Chemical Name: 1,3-Dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one dihydrochloride
Biological ActivityLinopirdine 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel.
Wang et al.
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.
Selectivity of linopirdine (DuP 966), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons.
Schnee and Brown
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
Impact of altered cholinergic tones on the neurovascular coupling response to whisker stimulation.
Authors: Lecrux Et al.
J Neurosci 2017;37:1518
XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits.
Authors: Greene Et al.
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
Electrophysiological characterization of the M-current in rat hypoglossal motoneurons
Authors: Ghezzi Et al.
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
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
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
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
Distinct muscarinic acetylcholine receptor subtypes mediate pre- and postsynaptic effects in rat neocortex.
Authors: Gigout Et al.
BMC Neurosci 2012;13:42
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
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
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.
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Reviews for Linopirdine dihydrochloride
Average Rating: 5 (Based on 1 Review)
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Our lab is working with Voltage gated potassium channel for a while and I have used a few potent Kv channel blockers to measure out the % blocking showed by them. This product gave reproducible data, stable in biological lab conditions and the work was published. So overall very happy with the purchase of the compound.