Linopirdine

A Blocker of KCNQ (KV7) Channels
    Cat #: L-155
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 391.46
    Purity: >98%
    Formulation Lyophilized powder.
    Effective concentration 0.1-300 µM.
    Structure
    Chemical name 1-phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one.
    Molecular formula C26H21N3O.
    CAS No.: 105431-72-9.
    Activity Linopirdine blocks KCNQ channels with an IC50 of 2.4 μM for KV7.2/3 heteromers1.
    References - Activity
    1. Aiken, S.P. et al. (2012) Br. J. Pharmacol. 115, 1163.

    Storage before reconstitution Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Reconstitution 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage after reconstitution Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    Alomone Labs Linopirdine inhibits KCNQ2/KCNQ3 channels expressed in Xenopus oocytes.
    A. Time course of KCNQ2/KCNQ3 maximal current amplitude, elicited by 700 ms voltage step from holding potential of -100 mV to -20 mV, delivered every 10 seconds. Application of 300 µM Linopirdine (#L-155) inhibits the KCNQ2/KCNQ3 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 300 µM Linopirdine as indicated.
    References - Scientific Background
    1. Wickenden, A.D. et al. (2008) Mol. Pharmacol. 73, 977.
    2. Schnee, M.E. and Brown, B.S. (1998) J. Pharmacol. Exp. Ther. 286, 709.
    3. Aiken, S.P. et al. (1995) Br. J. Pharmacol. 115, 1163.
    Scientific background KCNQ2 (KV7.2) and KCNQ3 (KV7.3) are voltage-gated K+ channel subunits that underlie the neuronal M current1. Linopirdine, a putative cognition enhancing drug, increases acetylcholine (ACh) release in rat brain tissue and improves performance in animal models of learning and memory. In addition to ACh, Linopirdine has been shown to enhance the in vitro release of dopamine and 5-hydroxytryptamine (5-HT), and, to a lesser extent, γ-aminobutyric acid and glutamate2. The enhanced release of one or more neurotransmitters may account for the activity linopirdine displays in behavioral models of learning and memory3. The mechanism whereby linopirdine enhances acetylcholine release has been proposed to involve inhibition of the M-type K+ current (IM). Linopirdine is selective for IM with an IC50 value of 2.4 μM2.
    Target KCNQ K+ channels
    Last update: 07/01/2019

    Linopirdine (#L-155) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Citations
    Product citations
    1. Paz, R.M. et al. (2018) Neuropharmacology 137, 309.
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