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 a voltage-gated potassium channel Kv3 modulator that can be used to study neurologic-level diseases.

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 a₁-adrenergic receptor antagonist and a clinical modulator of multidrug resistance.

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

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.

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.

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.

Dexmecamylamine( TC-5214, NIH-11008) is used as a nicotinic channel modulator with antidepressant activity.

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective positive modulator of Nav1.1 channels and also increases the activity of Nav1.2 and Nav1.5 channels while not affecting Nav1.4, Nav1.6, and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

KCa2 (small conductance Ca2+-activated potassium) channel negative allosteric modulator (IC50 = 1.1 μM). Increases the EC50 of Ca2+ on KCa2.3 channels by ~3-fold. Prolongs atrial effective refractory period (AERP) in rats. Reduces atrial fibrillation (AF) duration and prolongs atrial refractoriness without affecting ventricular refractory period in an animal AF model. Diness et al (2017) Termination of vernakalant-resistant atrial fibrillation by inhibition of small-conductance Ca2+-activated K+ channels in pigs. Circ.Arrhythm.Electrophysiol. 10 e005125 PMID:29018164 |Simó-Vicens et al (2017) A new negative allosteric modulator, AP14145, for the study of small conductance calcium-activated potassium (KCa2) channels. Br.J.Pharmacol. 174 4396 PMID:28925012

AP14145 hydrochloride is a potent negative allosteric modulator of K Ca 2 (SK) channels, specifically targeting K Ca 2.2 (SK2) and K Ca 2.3 (SK3) channels with an IC 50 of 1.1 μM. Inhibition of AP14145 hydrochloride is highly influenced by S508 and A533 amino acids present in the channel. This compound effectively extends the atrial effective refractory period (AERP) in rats and exhibits antiarrhythmic properties in a Vernakalant-resistant porcine model of atrial fibrillation (AF).

SK3 Channel-IN-1 (compound 7a) is a potent and selective SK3 channel modulator that effectively inhibits breast cancer MDA-MB-435 cell migration with low cytotoxicity in other cell lines, and it modulates ion channel activity in cancer cells [1].

Azidopine is a photoactive dihydropyridine channel blocker which may also act as a multidrug resistant (MDR) modulator.