XE 991 dihydrochloride
Cat. No. 2000
Chemical Name: 10,10-bis(4-Pyridinylmethyl)-9(10H)
Biological ActivityPotent 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.
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 / 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:
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.
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.
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.
Xu et al (2009) MinK-dependent internalization of the IKs potassium channel. Cardiovasc Res 82 430. PMID: 19202166.
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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