title: Celecoxib and ion channels: a story of unexpected discoveries.
abstract: Celecoxib (Celebrex), a highly popular selective inhibitor of cyclooxygenase-2, can modulate ion channels and alter functioning of neurons and myocytes at clinically relevant concentrations independently of cyclooxygenase inhibition. In experimental systems varying from Drosophila to primary mammalian and human cell lines, celecoxib inhibits many voltage-activated Na(+), Ca(2+), and K(+) channels, including NaV1.5, L- and T-type Ca(2+) channels, KV1.5, KV2.1, KV4.3, KV7.1, KV11.1 (hERG), while stimulating other K(+) channels-KV7.2-5 and, possibly, KV11.1 (hERG) channels under certain conditions. In this review, we summarize the information currently available on the effects of celecoxib on ion channels, examine mechanistic aspects of drug action and the concomitant changes at the cellular and organ levels, and discuss these findings in the therapeutic context.
authors.affiliation: Department of Physical Sciences, Division of Biophysics, University of Oulu, PO Box 3000, 90014 Oulun Yliopisto, Finland. Electronic address: roman.frolov@oulu.fi.
authors.forename: Roman V
authors.initials: RV
authors.lastname: Frolov
authors.affiliation: Department of Pharmacology and Toxicology, State University of New York at Buffalo, Buffalo, NY 14214, USA.
authors.forename: Satpal
authors.initials: S
authors.lastname: Singh
mesh_terms: D000818:Animals; D000068579:Celecoxib; D052246:Cyclooxygenase 2 Inhibitors / Q000494:pharmacology*; D006801:Humans; D007473:Ion Channels / Q000037:antagonists & inhibitors / Q000378:metabolism*; D011720:Pyrazoles / Q000494:pharmacology*; D013449:Sulfonamides / Q000494:pharmacology*
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D007473:Ion Channels; D011720:Pyrazoles; D013449:Sulfonamides; D000068579:Celecoxib
keywords: COX-2 inhibitor; Calcium channel; Celecoxib; Potassium channel; Sodium channel