kv7.4

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.

ZTZ240 is a KCNQ2 channel activator used in the study of epilepsy.

Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active activator of Kv7.2/Kv7.3 channels and the TSPO. It 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). This compound protects motor neurons from degeneration caused by exposure to astrocyte-conditioned media from mice and humans with amyotrophic lateral sclerosis/frontotemporal dementia. Additionally, Kv7.2/Kv7.3 activator-3 stimulates axonal growth in dorsal root ganglia through TSPO and Kv7.2/3 activation and exhibits anticonvulsant effects in epilepsy models. It alleviates hyperalgesia in diabetic neuropathy patients, enhances the survival and regeneration of neurons after cervical neuropathy in rats, and accelerates the recovery of normal function in sensory and motor neurons.

NC00075159 is an opener of human KCNQ4 (Kv7.4) potassium channel.

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.

ML213 (CID-3111211) is a selective activator of Kv7.2 (KCNQ2) and Kv7.4 (KCNQ4) channels, enhances Kv7.2 and Kv7.4 channels with EC50s of 230 and 510 nM, respectively.

ML 297 is a selective Kir3.1/3.2 (GIRK1/2) channel activator (IC50 values are 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively). ML 297 exhibits no effect on GIRK2, GIRK2/3, Kir2.1 and Kv7.4 channels, and has minimal effect on a panel of other ion channels, receptors and transporters.

Ssm Spooky Toxin, derived from Scolopendra mutilans, exhibits potent lethality affecting both hematological and respiratory systems primarily through the inhibition of KCNQ (voltage-gated potassium channel family 7) channels. It demonstrates IC50 values of 2.8 μM for Kv7.4, 5.26 μM for Kv1.3, and 0.1-0.3 M for the Shal channel, respectively. Additionally, this toxin impedes cytokine production by selectively targeting the KV1.3 channel in T cells and is crucial for the centipede's circulatory system functions [1] [2] [3].

Bimokalner (Bimokalnerum) is an activator of the voltage-gated potassium channel (Kv7.4).

Ssm Spooky Toxin TFA, found in Scolopendra mutilans, effectively inhibits the KCNQ (voltage-gated potassium channel family 7) channels. Its IC50 values for Kv7.4, Kv1.3, and Shal channels are 2.8 μM, 5.26 μM, and 0.1-0.3 M, respectively. This toxin suppresses cytokine production by specifically targeting KV1.3 channels in T cells and plays a crucial role in the centipede's circulatory system.