Sigma receptors: from discovery to highlights of their implications in the cardiovascular system.
Sigma receptors are the targets of many ligands, of which some (the haloperidol for instance) are psychoactive, and of substances known to have antiarrhythmic effects (amiodarone and clofilium). They are involved in a variety of cardiovascular functions, such as the regulation of cardiac contractility and rhythm and the regulation of coronary and peripheral arterial vasomotricity. This short review will focus on some aspects regarding the ligands, the binding sites, the intracellular coupling and the cardiovascular functions of these enigmatic receptors.
Monassier
Laurent
L
Laboratoire de Neurobiologie et Pharmacologie Cardiovasculaire, Faculté de Médecine, 11 rue Humann, 67085 Strasbourg Cedex, France. Laurent.Monassier@medecine.u-strasbg.fr
Bousquet
Pascal
P
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology; D002319:Cardiovascular System / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D009200:Myocardial Contraction / Q000187:drug effects / Q000502:physiology; D017480:Receptors, sigma / Q000378:metabolism*
D000889:Anti-Arrhythmia Agents; D008024:Ligands; D017480:Receptors, sigma