title: BK channel activators and their therapeutic perspectives.
abstract: The large conductance calcium- and voltage-activated K(+) channel (KCa1.1, BK, MaxiK) is ubiquitously expressed in the body, and holds the ability to integrate changes in intracellular calcium and membrane potential. This makes the BK channel an important negative feedback system linking increases in intracellular calcium to outward hyperpolarizing potassium currents. Consequently, the channel has many important physiological roles including regulation of smooth muscle tone, neurotransmitter release and neuronal excitability. Additionally, cardioprotective roles have been revealed in recent years. After a short introduction to the structure, function and regulation of BK channels, we review the small organic molecules activating BK channels and how these tool compounds have helped delineate the roles of BK channels in health and disease.
authors.affiliation: Department of Biomedical Sciences, Faculty of Health Sciences, Danish Arrhythmia Research Centre, University of Copenhagen Copenhagen, Denmark ; Acesion Pharma Copenhagen, Denmark.
authors.forename: Bo H
authors.initials: BH
authors.lastname: Bentzen
authors.affiliation: Department of Biomedical Sciences, Faculty of Health Sciences, Danish Arrhythmia Research Centre, University of Copenhagen Copenhagen, Denmark.
authors.forename: Søren-Peter
authors.initials: SP
authors.lastname: Olesen
authors.affiliation: H. Lundbeck A/S Copenhagen, Denmark.
authors.forename: Lars C B
authors.initials: LC
authors.lastname: Rønn
authors.affiliation: Acesion Pharma Copenhagen, Denmark ; H. Lundbeck A/S Copenhagen, Denmark.
authors.forename: Morten
authors.initials: M
authors.lastname: Grunnet
keywords: BK; KCNMA1; KCa1.1; MaxiK; activators; high-conductance calcium-activated potassium channels; openers; pharmacology