channel modulator

KCa2 channel modulator 1 (compound 2o) is an effective, subtype-selective K/Ca2 channel positive modulator that potentiates rat KCa2.2 channels with an EC50 value of 0.99 μM and human KCa2.3 channels with an EC50 value of 0.19 μM [1].

KCa2 channel modulator 2 (compound 2q) is an effective, subtype-selective K/Ca 2 channel positive modulator with similar potency on the human K Ca 2.3 channel and rat K Ca 2.2a subtypes, exhibiting EC50 values of 0.60 μM and 0.64 μM, respectively [1].

Calcium channel-modulator-1, a calcium channel-modulator (IC50: 0.8 μM), specializes in blocking aortic constriction.

Kv3 modulator 1 is an imidazolidinedione-type orthosteric modulator of Kv3 voltage-gated potassium channels. Kv3 modulator 1 reverses mechanical hyperalgesia in rat models of neuropathic and inflammatory pain, with rapid onset and sustained, dose-dependent effects. Kv3 modulator 1 can be used to study the mechanisms underlying inflammatory pain and neurological disorders such as epilepsy and schizophrenia.

SAK3 is a novel modulator of nAChR activity that enhances T-type voltage-gated Ca2+ channel (T-VGCC) activity, and has potentiating effects on both Cav3.1 and Cav3.3 T-type Ca2+ channel currents.SAK3 is neuroprotective against scopolamine-induced cholinergic dysfunction in human neuroblastoma SH-SY5Y cells.SAK3 is used for the study of memory deficits and Alzheimer's disease. SAK3 can be used to study memory deficits and Alzheimer's disease.

GAL-021 an intravenous BKCa-channel blocker.

Niguldipine Free Base is a calcium channel blocker and antagonist with an IC₅₀=0.9 μM for Cav 3.2, suitable for cardiovascular system research.

HC-056456 (3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide) is a CatSper channel modulator.

Duramycin is a lantibiotic peptide antibiotic derived from Streptomyces cinnamoneus. It also functions as an ion channel modulator and has been investigated for cystic fibrosis (CF).

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.

AUT2 is a Kv3.1 channel modulator with the potential to treat sensory hyperreactivity in patients with FXS by shifting the activation of high-threshold currents to more negative potentials. This shift reduces high-threshold K+ currents and increases low-threshold K+ currents in neurons, restoring wave IV of the ABR. Due to its ability to regulate neuronal excitability, AUT2 is also promising for the treatment of hearing impairments.

AP30663 is a negative allosteric modulator of the KCa2 channel.

D3/5-HT receptor modulator-1 (compound 5i) is a selective antagonist of the dopamine D3 and 5-HT2A receptors, and a partial agonist at the 5-HT1A receptor. It exhibits Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the dopamine D3, 5-HT2A, and 5-HT1A receptors respectively. The compound shows lower affinity for the dopamine D2 receptor, 5-HT2C receptor, and hERG channel. D3/5-HT receptor modulator-1 possesses atypical antipsychotic properties.

Kv7.2/Kv7.3 modulator-2 (compound 7d) is a Kv7.2/Kv7.3 channel modulator with a pEC50 value of 7.42 for activating the Kv7.2/3 channels. This compound is applicable in the research of epilepsy, depression, brain injury, and pain.

P-gp modulator-7 (Compound 9e) is an inhibitor of P-glycoprotein (P-gp). It uniquely occupies the channel entrance of P-gp in a T-shaped conformation, blocking the peristaltic extrusion mechanism of transmembrane domains TM12 and TM9. This action inhibits P-gp from pumping drugs out of cells and reverses multidrug resistance (MDR) in tumor cells. P-gp modulator-7 shows promise for cancer research.

Maxi-K modulator 1 (Example 1) is a modulating agent for the large conductance calcium-activated potassium (Maxi-K) channels. It serves as a potent stimulator of Maxi-K channel activity and is applicable in research on Fragile X syndrome.

GMQ is an acid-sensitive ion channel modulator and a competitive GABAAR antagonist. It preferentially, efficiently, and competitively inhibits GABAA receptors, including α1β2, α1β2γ2, α4β2γ2, and α5β2γ2 subtypes. By inhibiting GABAergic neurotransmission, GMQ enhances neuronal excitability. Additionally, in the gastrointestinal system, GMQ exhibits antihistamine properties and can suppress gastric acid secretion.

TMEM16A modulator-1 (compound 36) is a positive modulator of calcium-activated chloride channel (CaCC) TMEM16A. It is useful for research associated with TMEM16A-related diseases, particularly in studying respiratory system diseases and conditions.

KCNQ2 modulator-1 is an agent that modulates the KCNQ2 channel.

Lifarizine methanesulfonate is a modulator of sodium-calcium channel that reduces ischemic brain damage.

BDF 9148, a Na(+)-channel modulator, increases the contractile force of guinea-pig atria and papillary muscles.

LUF7346 is a potent negative allosteric modulator of Kv11.1 (hERG) channel with an IC₅₀ of 35.6 ± 3.2 nM.

PZ-II-029 is a modulator of α6β3γ2-selective GABAA channel.

VU0405601 is a potent pharmacological activator of the KV11.1 channel (hERG) that functions as a hERG agonist, thereby protecting cardiac tissue against arrhythmias and ventricular tachycardia induced by other hERG-inhibiting compounds such as Dofetilide.