Linopirdine dihydrochloride
Chemical Name: 1,3-Dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one dihydrochloride
Purity: ≥99%
Biological Activity
Linopirdine dihydrochloride is a 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
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel.
Wang et al.
Science, 1998;282:1890 -
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 -
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
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Citations for Linopirdine dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Linopirdine dihydrochloride include:
12 Citations: Showing 1 - 10
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Impact of altered cholinergic tones on the neurovascular coupling response to whisker stimulation.
Authors: Lecrux Et al.
J Neurosci 2017;37:1518
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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
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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
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Electrophysiological characterization of the M-current in rat hypoglossal motoneurons
Authors: Ghezzi Et al.
Neuroscience 2016;340:62
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Role of Kv7 channels in responses of the pulmonary circulation to hypoxia.
Authors: Sedivy Et al.
Am J Physiol Lung Cell Mol Physiol 2015;308:L48
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Fine Tuning of CaV1.3 Ca2+ channel properties in adult inner hair cells positioned in the most sensitive region of the Gerbil Cochlea.
Authors: Zampini Et al.
PLoS One 2014;9:e113750
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Serum starvation-induced voltage-gated potassium channel Kv7.5 expression and its regulation by Sp1 in canine osteosarcoma cells.
Authors: Lee Et al.
Int J Mol Sci 2014;15:977
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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
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Distinct muscarinic acetylcholine receptor subtypes mediate pre- and postsynaptic effects in rat neocortex.
Authors: Gigout Et al.
BMC Neurosci 2012;13:42
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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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p75 and TrkA signaling regulates sympathetic neuronal firing patterns via differential modulation of voltage-gated currents.
Authors: Luther and Birren
J Neurosci 2009;29:5411
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KCNQ currents and their contribution to resting membrane potential and the excitability of interstitial cells of Cajal from the guinea pig bladder.
Authors: Anderson Et al.
J.Urol 2009;182:330
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