1361107-81-4
Chemical Structure
Kv7.2/Kv7.3 activator-3
- CAS No.: 1361107-81-4
- Formula:C22H20F4N2O3
- Molecular Weight:436.40
IUPAC Name: N-(3-fluorobenzyl)-1-(2-methoxyethyl)-4-methyl-2-oxo-7-(trifluoromethyl)-1,2-dihydroquinoline-3-carboxamide
InChIKey: XPANITDISRRBCJ-UHFFFAOYSA-N
SMILES: O=C(C1=C(C)C2=C(N(CCOC)C1=O)C=C(C(F)(F)F)C=C2)NCC3=CC=CC(F)=C3
Biological Activity: Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons[1][2][3][4].
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Kv7.2/Kv7.3 activator-3 | Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons. | |||||||||||||||||||||
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- [1]. Masegosa VM, et al. Novel Dual Mechanism GRT-X Agonist Acting on Kv7 Potassium Channel/Translocator Protein Receptor Prevents Motoneuron Degeneration Following Exposure to Mouse and Human Amyotrophic Lateral Sclerosis/Frontotemporal Dementia Astrocyte-Conditioned Media. ACS Chem Neurosci. 2025 Aug 6;16(15):2887-2900 [Content Brief]
- [2]. El Chemali L, et al. GRT-X Stimulates Dorsal Root Ganglia Axonal Growth in Culture via TSPO and Kv7.2/3 Potassium Channel Activation. Int J Mol Sci. 2024 Jul 3;25(13):7327. [Content Brief]
- [3]. Bloms-Funke P, et al. The novel dual-mechanism Kv7 potassium channel/TSPO receptor activator GRT-X is more effective than the Kv7 channel opener retigabine in the 6-Hz refractory seizure mouse model. Neuropharmacology. 2022 Feb 1;203:108884. [Content Brief]
- [4]. Bloms-Funke P et al.. A novel dual mode-of-action anti-hyperalgesic compound in rats which is neuroprotective and promotes neuroregeneration. Eur J Pharmacol. 2022 May 15;923:174935. [Content Brief]
Keywords
