kv7

Kv7.2 Kv7.3 agonist 1 (Compound 16) is an orally effective agonist for the KV7.2 7.3 channels (KV7.2 7.3 channel KCNQ2 3) with an EC50 of 1.03 μM. This compound demonstrates analgesic effects in mouse models of chronic constriction injury (CCI) and Streptozotocin-induced diabetic peripheral neuropathy (DPNP), with ED50 values of 12.02 mg kg and 9.63 mg kg, respectively.

Kv7.2 Modulator 1 (compound 10), a modulator of the Kv7.2 channel, is utilized in epilepsy research.

Kv7.2 Kv7.3 Activator-1 (compound 517) serves as a powerful activator of the Kv7.2 Kv7.3 channels, exhibiting an EC50 value of less than 1 µM. It holds potential for use in neurological disease research.

XE991 is a novel and selective Kv7 (KCNQ) channel blocker.XE 991 dihydrochloride inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channels, and M-current, and can be used for the study of neurological diseases.

DMP-543 (XR-543) is a KV7 channel blocker that enhances neurotransmitter release.

Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo.

Linopirdine (DuP 996) is a TRPV1 agonist. Linopirdine is an orally active and selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor (IC50: 2.4 μM). Linopirdine is a cognitive enhancer. It acts by stimulating release of acetylcholine and other neurotransmitters.Linopirdine is a putative cognition-enhancing drug that increases acetylcholine release in rat brain tissue.

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

KV7 (KCNQ) voltage-gated potassium channels blocker

QO-58 is a novel Kv7 activator (opener) that activates neuronal Kv7 KCNQ M channels, dose-dependently activating Kv7 currents, enhancing native neuronal M currents, and causing a decrease in evoked action potentials. It has anti-nociceptive effects on inflammatory pain and can be used for neuronal excitability disorders.

PF05020182 is novel potent and selective Kv7.2 4 potassium channel opener. PF-05020182 (2) significantly inhibits convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 support further development as an adjunctive treatment of refractory epilepsy. Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in controlling spontaneous electrical activity during epileptic seizures.