ICA-027243
Names
[ CAS No. ]:
325457-89-4
[ Name ]:
ICA-027243
[Synonym ]:
Benzamide,N-(6-chloro-3-pyridinyl)-3,4-difluoro
ZTZ233
UNII-VU7278D853
Biological Activity
[Description]:
ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects[1][2].
[Related Catalog]:
[Target]
EC50: 0.38 μM (KCNQ2/Q3 potassium channel)[2]
[In Vitro]
In SH-SY5Y human neuroblastoma cells, ICA-27243 produces membrane potential hyperpolarization that could be prevented by coadministration with the M-current inhibitors XE-991 and Linopirdine. ICA-27243 enhances both 86Rb+ efflux (EC50 = 0.2 μM) and whole-cell currents in Chinese hamster ovary cells stably expressing heteromultimeric KCNQ2/Q3 channels (EC50 = 0.4 μM). Activation of KCNQ2/Q3 channels is associated with a hyperpolarizing shift of the voltage dependence of channel activation (V1/2 shift of -19 mV at 10 μM)[1].
[In Vivo]
ICA-27243 (1-100 mg/kg; oral administration; male CD-1 mice) has anticonvulsant activity (ED50 of 8.4 mg/kg) in the mouse maximal electroshock epilepsy model[1]. Animal Model: Male CD-1 mice with electroshock assay[1] Dosage: 1-100 mg/kg Administration: Oral administration Result: Produced a dose-dependent increase in the latency to hind limb extension, exhibiting an ED50 value of 8.4 mg/kg.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C12H7ClF2N2O
[ Molecular Weight ]:
268.64700
[ Exact Mass ]:
268.02100
[ PSA ]:
45.48000
[ LogP ]:
3.64950