Catalog Number: 1999
Alternate Names: DuP 996
Chemical Name: 1,3-Dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one dihydrochloride
Biological Activity
Blocker of KV7 (KCNQ) voltage-gated potassium channels; blocks KV7.1 + 7.3 (KCNQ2 + 3) / M-currents (IC50 = 4 - 7 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 8.9 μM). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo.
Technical Data
  • M.Wt:
    464.39
  • Formula:
    C26H21N3O.2HCl
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    113168-57-3
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine.
    Zaczek et al.
    J.Pharmacol.Exp.Ther., 1998;285:724
  2. Selectivity of linopirdine (DuP 966), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons.
    Schnee and Brown
    J.Pharmacol.Exp.Ther., 1998;286:709
  3. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel.
    Wang et al.
    Science, 1998;282:1890
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Linopirdine dihydrochloride include:

5 Citations: Showing 1 - 5
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  1. XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits.
    Authors: Greene Et al.
    J.Pharmacol.Exp.Ther. 2017;362:177
  2. Absence of Neuroplastin-65 Affects Synaptogenesis in Mouse Inner Hair Cells and Causes Profound Hearing Loss.
    Authors: Carrott Et al.
    J Pharmacol Exp Ther 2016;36:222
  3. Electrophysiological characterization of the M-current in rat hypoglossal motoneurons
    Authors: Ghezzi? Et al.
    Neuroscience 2016;340:62
  4. Burst activity and ultrafast activation kinetics of CaV1.3 Ca2+ channels support presynaptic activity in adult gerbil hair cell ribbon synapses.
    Authors: Zampini Et al.
    Front Cell Neurosci 2013;591:3811
  5. KCNQ modulators reveal a key role for KCNQ potassium channels in regulating the tone of rat pulmonary artery smooth muscle.
    Authors: Joshi Et al.
    J Physiol 2009;329:368

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