A imidazoline compound that stimulate insulin release by inhibition of ATP-dependent K+ channels and inducing of Ca2+ mobilization in mouse pancreatic beta-cells.

A low micromolar (EC50=9.7 uM, K2P2.1), selective activator of temperature- and mechano-sensitive K2P potassium channels.

A novel potent, selective Kv2 channel inhibitor that potently inhibits Kv2.1 and Kv2.2 with IC50 of 0.14 and 0.09 uM, respectively.

A novel selective, small molecule large-conductance Ca(2+)-activated K(+) channel (BKCa, KCa1.1, MaxiK) positive modulator with EC50 of 11 uM.

A novel specific, cell permeant modulator of Kv3 channels with EC50 of 0.9 and 1.9 uM for Kv3.1b and Kv3.2a, respectively.

A novel, highly potent positive modulator of Kv7 channels with EC50 of 100 nM (Kv7.2-Kv7.5).

A potent inwardly rectifying K+ channel Kir7.1 inhibitor with IC50 of 5.6 uM in T1+ flux assays.

BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM). BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively

A potent Kir7.1 inhibitor with IC50 of 2.0 uM, induces long-lasting uterine contractility similar to those observed with VU590..

A potent, selective renal outer medullary potassium channel (ROMK, Kir1.1) inhibitor with IC50 of 0.24 uM in T1+ flux assays.

A potent, selective, and oral renal outer medullary potassium channel (ROMK) inhibitor with IC50 of 68 nM.

A selective renal outer medullary potassium channel (ROMK, Kir1.1) inhibitor with IC50 of 8 uM in T1+ flux assays, does not inhibit Kir7.1 at 100 uM.

A selective, potent peptidyl blocker of the big conductance Ca2+-activated K+ channel (BKCa, KCa1.1, MaxiK) with IC50 of 0.25 nM.

A selective, potent peptidyl blocker of the big conductance Ca2+-activated K+ channel (BKCa, KCa1.1, MaxiK).

Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM.

AP14145 (AP-14145) is a potent, selective negative allosteric modulator of KCa2.2 and KCa2.3 with equal potency (IC50=1.1±0.3 uM).

AUT-1 is a novel specific, cell permeant modulator of Kv3 channels with EC50 of 4.7 and 4.9 uM for Kv3.1b and Kv3.2a, respectively.

Azimilide 2Hcl(NE-10064 2Hcl) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.

Chlorpromazine Hydrochloride is a dopamine and potassium channel inhibitor used as the prototypical phenothiazine antipsychotic drug.

Diazoxide is a well-known small molecule that activates KATP channels in the smooth muscle of blood vessels and pancreatic beta-cells by increasing membrane permeability to potassium ions.

Dronedarone is a Class III antiarrhythmic and a multi-channel blocker for atrial fibrillation. It blocks potassium and sodium and is a calcium channel protein inhibitor.

E-4031 is a benzenesulfonamide antiarrhythmic agent; blocks the ATP-sensitive potassium channel.

Flupirtine maleateis a non-opioid, centrally acting analgesia, muscle relaxation and neuroprotection. Currently under a clinical trial (recruiting phase) as a treatment for Multiple Sclerosis and has been used as an analgesic.

GAL-021 is a new intravenous BKCa-channel blocker.

ICA 069673 is a potassium channel opener with selective action for KCNQ2 and KCNQ3 (EC50=0.69 μM). No meeasurable activity was displayed over a variety of cardiac ion channels.

IK1 inhibitor PA-6 is an efficient, specific inhibitor of inward rectifier current (IK1), blocks KIR2.x currents of human and mouse with IC50 of 12-15 nM.

Inhibitor of ATP-sensitive K+ channel activity in MIN 6 cells. Has also been shown to bind sulfonylurea receptors as well.

ML-213 (CID-3111211) is a selective KV7.2 (KCNQ2) and KV7.4 (KCNQ4) channel opener (EC50 values are 230 and 510 nM for KV7.2 and KV7.4 respectively).

ML-277 is a potent activator of KCNQ1 ( K(v)7.1) channels (EC50 = 260 nM).

ML297 (VU0456810) is the First Potent and Selective Activator of the GIRK Potassium Channel, Displays Antiepileptic Properties in Mice.

ML335 is a selective activator of both TREK-1 and TREK-2.

ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3) with IC50 of 4 nM(thallium influx fluorescent assay) and 16 nM(automated electrophysiology assay).

ML402 is a selective TREK-1 activator.

Nicorandil is potassium channel activator.

Nimodipine(Nimotop) is a dihydropyridine derivative and an analogue of the calcium channel blocker nifedipine, with antihypertensive activity.Nimodipine decreases intracellular free Ca2+,Beclin-1 and autophagy.

NS 11021 is an activator of large-conductance Ca2+-activated potassium channels (BKCa, KCa1.1).

NS-1619 is a selective MaxiKα (large conductance calcium activated potassium channel) activator.

NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator (EC50 = 10.5 μM).

NS309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels); increases Ca2+ sensitivity. Displays no activity at BK channels.

