Catalog Number: 2000
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.
Background References
  1. 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.
    J.Pharmacol.Exp.Ther., 1998;285:724
  2. Molecular basis for differential sensitivity of KCNQ and IKs channels to the cognitive enhancer XE991.
    Wang et al.
    Mol.Pharmacol., 2000;57:1218
  3. KCNQ/M currents in sensory neurons: significance for pain therapy.
    Passmore et al.
    J.Neurosci., 2003;23:7227
  4. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel.
    Wang et al.
    Science, 1998;282:1890
Citations:

The citations listed below are publications that use Tocris products. Selected citations for XE 991 dihydrochloride include:

24 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. Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca2+-activated chloride channels.
    Authors: Salzer Et al.
    Neuropharmacology 2016;110 (A):277
  3. Kv1 channels and neural processing in vestibular calyx afferents.
    Authors: Meredith Et al.
    Mol Pharmacol 2015;9:85
  4. 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
  5. 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
  6. 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
  7. 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
  8. KV7 Channels Regulate Firing during Synaptic Integration in GABAergic Striatal Neurons.
    Authors: Pérez-Ramírez Et al.
    PLoS One 2015;2015:472676
  9. Effects of KCNQ2 gene truncation on M-type Kv7 potassium currents.
    Authors: Robbins Et al.
    PLoS One 2013;8:e71809
  10. 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
  11. 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
  12. Functional significance of M-type potassium channels in nociceptive cutaneous sensory endings.
    Authors: Passmore Et al.
    Front Mol Neurosci 2012;5:63
  13. 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
  14. Restoration of ion channel function in deafness-causing KCNQ4 mutants by synthetic channel openers.
    Authors: Leitner Et al.
    Br J Pharmacol 2012;165:2244
  15. AKAP79/150 signal complexes in G-protein modulation of neuronal ion channels.
    Authors: Zhang Et al.
    J Neurosci 2011;31:7199
  16. 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
  17. The contribution of Kv7 channels to pregnant mouse and human myometrial contractility.
    Authors: McCallum Et al.
    J Neurosci 2011;15:577
  18. 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
  19. MinK-dependent internalization of the IKs potassium channel.
    Authors: Xu Et al.
    Cardiovasc Res 2009;82:430
  20. 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
  21. 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
  22. 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
  23. 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
  24. 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
Expand to show all 24 Citations

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