title: Current status of A1 adenosine receptor allosteric enhancers.
abstract: Adenosine is an ubiquitous nucleoside involved in various physiological and pathological functions by stimulating A1, A2A, A2B and A3 adenosine receptors (ARs). Allosteric enhancers to A1ARs may represent novel therapeutic agents because they increase the activity of these receptors by mediating a shift to their active form in the A1AR-G protein ternary complex. In this manner, they are able to amplify the action of endogenous adenosine, which is produced in high concentrations under conditions of metabolic stress. A1AR allosteric enhancers could be used as a justifiable alternative to the exogenous agonists that are characterized by receptor desensitization and downregulation. In this review, an analysis of some of the most interesting allosteric modulators of A1ARs has been reported.
authors.affiliation: Dipartimento di Scienze Chimiche e Farmaceutiche, Via Fossato di Mortara 17-19, 44121, Università di Ferrara, Ferrara, Italy.
authors.forename: Romeo
authors.initials: R
authors.lastname: Romagnoli
authors.affiliation: Dipartimento di Scienze Chimiche e Farmaceutiche, Via Fossato di Mortara 17-19, 44121, Università di Ferrara, Ferrara, Italy.
authors.forename: Pier Giovanni
authors.initials: PG
authors.lastname: Baraldi
authors.affiliation: Alta Vetta Pharmaceutical Consulting, L.L.C., Durham, NC, USA.
authors.forename: Allan R
authors.initials: AR
authors.lastname: Moorman
authors.affiliation: Dipartimento di Scienze Mediche, Sezione di Farmacologia, Università di Ferrara, Ferrara, Italy.
authors.forename: Pier Andrea
authors.initials: PA
authors.lastname: Borea
authors.affiliation: Dipartimento di Scienze Mediche, Sezione di Farmacologia, Università di Ferrara, Ferrara, Italy.
authors.forename: Katia
authors.initials: K
authors.lastname: Varani
mesh_terms: D058907:Adenosine A1 Receptor Agonists / Q000737:chemistry / Q000494:pharmacology*; D000494:Allosteric Regulation / Q000187:drug effects*; D000818:Animals; D006801:Humans; D008024:Ligands; D043682:Receptor, Adenosine A1 / Q000737:chemistry / Q000378:metabolism*; D013876:Thiophenes / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D058907:Adenosine A1 Receptor Agonists; D008024:Ligands; D043682:Receptor, Adenosine A1; D013876:Thiophenes