KCNQ-Channels

KCNQ-channels, HERG-channels, and Shaker-related Kv-channels. [Pg.1311]

Kainate Receptor Kallidin, Lysyl-Bradykinin Kallikrein KCNQ-Channels KCOs... [Pg.1495]

Flupirtine was the first compound identified to affect KCNQ channels and has been used in man to treat pain. However, only recently has this drug been shown to be an activator of Kv7 channels (see Munro and Dalby-Brown 2007). The clinical efficacy of flupirtine was originally postulated to occur through receptor-dependent mechanisms, but as noted by Munro and Dalby-Brown (2007) it is likely that Kv7 channel activation occurs at clinically relevant exposure levels. Retigabine, a flupirtine analog, is currently in clinical trials for the treatment of epilepsy and pain and has been the most widely used tool to explore both the in vitro and in vivo effects of Kv7 activation. This compound was initially shown to increase K+ channel activity in a neuroblastoma cell line (Rundfeldt 1997 see also Rundfeldt 1999) and subsequently was... [Pg.33]

Gerlach AC (2006) KCNQ channels as targets for anti-nociceptive therapies. Soc Neurosci, online P401.3... [Pg.50]

Munro G, Dalby-Brown W (2007) Kv7 (KCNQ) channel modulators and neuropathic pain. J Med Chem 50(ll) 2576-2582... [Pg.52]

I. Thallium Flux Assay for KCNQ Channel Openers... [Pg.440]

Zhang H, Craciun LC, Mirshahi T, Rohacs T, Lopes CMB, et al. (2003) P1P2 Activates KCNQ Channels, and Its Hydrolysis Underlies Receptor-Mediated Inhibition of M Currents. Neuron 37 963-975. [Pg.32]

This synopsis refers only to actions demonstrated within or close to therapeutic concentrations of drugs. Abbreviations (+) to (+++) weak to strong efficacy, (-) no efficacy, ( ) not investigated. HVA high threshold Ca2 channels, T T-type Ca2+ channels, L L-type Ca2+ channels, iNap persistent sodium current, DR delayed rectifier K channels, KCNQ KCNQ subtypes of K+ channels. [Pg.129]

Jentsch TJ (2000) Neuronal KCNQ potassium channels physiology and role in disease. Nat Rev Neurosci 1 21-30... [Pg.997]

Robbins, J., KCNQ potassium channels physiology, pathophysiology, and pharmacology, Pharmacology and Therapeutics 2001, 90, 1-19. [Pg.349]

Dost R, Rostock A, Rundfeldt (2004) The anti-hyperalgesic activity of retigabine is mediated by KCNQ potassium channel activation. Nauyn-Schmiedeberg s Arch Pharmacol 369 382-390... [Pg.50]

Schenzer A, Friedrich T, Pusch M et al. (2005) Molecular determinants of KCNQ (Kv7) K+ channel sensitivity to the anticonvulsant retigabine. J Neurosci 25(20) 5051-5060... [Pg.53]

Suh B-C, Inoue T, Meyer T et al. (2006) Rapid chemically induced changes of PtdIns(4,5)P2 gate KCNQ ion channels. Science 314 1454-1457... [Pg.53]

Wickenden AD, Roeloffs R, McNaughton-Smith G et al. (2004) KCNQ potassium channels drug targets for the treatment of epilepsy and pain. Expert Opin Ther Patents 14(4) 1-13... [Pg.54]

Wu Y-J, Dworetsky SI (2005) Recent developments on KCNQ potassium channel openers. Curr Med Chem 12 453-460... [Pg.54]

Fluoro-2-oxindole derivatives, (IV), prepared by Dworetzky (5) were effective modulators of KCNQ potassium channels and used in treating migraine and mechanistically related disease. [Pg.441]

Wang HS, Brown BS, McKinnon D, Co-henlS. 2000. Molecular basis for differential sensitivity of KCNQ and IKs channels to the cognitive enhancer XE991. Mol. Pharmacol. 57 1218-23... [Pg.460]

Schroeder BC, Waldegger S, Fehr S, Bleich M, Warth R, et al. 2000. A constitu-tively open potassium channel formed by KCNQ 1 and KCNE3. Nature 403 196-99... [Pg.460]

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