title: Targeting adenosine receptors in the development of cardiovascular therapeutics.
abstract: Adenosine receptor stimulation has negative inotropic and dromotropic actions, reduces cardiac ischemia-reperfusion injury and remodeling, and prevents cardiac arrhythmias. In the vasculature, adenosine modulates vascular tone, reduces infiltration of inflammatory cells and generation of foam cells, and may prevent the development of atherosclerosis as a result. Modulation of insulin sensitivity may further add to the anti-atherosclerotic properties of adenosine signaling. In the kidney, adenosine plays an important role in tubuloglomerular feedback and modulates tubular sodium reabsorption. The challenge is to take advantage of the beneficial actions of adenosine signaling while preventing its potential adverse effects, such as salt retention and sympathoexcitation. Drugs that interfere with adenosine formation and elimination or drugs that allosterically enhance specific adenosine receptors seem to be most promising to meet this challenge.
authors.affiliation: Department of Pharmacology-Toxicology 149 and Internal Medicine 463, Radboud University Nijmegen Medical Centre, PO Box 9101, 6500 HB Nijmegen, The Netherlands.
authors.forename: Niels P
authors.initials: NP
authors.lastname: Riksen
authors.forename: Gerard A
authors.initials: GA
authors.lastname: Rongen
mesh_terms: D000241:Adenosine / Q000009:adverse effects / Q000494:pharmacology*; D000818:Animals; D001145:Arrhythmias, Cardiac / Q000517:prevention & control; D050197:Atherosclerosis / Q000517:prevention & control; D002317:Cardiovascular Agents / Q000009:adverse effects / Q000494:pharmacology*; D002318:Cardiovascular Diseases / Q000188:drug therapy*; D006801:Humans; D007328:Insulin / Q000378:metabolism; D007668:Kidney / Q000378:metabolism; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D015427:Reperfusion Injury / Q000517:prevention & control; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D002317:Cardiovascular Agents; D007328:Insulin; D018047:Receptors, Purinergic P1; D000241:Adenosine