title: Ligand bias prevents class equality among beta-blockers.
abstract: β-Blockers are used for a wide range of diseases from hypertension to glaucoma. In some diseases/conditions all β-blockers are effective, while in others only certain subgroups are therapeutically beneficial. The best-documented example for only a subset of β-blockers showing clinical efficacy is in heart failure, where members of the class have ranged from completely ineffective, to drugs of choice for treating the disease. Similarly, β-blockers were tested in murine asthma models and two pilot clinical studies. A different subset was found to be effective for this clinical indication. These findings call into question the current system of classifying these drugs. To consider 'β-blockers', as a single class is misleading when considering their rigorous pharmacological definition and their appropriate clinical application.
authors.affiliation: Department of Pharmacological and Pharmaceutical Sciences, University of Houston, Houston, TX, USA.
authors.forename: Vaidehi J
authors.initials: VJ
authors.lastname: Thanawala
authors.affiliation: Department of Pharmacological and Pharmaceutical Sciences, University of Houston, Houston, TX, USA.
authors.forename: Gloria S
authors.initials: GS
authors.lastname: Forkuo
authors.affiliation: Department of Biochemistry, Université de Montréal, Montréal, Quebec, Canada; Institute for Research in Immunology and Cancer, Université de Montréal, Montréal, Quebec, Canada.
authors.forename: Wayne
authors.initials: W
authors.lastname: Stallaert
authors.affiliation: Consultant in Pharmacology, Cheshire, UK.
authors.forename: Paul
authors.initials: P
authors.lastname: Leff
authors.affiliation: Department of Biochemistry, Université de Montréal, Montréal, Quebec, Canada; Institute for Research in Immunology and Cancer, Université de Montréal, Montréal, Quebec, Canada.
authors.forename: Michel
authors.initials: M
authors.lastname: Bouvier
authors.affiliation: Department of Pharmacological and Pharmaceutical Sciences, University of Houston, Houston, TX, USA. Electronic address: rabond@uh.edu.
authors.forename: Richard
authors.initials: R
authors.lastname: Bond
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000145:classification / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D001249:Asthma / Q000188:drug therapy / Q000378:metabolism; D006801:Humans; D008024:Ligands; D018343:Receptors, Adrenergic, beta-2 / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: D000319:Adrenergic beta-Antagonists; D008024:Ligands; D018343:Receptors, Adrenergic, beta-2