XE 991 dihydrochloride

  ( 30 citations )    
Product Datasheet
Catalog Number:2000
Chemical Name:10,10-bis(4-Pyridinylmethyl)-9(10H)-anthracenone dihydrochloride
Product Details
Citations (30)
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:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
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.
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The citations listed below are publications that use Tocris products. Selected citations for XE 991 dihydrochloride include:

30 Citations: Showing 1 - 10
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  1. XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits.
    Authors: Greene Et al.
    J.Pharmacol.Exp.Ther.  2017;362:177
  2. M-current inhibition rapidly induces a unique CK2-dependent plasticity of the axon initial segment.
    Authors: Lezmy
    Proc Natl Acad Sci U S A  2017;114(47):E10234
  3. Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels.
    Authors: Salzer Et al.
    Neuropharmacology  2016;110 (A):277
  4. Kv1 channels and neural processing in vestibular calyx afferents.
    Authors: Meredith Et al.
    Mol Pharmacol  2015;9:85
  5. 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
  6. 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
  7. N-methyl-D-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
  8. 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
  9. KV7 Channels Regulate Firing during Synaptic Integration in GABAergic Striatal Neurons.
    Authors: Pérez-Ramírez Et al.
    PLoS One  2015;2015:472676
  10. Effects of KCNQ2 gene truncation on M-type Kv7 potassium currents.
    Authors: Robbins Et al.
    PLoS One  2013;8:e71809
  11. 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
  12. Raised activity of L-type calcium channels renders neurons prone to form paroxysmal depolarization shifts.
    Authors: Rubi Et al.
    Neuromolecular Med  2013;15:476
  13. 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
  14. 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
  15. Functional significance of M-type potassium channels in nociceptive cutaneous sensory endings.
    Authors: Passmore Et al.
    Front Mol Neurosci  2012;5:63
  16. Increased Kv1 channel expression may contribute to decreased sIPSC frequency following chronic inhibition of NR2B-containing NMDAR.
    Authors: He Et al.
    Neuropsychopharmacology  2012;37:1338
  17. Restoration of ion channel function in deafness-causing KCNQ4 mutants by synthetic channel openers.
    Authors: Leitner Et al.
    Br J Pharmacol  2012;165:2244
  18. KV7 channels regulate muscle tone and nonadrenergic noncholinergic relaxation of the rat gastric fundus.
    Authors: Ipavec Et al.
    Pharmacol Res  2011;64:397
  19. AKAP79/150 signal complexes in G-protein modulation of neuronal ion channels.
    Authors: Zhang Et al.
    J Neurosci  2011;31:7199
  20. 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
  21. The contribution of Kv7 channels to pregnant mouse and human myometrial contractility.
    Authors: McCallum Et al.
    J Neurosci  2011;15:577
  22. Norepinephrine causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+.
    Authors: Zemkova Et al.
    Endocrinology  2011;152:3842
  23. MinK-dependent internalization of the IKs potassium channel.
    Authors: Xu Et al.
    Cardiovasc Res  2009;82:430
  24. 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
  25. Endolymphatic sodium homeostasis by extramacular epithelium of the saccule.
    Authors: Kim and Marcus
    J Neurosci  2009;29:15851
  26. 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.
    J.Urol.  2009;182:330
  27. 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
  28. 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
  29. 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
  30. 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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