product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
XE 991 dihydrochloride
catalog :
2000/10
quantity :
10 mg (also 50 mg)
price :
233 USD
more info or order :
citations: 34
Reference
Pagani M, Albisetti G, Sivakumar N, Wildner H, Santello M, Johannssen H, et al. How Gastrin-Releasing Peptide Opens the Spinal Gate for Itch. Neuron. 2019;: pubmed publisher
Georgilis A, Klotz S, Hanley C, Herranz N, Weirich B, Morancho B, et al. PTBP1-Mediated Alternative Splicing Regulates the Inflammatory Secretome and the Pro-tumorigenic Effects of Senescent Cells. Cancer Cell. 2018;34:85-102.e9 pubmed publisher
Lezmy J, Lipinsky M, Khrapunsky Y, Patrich E, Shalom L, Peretz A, 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:E10234-E10243 pubmed publisher
Greene D, Kang S, Hoshi N. XE991 and Linopirdine Are State-Dependent Inhibitors for Kv7/KCNQ Channels that Favor Activated Single Subunits. J Pharmacol Exp Ther. 2017;362:177-185 pubmed publisher
Salzer I, Gantumur E, Yousuf A, Boehm S. Control of sensory neuron excitability by serotonin involves 5HT2C receptors and Ca(2+)-activated chloride channels. Neuropharmacology. 2016;110:277-286 pubmed publisher
Parent M, Amarante L, Swanson K, Laubach M. Cholinergic and ghrelinergic receptors and KCNQ channels in the medial PFC regulate the expression of palatability. Front Behav Neurosci. 2015;9:284 pubmed publisher
Sobieski C, Jiang X, Crawford D, Mennerick S. Loss of Local Astrocyte Support Disrupts Action Potential Propagation and Glutamate Release Synchrony from Unmyelinated Hippocampal Axon Terminals In Vitro. J Neurosci. 2015;35:11105-17 pubmed publisher
Pérez Ramírez M, Laville A, Tapia D, Duhne M, Lara González E, Bargas J, et al. KV7 Channels Regulate Firing during Synaptic Integration in GABAergic Striatal Neurons. Neural Plast. 2015;2015:472676 pubmed publisher
Meredith F, Kirk M, Rennie K. Kv1 channels and neural processing in vestibular calyx afferents. Front Syst Neurosci. 2015;9:85 pubmed publisher
Bordas C, Kovács A, Pál B. The M-current contributes to high threshold membrane potential oscillations in a cell type-specific way in the pedunculopontine nucleus of mice. Front Cell Neurosci. 2015;9:121 pubmed publisher
Lee K, Royston S, Vest M, Ley D, Lee S, Bolton E, et al. N-methyl-D-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity. Mol Brain. 2015;8:4 pubmed publisher
Robbins J, Passmore G, Abogadie F, Reilly J, Brown D. Effects of KCNQ2 gene truncation on M-type Kv7 potassium currents. PLoS ONE. 2013;8:e71809 pubmed publisher
Rubi L, Schandl U, Lagler M, Geier P, Spies D, Gupta K, et al. Raised activity of L-type calcium channels renders neurons prone to form paroxysmal depolarization shifts. Neuromolecular Med. 2013;15:476-92 pubmed publisher
Ooi L, Gigout S, Pettinger L, Gamper N. Triple cysteine module within M-type K+ channels mediates reciprocal channel modulation by nitric oxide and reactive oxygen species. J Neurosci. 2013;33:6041-6 pubmed publisher
Boehlen A, Henneberger C, Heinemann U, Erchova I. Contribution of near-threshold currents to intrinsic oscillatory activity in rat medial entorhinal cortex layer II stellate cells. J Neurophysiol. 2013;109:445-63 pubmed publisher
Köhn C, Schleifenbaum J, Szijártó I, Markó L, Dubrovska G, Huang Y, et al. Differential effects of cystathionine-?-lyase-dependent vasodilatory H2S in periadventitial vasoregulation of rat and mouse aortas. PLoS ONE. 2012;7:e41951 pubmed publisher
Passmore G, Reilly J, Thakur M, Keasberry V, Marsh S, Dickenson A, et al. Functional significance of M-type potassium channels in nociceptive cutaneous sensory endings. Front Mol Neurosci. 2012;5:63 pubmed publisher
He S, Shao L, Rittase W, Bausch S. Increased Kv1 channel expression may contribute to decreased sIPSC frequency following chronic inhibition of NR2B-containing NMDAR. Neuropsychopharmacology. 2012;37:1338-56 pubmed publisher
Bi Y, Chen H, Su J, Cao X, Bian X, Wang K. Visceral hyperalgesia induced by forebrain-specific suppression of native Kv7/KCNQ/M-current in mice. Mol Pain. 2011;7:84 pubmed publisher
