XE 991 dihydrochloride

Cat. No. 2000

XE 991 dihydrochloride C26H20N2O.2HCl [122955-13-9]

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Chemical Name: 10,10-bis(4-Pyridinylmethyl)-9(10H)-anthracenone dihydrochloride

Biological Activity

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.

Technical Data

M.Wt:
449.37
Formula:
C26H20N2O.2HCl
Solubility:
Soluble to 100 mM in water
Purity:
>99 %
Storage:
Desiccate at RT
CAS No:
122955-13-9

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Passmore et al (2003) KCNQ/M currents in sensory neurons: significance for pain therapy. J.Neurosci. 23 7227. PMID: 12904483.

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.

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.

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Citations are publications that use Tocris products. Selected citations for XE 991 dihydrochloride include:

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.

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-methyl-D-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity. J Neurosci 8 4. PMID: 25599691.

Meredith et al (2015) Kv1 channels and neural processing in vestibular calyx afferents. Mol Pharmacol 9 85. PMID: 26082693.

Pérez-Ramírez et al (2015) KV7 Channels Regulate Firing during Synaptic Integration in GABAergic Striatal Neurons. PLoS One 2015 472676. PMID: 26113994.

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.

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.

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.

Robbins et al (2013) Effects of KCNQ2 gene truncation on M-type Kv7 potassium currents. PLoS One 8 e71809. PMID: 23977150.

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.

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.

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.

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.

McCallum et al (2011) The contribution of Kv7 channels to pregnant mouse and human myometrial contractility. J Neurosci 15 577. PMID: 20132415.

Zemkova et al (2011) Norepinephrine 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.

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.

Xu et al (2009) MinK-dependent internalization of the IKs potassium channel. Cardiovasc Res 82 430. PMID: 19202166.

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.

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.

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.

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Keywords: XE 991 dihydrochloride, supplier, KCNQ, channel, blockers, Potassium, KV, Channels, voltage-gated, voltage-dependent, K+, KCNQ2, KCNQ3, KCNQ1, XE991, dihydrochloride, KV7.1, Tocris Bioscience, Voltage-gated Potassium (KV) Channel Blocker products

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