Novel treatment strategies for smooth muscle disorders: Targeting Kv7 potassium channels

JM Haick, KL Byron - Pharmacology & therapeutics, 2016 - Elsevier
Smooth muscle cells provide crucial contractile functions in visceral, vascular, and lung
tissues. The contractile state of smooth muscle is largely determined by their electrical …

Cyclic AMP-dependent regulation of Kv7 voltage-gated potassium channels

J Van der Horst, IA Greenwood, TA Jepps - Frontiers in physiology, 2020 - frontiersin.org
Voltage-gated Kv7 potassium channels, encoded by KCNQ genes, have major physiological
impacts cardiac myocytes, neurons, epithelial cells, and smooth muscle cells. Cyclic …

Urinary bladder smooth muscle ion channels: expression, function, and regulation in health and disease

J Malysz, GV Petkov - American Journal of Physiology …, 2020 - journals.physiology.org
Urinary bladder smooth muscle (UBSM), also known as detrusor smooth muscle, forms the
bladder wall and ultimately determines the two main attributes of the organ: urine storage …

Pharmacological targeting of neuronal Kv7. 2/3 channels: a focus on chemotypes and receptor sites

F Miceli, MV Soldovieri, P Ambrosino… - Current medicinal …, 2018 - ingentaconnect.com
Background: The Kv7 (KCNQ) subfamily of voltage-gated potassium channels consists of 5
members (Kv7. 1-5) each showing characteristic tissue distribution and physiological roles …

The urinary safety profile and secondary renal effects of retigabine (ezogabine): A first‐in‐class antiepileptic drug that targets KCNQ (Kv7) potassium channels

N Brickel, P Gandhi, K VanLandingham… - …, 2012 - Wiley Online Library
Retigabine (RTG; international nonproprietary name)/ezogabine (EZG; North American
adopted name), a first‐in‐class antiepileptic drug (AED) that reduces neuronal excitability …

One man's side effect is another man's therapeutic opportunity: targeting Kv7 channels in smooth muscle disorders

TA Jepps, SP Olesen… - British journal of …, 2013 - Wiley Online Library
Retigabine is a first in class anticonvulsant that has recently undergone clinical trials to test
its efficacy in epileptic patients. Retigabine's novel mechanism of action–activating Kv7 …

Functional expression of KCNQ (Kv7) channels in guinea pig bladder smooth muscle and their contribution to spontaneous activity

UA Anderson, C Carson, L Johnston… - British journal of …, 2013 - Wiley Online Library
Background and Purpose The aim of the study was to determine whether KCNQ channels
are functionally expressed in bladder smooth muscle cells (SMC) and to investigate their …

Vasorelaxant effects of novel Kv7.4 channel enhancers ML213 and NS15370

TA Jepps, BH Bentzen, JB Stott… - British journal of …, 2014 - Wiley Online Library
Background and Purpose The KCNQ‐encoded voltage‐gated potassium channel family (Kv
7.1‐Kv 7.5) are established regulators of smooth muscle contractility, where Kv 7.4 and Kv …

Electrophysiological and pharmacological characterization of a novel and potent neuronal Kv7 channel opener SCR2682 for antiepilepsy

F Zhang, Y Liu, F Tang, B Liang, H Chen… - The FASEB …, 2019 - Wiley Online Library
ABSTRACT Voltage‐gated Kv7/KCNQ/M potassium channels play an essential role in the
control of membrane potential and neuronal excitability. Activation of the neuronal …

How to Replace the Lost keys? Strategies Toward Safer KV7 Channel Openers

C Bock, A Link - Future Medicinal Chemistry, 2019 - Taylor & Francis
The highly structurally similar drugs flupirtine and retigabine have been regarded as safe
and effective for many years but lately they turned out to exert intolerable side effects. While …