have been so many other developments that an update is needed. The fact that the structure of one of the adenosine receptors has recently been solved has already led to new ways of in silico screening of ligands. The evidence that adenosine receptors can form homo- and heteromultimers has accumulated, but the functional significance of such complexes remains unclear. The availability of mice with genetic modification of all the adenosine receptors has led to a clarification of the functional roles of adenosine, and to excellent means to study the specificity of drugs. There are also interesting associations between disease and structural variants in one or more of the adenosine receptors. Several new selective agonists and antagonists have become available. They provide improved possibilities for receptor classification. There are also developments hinting at the usefulness of allosteric modulators. Many drugs targeting adenosine receptors are in clinical trials, but the established therapeutic use is still very limited.
authors.affiliation: Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden. bertil.fredholm@ki.se
authors.forename: Bertil B
authors.initials: BB
authors.lastname: Fredholm
authors.forename: Adriaan P
authors.initials: AP
authors.lastname: IJzerman
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Jacobson
authors.forename: Joel
authors.initials: J
authors.lastname: Linden
authors.forename: Christa E
authors.initials: CE
authors.lastname: Müller
mesh_terms: D000818:Animals; D030801:Animals, Genetically Modified; D006801:Humans; D007390:International Agencies; D058990:Molecular Targeted Therapy; D058906:Purinergic P1 Receptor Agonists / Q000494:pharmacology / Q000627:therapeutic use; D058915:Purinergic P1 Receptor Antagonists / Q000494:pharmacology / Q000627:therapeutic use; D018047:Receptors, Purinergic P1 / Q000737:chemistry / Q000145:classification* / Q000235:genetics / Q000502:physiology*; D009626:Terminology as Topic
chemical_list: D058906:Purinergic P1 Receptor Agonists; D058915:Purinergic P1 Receptor Antagonists; D018047:Receptors, Purinergic P1