XE 991 dihydrochloride
Chemical Name: 10,10-bis(4-Pyridinylmethyl)-9(10H)-anthracenone dihydrochloride
Biological ActivityXE 991 dihydrochloride is a 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.
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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.
Molecular basis for differential sensitivity of KCNQ and IKs channels to the cognitive enhancer XE991.
Wang et al.
KCNQ/M currents in sensory neurons: significance for pain therapy.
Passmore et al.
Citations for XE 991 dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for XE 991 dihydrochloride include:
34 Citations: Showing 1 - 10
How Gastrin-Releasing Peptide Opens the Spinal Gate for Itch.
Authors: Pagani Et al.
PTBP1-Mediated Alternative Splicing Regulates the Inflammatory Secretome and the Pro-tumorigenic Effects of Senescent Cells.
Authors: Georgilis Et al.
Cancer Cell 2018;34:85
XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits.
Authors: Greene Et al.
M-current inhibition rapidly induces a unique CK2-dependent plasticity of the axon initial segment.
Proc Natl Acad Sci U S A 2017;114(47):E10234
Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels.
Authors: Salzer Et al.
Neuropharmacology 2016;110 (A):277
Kv1 channels and neural processing in vestibular calyx afferents.
Authors: Meredith Et al.
Mol Pharmacol 2015;9:85
Cholinergic and ghrelinergic receptors and KCNQ channels in the medial PFC regulate the expression of palatability.
Authors: Parent Et al.
Front Syst Neurosci 2015;9:284
The M-current contributes to high threshold membrane potential oscillations in a cell type-specific way in the pedunculopontine nucleus of mice.
Authors: Bordas Et al.
Mol Brain 2015;9:121
N-MthD.-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity.
Authors: Lee Et al.
J Neurosci 2015;8:4
Loss of Local Astrocyte Support Disrupts Action Potential Propagation and Glutamate Release Synchrony from Unmyelinated Hippocampal Axon Terminals In Vitro.
Authors: Sobieski Et al.
Front Behav Neurosci 2015;35:11105
KV7 Channels Regulate Firing during Synaptic Integration in GABAergic Striatal Neurons.
Authors: Pérez-Ramírez Et al.
PLoS One 2015;2015:472676
Effects of KCNQ2 gene truncation on M-type Kv7 potassium currents.
Authors: Robbins Et al.
PLoS One 2013;8:e71809
Triple cysteine module within M-type K+ channels mediates reciprocal channel modulation by nitric oxide and reactive oxygen species.
Authors: Ooi Et al.
Neural Plast 2013;33:6041
Raised activity of L-type calcium channels renders neurons prone to form paroxysmal depolarization shifts.
Authors: Rubi Et al.
Neuromolecular Med 2013;15:476
Contribution of near-threshold currents to intrinsic oscillatory activity in rat medial entorhinal cortex layer II stellate cells.
Authors: Boehlen Et al.
J Neurophysiol 2013;109:445
Differential effects of cystathionine-γ-lyase-dependent vasodilatory H2S in periadventitial vasoregulation of rat and mouse aortas.
Authors: Köhn Et al.
J Physiol 2012;7:e41951
Functional significance of M-type potassium channels in nociceptive cutaneous sensory endings.
Authors: Passmore Et al.
Front Mol Neurosci 2012;5:63
Increased Kv1 channel expression may contribute to decreased sIPSC frequency following chronic inhibition of NR2B-containing NMDAR.
Authors: He Et al.
Restoration of ion channel function in deafness-causing KCNQ4 mutants by synthetic channel openers.
Authors: Leitner Et al.
Br J Pharmacol 2012;165:2244
Visceral hyperalgesia induced by forebrain-specific suppression of native Kv7/KCNQ/M-current in mice.
Authors: Bi Et al.
Mol Pain 2011;7:84
KV7 channels regulate muscle tone and nonadrenergic noncholinergic relaxation of the rat gastric fundus.
Authors: Ipavec Et al.
Pharmacol Res 2011;64:397
AKAP79/150 signal complexes in G-protein modulation of neuronal ion channels.
Authors: Zhang Et al.
J Neurosci 2011;31:7199
Dynamic interplay of excitatory and inhibitory coupling modes of neuronal L-type calcium channels.
Authors: Geier Et al.
Am J Physiol Cell Physiol 2011;300:C937
The contribution of Kv7 channels to pregnant mouse and human myometrial contractility.
Authors: McCallum Et al.
J Neurosci 2011;15:577
NE causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+.
Authors: Zemkova Et al.
MinK-dependent internalization of the IKs potassium channel.
Authors: Xu Et al.
Cardiovasc Res 2009;82:430
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 Neurosci 2009;329:368
Endolymphatic sodium homeostasis by extramacular epithelium of the saccule.
Authors: Kim and Marcus
J Neurosci 2009;29:15851
Regulation of ENaC-mediated sodium transport by glucocorticoids in Reissner's membrane epithelium.
Authors: Kim Et al.
Am J Physiol Cell Physiol 2009;296:C544
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.
The KCNQ/M-current modulates arterial baroreceptor function at the sensory terminal in rats.
Authors: Wladyka Et al.
J Pharmacol Exp Ther 2008;586:795
Inhibition of M current in sensory neurons by exogenous proteases: a signaling pathway mediating inflammatory nociception.
Authors: Linley Et al.
Br J Pharmacol 2008;28:11240
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.
Authors: Strøbaek Et al.
J Cell Mol Med 2006;70:1771
Electrophysiological and functional effects of the KCNQ channel blocker XE991 on murine portal vein smooth muscle cells.
Authors: Yeung and Greenwood
J Pharmacol Exp Ther 2005;146:585
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