Leitner M, Feuer A, Ebers O, Schreiber D, Halaszovich C, Oliver D. Restoration of ion channel function in deafness-causing KCNQ4 mutants by synthetic channel openers. Br J Pharmacol. 2012;165:2244-59 pubmed publisher
Zemkova H, Stojilkovic S, Klein D. Norepinephrine causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+. Endocrinology. 2011;152:3842-51 pubmed publisher
Ipavec V, Martire M, Barrese V, Taglialatela M, Curro D. KV7 channels regulate muscle tone and nonadrenergic noncholinergic relaxation of the rat gastric fundus. Pharmacol Res. 2011;64:397-409 pubmed publisher
Zhang J, Bal M, Bierbower S, Zaika O, Shapiro M. AKAP79/150 signal complexes in G-protein modulation of neuronal ion channels. J Neurosci. 2011;31:7199-211 pubmed publisher
Geier P, Lagler M, Boehm S, Kubista H. Dynamic interplay of excitatory and inhibitory coupling modes of neuronal L-type calcium channels. Am J Physiol Cell Physiol. 2011;300:C937-49 pubmed publisher
McCallum L, Pierce S, England S, Greenwood I, Tribe R. The contribution of Kv7 channels to pregnant mouse and human myometrial contractility. J Cell Mol Med. 2011;15:577-86 pubmed publisher
Kim S, Marcus D. Endolymphatic sodium homeostasis by extramacular epithelium of the saccule. J Neurosci. 2009;29:15851-8 pubmed publisher
Anderson U, Carson C, McCloskey K. KCNQ currents and their contribution to resting membrane potential and the excitability of interstitial cells of Cajal from the guinea pig bladder. J Urol. 2009;182:330-6 pubmed publisher
Xu X, Kanda V, Choi E, Panaghie G, Roepke T, Gaeta S, et al. MinK-dependent internalization of the IKs potassium channel. Cardiovasc Res. 2009;82:430-8 pubmed publisher
Joshi S, Sedivy V, Hodyc D, Herget J, Gurney A. KCNQ modulators reveal a key role for KCNQ potassium channels in regulating the tone of rat pulmonary artery smooth muscle. J Pharmacol Exp Ther. 2009;329:368-76 pubmed publisher
Kim S, Kim K, Raveendran N, Wu T, Pondugula S, Marcus D. Regulation of ENaC-mediated sodium transport by glucocorticoids in Reissner's membrane epithelium. Am J Physiol Cell Physiol. 2009;296:C544-57 pubmed publisher
Linley J, Rose K, Patil M, Robertson B, Akopian A, Gamper N. Inhibition of M current in sensory neurons by exogenous proteases: a signaling pathway mediating inflammatory nociception. J Neurosci. 2008;28:11240-9 pubmed publisher
Wladyka C, Feng B, Glazebrook P, Schild J, Kunze D. The KCNQ/M-current modulates arterial baroreceptor function at the sensory terminal in rats. J Physiol. 2008;586:795-802 pubmed
Strøbaek D, Hougaard C, Johansen T, Sørensen U, Nielsen E, Nielsen K, et al. 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. Mol Pharmacol. 2006;70:1771-82 pubmed
Yeung S, Greenwood I. Electrophysiological and functional effects of the KCNQ channel blocker XE991 on murine portal vein smooth muscle cells. Br J Pharmacol. 2005;146:585-95 pubmed
image
image 1 :
Tocris Bioscience 2000/10 image 1
Cat.No. 2000 - XE 991 dihydrochloride C26H20N2O.2HCl CAS No. 122955-13-9
product information
brand :
Tocris
MasterCode :
2000
SKU :
2000/10
product name :
XE 991 dihydrochloride
target :
Voltage-gated Potassium Channel Blockers
category :
Small Molecules
unit size :
10 mg (also 50 mg)
purity :
99%
observed molecular weight :
449.37
url print :
?utm_source=biocompare&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
XE 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 u M) and KV7.1 (KCNQ1) homomeric channels (IC50 = 0.75 u M) but is less potent against KV7.1/minK channels (IC50 = 11.1 u M). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo .
extended description :
Potent, selective KV7 (KCNQ) channel blocker; blocks M-currents
chemical name text :
10,10-bis(4-Pyridinylmethyl)-9(10H)-anthracenone dihydrochloride
formula :
C 26 H 20 N 2 O.2HCl
formula text :
C26H20N2O.2HCl
cas num :
122955-13-9
USD :
233 USD
product details :
Potent, selective KV7 (KCNQ) channel blocker; blocks M-currents
storage :
Desiccate at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK