XE 991 dihydrochloride

Names

[ Name ]:
XE 991 dihydrochloride

[Synonym ]:
10,10-bis(pyridin-4-ylmethyl)anthracen-9-one,dihydrochloride

Biological Activity

[Description]:

XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively[1].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[References]

[1]. Wang HS, et al. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science. 1998 Dec 4;282(5395):1890-3.

[2]. Zaczek R, 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. J Pharmacol Exp Ther. 1998 May;285(2):724-30.

Chemical & Physical Properties

[ Boiling Point ]:
625.3ºC at 760mmHg

[ Molecular Formula ]:
C₂₆H₂₀N₂O

[ Molecular Weight ]:
376.45

[ Flash Point ]:
332ºC

[ Exact Mass ]:
376.15800

[ PSA ]:
42.85000

[ LogP ]:
4.79250

[ Vapour Pressure ]:
6.84E-16mmHg at 25°C

[ Storage condition ]:
2-8°C

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
CB1530000

Articles

Loss of Local Astrocyte Support Disrupts Action Potential Propagation and Glutamate Release Synchrony from Unmyelinated Hippocampal Axon Terminals In Vitro.

J. Neurosci. 35 , 11105-17, (2015)

Neuron-astrocyte interactions are critical for proper CNS development and function. Astrocytes secrete factors that are pivotal for synaptic development and function, neuronal metabolism, and neuronal...

Inhibition of post-synaptic Kv7/KCNQ/M channels facilitates long-term potentiation in the hippocampus.

PLoS ONE 7 , e30402, (2012)

Activation of muscarinic acetylcholine receptors (mAChR) facilitates the induction of synaptic plasticity and enhances cognitive function. In the hippocampus, M(1) mAChR on CA1 pyramidal cells inhibit...

Raised activity of L-type calcium channels renders neurons prone to form paroxysmal depolarization shifts.

Neuromolecular Med. 15 , 476-92, (2013)

Neuronal L-type voltage-gated calcium channels (LTCCs) are involved in several physiological functions, but increased activity of LTCCs has been linked to pathology. Due to the coupling of LTCC-mediat...

Related Compounds

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