Potassium channel activation: A potential therapeutic approach?

In vivo analgesic, anti-inflammatory potential in Swiss albino mice and in vitro thrombolytic activity of hydroalcoholic fruits extract from Daemonorops robusta Warb

“…Our present study also demonstrated that glibenclamide, an ATP-sensitive K+ channel antagonist, partly reversed the antinociceptive activity shown by MEDR. The results of this study, therefore, might indicate the involvement of ATP sensitive K+ channel opening and subsequent efflux of K+ ion and membrane repolarization and/or hyperpolarization by MEDR which reduces the membrane excitability (Lawson, 1996).…”

Synthesis and characterization of a novel tritiated KATP channel opener with a benzopyran structure

“…They are compounds of great therapeutic interest (Evans & Stemp, 1996;Lawson, 1996) having potential for diseases as diverse as asthma (Fozard & Manley, 2000), urogenital dysfunction (Brading & Turner, 1996), cardiac ischaemia (Grover & Garlid, 2000) and hair growth (Lawson, 1996). A major problem in developing therapeutic agents has been the limited tissue selectivity of the KCOs, since the dominant systemic eect of most KCOs is to lower peripheral resistance and blood pressure (Edwards & Weston, 1994;Lawson, 1996;Quast, 1996). However, with the availability of recombinant K ATP channels, the interaction of K ATP channel openers with the dierent Kir6.x/SURx combinations can be studied in unprecedented detail.…”

“…K ATP channels are the target of the hypoglycaemic sulphonylureas (SUs) which close the channel preferentially in the pancreatic b-cell to promote insulin secretion; they are activated by the K + channel openers (KCOs), a class of drugs with multiple therapeutic applications (see below) (Edwards & Weston, 1993;Lawson, 1996;Quast, 1996). K ATP channels are composed of two types of subunits, inwardly rectifying K + channels (Kir6.x) and sulphonylurea receptors (SURs), arranged as a heterooctamer with 4 : 4 stoichiometry of the subunits (reviews: Ashcroft & Gribble, 1998;Aguilar-Bryan & Bryan, 1999;Seino, 1999).…”

ATP-sensitive potassium channels: novel potential roles in Parkinson’s disease

“…In this case, activation or inhibition of K ATP channels may influence the clinical situation of affected patients. Otherwise, the molecular diversity of the channels should allow the development of highly specific drugs, which may selectively target cell types, groups, or systems throughout the body, correcting or at least improving disturbed functions [32] . In this respect, it is important to understand the regional, cellular, and subcellular localizations of identified ATP-sensitive potassium channel subunits.…”