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.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 464.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.15 mL||10.77 mL||21.53 mL|
|5 mM||0.43 mL||2.15 mL||4.31 mL|
|10 mM||0.22 mL||1.08 mL||2.15 mL|
|50 mM||0.04 mL||0.22 mL||0.43 mL|
References are publications that support the products' biological activity.
Schnee and Brown (1998) Selectivity of linopirdine (DuP 966), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J.Pharmacol.Exp.Ther. 286 709 PMID: 9694925
Wang et al (1998) KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 282 1890 PMID: 9836639
Zaczek et al (1998) 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. J.Pharmacol.Exp.Ther. 285 724 PMID: 9580619
If you know of a relevant reference for Linopirdine dihydrochloride, please let us know.
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Keywords: Linopirdine dihydrochloride, supplier, KCNQ, channel, blockers, Potassium, KV, kv7, Channels, voltage-gated, voltage-dependent, K+, KCNQ2, KCNQ3, KCNQ1, DuP996, DuP, 996, Voltage-Gated, Potassium, Channels, Voltage-Gated, Potassium, Channels, Tocris Bioscience
5 Citations for Linopirdine dihydrochloride
Citations are publications that use Tocris products. Selected citations for Linopirdine dihydrochloride include:
Ghezzi et al (2016) Electrophysiological characterization of the M-current in rat hypoglossal motoneurons Neuroscience 340 62 PMID: 27984184
Greene et al (2017) XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits. J.Pharmacol.Exp.Ther. 362 177 PMID: 28483800
Carrott et al (2016) Absence of Neuroplastin-65 Affects Synaptogenesis in Mouse Inner Hair Cells and Causes Profound Hearing Loss. J Pharmacol Exp Ther 36 222 PMID: 26740663
Joshi et al (2009) KCNQ modulators reveal a key role for KCNQ potassium channels in regulating the tone of rat pulmonary artery smooth muscle. J Physiol 329 368 PMID: 19151245
Zampini et al (2013) Burst activity and ultrafast activation kinetics of CaV1.3 Ca2+ channels support presynaptic activity in adult gerbil hair cell ribbon synapses. Front Cell Neurosci 591 3811 PMID: 23713031
Do you know of a great paper that uses Linopirdine dihydrochloride from Tocris? If so please let us know.
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Literature in this Area
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.