K+ channels as potential targets for the treatment of gastrointestinal motor disorders

Risultato della ricerca: Contributo in rivistaArticolo in rivistapeer review

13 Citazioni (Scopus)

Abstract

K+ channels play important functional roles in excitable cells, as neurons and muscle cells. The activation or inhibition of K+ channels hyperpolarizes or depolarizes the cell membrane, respectively. These effects determine in the smooth muscle decrease or increase in Ca2+ influx through voltage-gated Ca2þ (CaV1.2) channels and relaxation or contraction, respectively. Recent studies highlight the importance of voltage-dependent type 7 K+ (KV7 or KCNQ) channels in regulating muscle tone and contractility in stomach and colon. KV7 channels, that include 5 subtypes (KV7.1–7.5), are activated at relatively negative potential values, close to those of the resting membrane potential for the smooth muscle cells of some segments of the gastrointestinal tract. Thus, they contribute to set the resting membrane potential and their blockade induces increase in smooth muscle contractility in stomach and colon. In addition, KV7 channel activation produces profound relaxations of gastric and colonic smooth muscle. Therefore, KV7 channel activators could be used to relax the smooth muscle and relieve symptoms in diseases such as functional dyspepsia and irritable bowel syndrome with prevalent diarrhea. The discovery of activators selective for the channel subtypes present in the smooth muscle, mainly KV7.4 and 7.5, would allow avoiding adverse cardiac and nervous system effects. A further step forward would be characterizing putative differences among the KV7 channel subtypes expressed in the various smooth muscles and synthesizing molecules specific for the gastrointestinal smooth muscle.
Lingua originaleEnglish
pagine (da-a)97-101
Numero di pagine5
RivistaEuropean Journal of Pharmacology
Volume733
DOI
Stato di pubblicazionePubblicato - 2014

Keywords

  • KCNQ channels
  • KV7 channels
  • Retigabine
  • Taenia coli

Fingerprint

Entra nei temi di ricerca di 'K+ channels as potential targets for the treatment of gastrointestinal motor disorders'. Insieme formano una fingerprint unica.

Cita questo