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XE 991 dihydrochloride
Potent and selective blocker of KV7 (KCNQ) voltage-gated potassium channels. Blocks KV7.2+7.3 (KCNQ2+3) / M-currents (IC50 = 0.6 - 0.98 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 0.75 μM) but is less potent against KV7.1/minK channels (IC50 = 11.1 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 449.37. Batch specific molecular weights may vary from batch to batch due to the degree 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||2.23 mL||11.13 mL||22.25 mL|
|5 mM||0.45 mL||2.23 mL||4.45 mL|
|10 mM||0.22 mL||1.11 mL||2.23 mL|
|50 mM||0.04 mL||0.22 mL||0.45 mL|
References are publications that support the biological activity of the product.
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
Wang et al (2000) Molecular basis for differential sensitivity of KCNQ and IKs channels to the cognitive enhancer XE991. Mol.Pharmacol. 57 1218 PMID: 10825393
Passmore et al (2003) KCNQ/M currents in sensory neurons: significance for pain therapy. J.Neurosci. 23 7227 PMID: 12904483
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Keywords: XE 991 dihydrochloride, XE 991 dihydrochloride supplier, KCNQ, channel, blockers, Potassium, KV, Channels, voltage-gated, voltage-dependent, K+, KCNQ2, KCNQ3, KCNQ1, XE991, dihydrochloride, KV7.1, Voltage-Gated, 2000, Tocris Bioscience
34 Citations for XE 991 dihydrochloride
Citations are publications that use Tocris products. Selected citations for XE 991 dihydrochloride include:
Georgilis et al (2018) PTBP1-Mediated Alternative Splicing Regulates the Inflammatory Secretome and the Pro-tumorigenic Effects of Senescent Cells. Cancer Cell 34 85 PMID: 29990503
Ooi et al (2013) Triple cysteine module within M-type K+ channels mediates reciprocal channel modulation by nitric oxide and reactive oxygen species. Neural Plast 33 6041 PMID: 23554485
Bi et al (2011) Visceral hyperalgesia induced by forebrain-specific suppression of native Kv7/KCNQ/M-current in mice. Mol Pain 7 84 PMID: 22029713
Zemkova et al (2011) NE causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+. Endocrinology 152 3842 PMID: 21828176
Zhang et al (2011) AKAP79/150 signal complexes in G-protein modulation of neuronal ion channels. J Neurosci 31 7199 PMID: 21562284
Geier et al (2011) Dynamic interplay of excitatory and inhibitory coupling modes of neuronal L-type calcium channels. Am J Physiol Cell Physiol 300 C937 PMID: 21228322
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 Neurosci 329 368 PMID: 19151245
Pagani et al (2019) How Gastrin-Releasing Peptide Opens the Spinal Gate for Itch. Neuron PMID: 31103358
Boehlen et al (2013) Contribution of near-threshold currents to intrinsic oscillatory activity in rat medial entorhinal cortex layer II stellate cells. J Neurophysiol 109 445 PMID: 23076110
Rubi et al (2013) Raised activity of L-type calcium channels renders neurons prone to form paroxysmal depolarization shifts. Neuromolecular Med 15 476 PMID: 23695859
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
Lezmy (2017) M-current inhibition rapidly induces a unique CK2-dependent plasticity of the axon initial segment. Proc Natl Acad Sci U S A 114 E10234 PMID: 29109270
Robbins et al (2013) Effects of KCNQ2 gene truncation on M-type Kv7 potassium currents. PLoS One 8 e71809 PMID: 23977150
Leitner et al (2012) Restoration of ion channel function in deafness-causing KCNQ4 mutants by synthetic channel openers. Br J Pharmacol 165 2244 PMID: 21951272
Passmore et al (2012) Functional significance of M-type potassium channels in nociceptive cutaneous sensory endings. Front Mol Neurosci 5 63 PMID: 22593734
He et al (2012) Increased Kv1 channel expression may contribute to decreased sIPSC frequency following chronic inhibition of NR2B-containing NMDAR. Neuropsychopharmacology 37 1338 PMID: 22218089
Strøbaek et al (2006) Inhibitory gating modulation of small conductance Ca2+-activated K+ channels by the synthetic compound (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphtylamine (NS8593) reduces afterhyperpolarizing current in hippocampal CA1 neurons. J Cell Mol Med 70 1771 PMID: 16926279
Ipavec et al (2011) KV7 channels regulate muscle tone and nonadrenergic noncholinergic relaxation of the rat gastric fundus. Pharmacol Res 64 397 PMID: 21740972
Kim and Marcus (2009) Endolymphatic sodium homeostasis by extramacular epithelium of the saccule. J Neurosci 29 15851 PMID: 20016101
Anderson et al (2009) KCNQ currents and their contribution to resting membrane potential and the excitability of interstitial cells of Cajal from the guinea pig bladder. J.Urol. 182 330 PMID: 19450820
Kim et al (2009) Regulation of ENaC-mediated sodium transport by glucocorticoids in Reissner's membrane epithelium. Am J Physiol Cell Physiol 296 C544 PMID: 19144862
Xu et al (2009) MinK-dependent internalization of the IKs potassium channel. Cardiovasc Res 82 430 PMID: 19202166
Yeung and Greenwood (2005) Electrophysiological and functional effects of the KCNQ channel blocker XE991 on murine portal vein smooth muscle cells. J Pharmacol Exp Ther 146 585 PMID: 16056238
McCallum et al (2011) The contribution of Kv7 channels to pregnant mouse and human myometrial contractility. J Neurosci 15 577 PMID: 20132415
Linley et al (2008) Inhibition of M current in sensory neurons by exogenous proteases: a signaling pathway mediating inflammatory nociception. Br J Pharmacol 28 11240 PMID: 18971466
Wladyka et al (2008) The KCNQ/M-current modulates arterial baroreceptor function at the sensory terminal in rats. J Pharmacol Exp Ther 586 795 PMID: 18048450
Salzer et al (2016) Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels. Neuropharmacology 110 (A) 277 PMID: 27511837
Pérez-Ramírez et al (2015) KV7 Channels Regulate Firing during Synaptic Integration in GABAergic Striatal Neurons. PLoS One 2015 472676 PMID: 26113994
Bordas et al (2015) The M-current contributes to high threshold membrane potential oscillations in a cell type-specific way in the pedunculopontine nucleus of mice. Mol Brain 9 121 PMID: 25904846
Lee et al (2015) N-MthD.-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity. J Neurosci 8 4 PMID: 25599691
Sobieski et al (2015) Loss of Local Astrocyte Support Disrupts Action Potential Propagation and Glutamate Release Synchrony from Unmyelinated Hippocampal Axon Terminals In Vitro. Front Behav Neurosci 35 11105 PMID: 26245971
Parent et al (2015) Cholinergic and ghrelinergic receptors and KCNQ channels in the medial PFC regulate the expression of palatability. Front Syst Neurosci 9 284 PMID: 26578914
Meredith et al (2015) Kv1 channels and neural processing in vestibular calyx afferents. Mol Pharmacol 9 85 PMID: 26082693
Köhn et al (2012) Differential effects of cystathionine-γ-lyase-dependent vasodilatory H2S in periadventitial vasoregulation of rat and mouse aortas. J Physiol 7 e41951 PMID: 22870268
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Literature in this Area
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Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
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.