NS6180 is a novel inhibitor of the intermediate-conductance Ca2+-activated K+ channel (KCa3.1)

Pinacidil monohydrate, an antihypertensive drug, is a potassium channel activator.

Retigabine 2Hcl (Ezogabine; D23129) is a Kv7.2-7.5 (KCNQ2-5) neuronal potassium channel opener witrh anticonvulsant activity.

RPR260243 was the first reported hERG channel activator.

Senicapoc(ICA17043) is a potent and selective Gardos channel blocker; blocked Ca(2+)-induced rubidium flux from human RBCs/ inhibited RBC dehydration with IC50s of 11 nM/30 nM, respectively. IC50 value: 11/30 nM [1] Target: Gardos channel in vitro: I

SKA-121 is a positive-gating modulator of intermediate-conductance calcium-activated potassium channels (IKCa1/KCa3.1) with an EC50 value of 109 nM using whole-cell patch-clamp electrophysiology with calcium in the internal solution.

The first potent, selective, CNS penetrating inward rectifier potassium channel Kir7.1 (KCNJ13) inhibitor with IC50 of 0.31 uM.

The first small-molecule inhibitor of renal outer medullary potassium channel (ROMK, Kir1.1) and Kir7.1 with IC50 of 294 nM for ROMK.

Tolazamide is a first generation sulfonylurea that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2; IC50 = 4.2 µM in HEK293 cells transfected with the human receptor).

Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic drug.

TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM).

Dofetilide N-oxide (UK-116856) is a metabolite of Dofetilide. Dofetilide is a class III antiarrhythmic agent that blocks potassium channels.

4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic.

NS8593 hydrochloride is a potent and selective small conductance Ca2+-activated K+ channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca2+), and does not affect the Ca2+-activated K+ channels of intermediate and large conductance (hIK and hBK channels, respectively).

A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization.

VU041 is a first submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti inward rectifier potassium 1 (Kir1) channels with IC50 values of 2.5 μM and 1.7 μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC50 of 12.7 μM), and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. VU041 also induces impaired Malpighian tubule function.

Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis.

Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.

Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K+ channels.

Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877). Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.

OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K+ channels and has Ca2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.

A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.

(±)-Naringenin is a naturally-occurring flavonoid. (±)-Naringenin displays vasorelaxant effect on endothelium-denuded vessels via the activation of BKCa channels in myocytes.

H3B-120 is a competitive, selective and allosteric inhibitor of carbamoyl phosphate synthetase 1 (CPS1) with IC50 of 1.5 μM and Ki of 1.4 μM. H3B-120 exhibits anti-tumor activity.

Dehydrosoyasaponin I (Soyasaponin Be;DHS-I), a triterpene glycoside, is a potent and reversible calcium-activated potassium (maxi-K) channels activator.

VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC50 of 61 nM.

AMP-PNP tetralithium (Adenylyl-imidodiphosphate tetralithium) is a non-hydrolysable analogue of ATP and inhibits KATP channels.

12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca2+-activated K+ (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca2+ and stimulates transmitter release.

Dihydroisopimaric acid activates large conductance Ca2+ activated K+ (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp.

5-Hydroxydecanoate sodium is a selective ATP-sensitive K+ (KATP) channel blocker (IC50 of ~30 μM). 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity.

A2793 is an efficient TWIK-related acid-sensitive K+ channel (TASK)-1 inhibitor, with an IC50 of 6.8 μM.

Minoxidil sulfate, a potent and ATP-sensitive K+ channel opener, is the sulfated metabolite of minoxidil. Minoxidil sulfate is considered as a vasodilator to promote hair growth in vivo.

2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4).

Tetraethylammonium chloride is a non-selective potassium channel blocker. Tetraethylammonium chloride is a good substrate for organic cation transporter (OCTN1). Tetraethylammonium chloride antitumor properties.

Cloperastine hydrochloride inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM.

Isopimaric acid is a potent opener of large conductance calcium activated K+ (BK) channels.

O-Nornuciferine, an aporphine-type alkaloid from lotus leaf, is a potent hERG channel inhibitor.

Charybdotoxin TFA, a 37-amino acid peptide isolated from venom of the scorpion Leiurus quinquestriatus var. hebraeus, is a K+ channel blocker.

ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.

ShK-Dap22 TFA is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 TFA is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.

Agitoxin-2 is a K+ channel inhibitor, with IC50 values of 201 pM and 144 pM for mKV1.3 and mKV1.1, respectively).

Agitoxin-2 TFA is a K+ channel inhibitor, with IC50 values of 201 pM and 144 pM for mKV1.3 and mKV1.1, respectively).

Spadin, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin binds specifically to TREK-1 with an affinity of 10 nM. Spadin is an efficient antidepressant in mice.

Spadin TFA, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin TFA binds specifically to TREK-1 with an affinity of 10 nM. Spadin TFA is an efficient antidepressant in mice.

Chlorahololide C, a lindenane sesquiterpenoid dimer, is isolated from Chloranthus holostegius. Chlorahololide C is a potent and selective potassium channel blocker, with an IC50 of 3.6 μM.

L-Palmitoylcarnitine chloride, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine chloride inhibits KATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2.

Quinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM.

Lei-Dab7 is a high affinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.

Nifekalant hydrochloride (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC50 of 10 µM. Nifekalant hydrochloride can be used for refractory ventricular tachyarrhythmias research.

Levosimendan D3 (Simsndan D3) is a deuterium labeled Levosimendan. Levosimendan is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.

UCL 1684 (dibromide) is a first nanomolar, non-peptidic small conductance calcium-activated potassium (SK) channel blocker. UCL 1684 (dibromide) is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of INa. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness.

Gliclazide D4 (S1702 D4) is the deuterium labeled Gliclazide. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic.

ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects.

Cesium chloride is a blocker of potassium channel. Cesium chloride prevents the decrease of Na+ transport produced by Alloxan. Cesium chloride has induced cardiac arrhythmias, including torsade de pointes in animal models.

DAD dichloride is a type of ion channel blocker that blocks voltage-gated potassium channels. DAD dichloride is a third-generation photoswitch that responds to visible light. DAD dichloride has the potential for restoring visual function.

DAD is a type of ion channel blocker that blocks voltage-gated potassium channels. DAD is a third-generation photoswitch that responds to visible light. DAD has the potential for restoring visual function.

BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.

Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist.

Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons.

Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA).

OSK-1 is a potent Kv channel blocker with IC50s of of 0.6 nM, 5.4 nM, 0.014 nM for Kv1.1, Kv1.2 and Kv1.3, respectively. OSK1 is a moderate blocker of Ca2+-activated KCa3.1 channel with an IC50 of 225 nM. OSK-1 belongs to α-KTx3 toxins and is used as a immunosuppressive drug.

Alloisolithocholic acid (AILCA) activates large-conductance calcium-activated potassium (BK) channels with an EC50 value of 44.21 μM in Xenopus oocytes.

Cibenzoline is a potent inhibitor of KATP channel with directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline is a class Ia antiarrhythmic drug. Cibenzoline has little anticholinergic activity. Cibenzoline markedly attenuate LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for the research of hypertrophic obstructive cardiomyopathy.

Pinacidil is a potent activator of potassium channel. Pinacidil is an antihypertensive agent which hyperpolarises vascular smooth muscle by opening K+-channels. Pinacidil significantly improves the reperfusion function and cardiac compliance. Pinacidil has direct cardioprotective efficacy.

Tipepidine reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine subsequently activates VTA dopamine neuron. Tipepidine, a non-narcotic antitussive, exerts an antidepressant-like effect.

Chromanol 293B is a selective blocker of the slow delayed rectifier K+ current (IKs) with IC50 of 1-10 μM and a weak inhibitor of KATP channel. Chromanol 293B also blocks the CFTR chloride current with an IC50 of 19 μM.

Clamikalant sodium (HMR 1098) is an ATP-sensitive potassium (KATP) channel blocker. Clamikalant sodium can be used for the research of arrhythmia.

DPO-1 is a potent inhibitor of the voltage-gated potassium channel subtype Kv1.5 and a blocker of ultrarapid delayed rectifier potassium current. DPO-1 prevents atrial arrhythmia.

KCa2 channel modulator 2 (compound 2q) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 2 exhibits similar potency on the rat KCa2.2a and human KCa2.3 channel subtypes, with EC50s of 0.64 μM and 0.60 μM, respectively

KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 1 potentiates human KCa2.3 channels with an EC50 value of 0.19 μM and 0.99 μM on the rat KCa2.2 channel subtype.

QO 58 is a potent modulator of K(v)7 channels. QO-58 increases the current amplitudes, shifts the voltage-dependent activation curve in a more negative direction and slows the deactivation of K(v)7.2/K(v)7.3 currents. QO-58 has the potential for the research of diseases associated with neuronal hyperexcitability.

Linoleoyl glycine is a modified polyunsaturated fatty acid. Linoleoyl glycine has activating effects on human KCNQ1/KCNE1 (hKCNQ1/hKCNE1) channels expressed in Xenopus oocytes.

A potent, selective hERG potassium channel (Kv11.1) activator.

A293 (AVE1231) is a potent and antiarrhythmic compound and selective inhibitor of two-pore-domain potassium channel TASK-1 (KCNK3, hK2P3.1).A293 (AVE1231) is an inhibitor of hKv1.5 currents with predominant action on channels in their open state.A293 (1 uM) prominently depolarized arterial smooth muscle and increased basal tone level and contractile responses to methoxamine of arteries from young rats but had almost no effect in adult rats.Pharmacological inhibition of atrial TASK-1 currents via A293 (AVE1231) exerts antiarrhythmic effects in vivo as well as in silico, resulting in acute cardioversion of paroxysmal trial fibrillation (AF).

Benzopyran-G1 is a selective inhibitor of cardiac acetylcholine-activated inwardly rectifying K+ current (IKACh), composed of Kir3.1/Kir3.4 heterotetrameric and Kir3.4 homotetrameric channel subunits.

CTIBD is a novel potent activator of the BKCa channel with EC50 of 3.9 uM.CTIBD showed significantly higher potency compared with three other known BKCa activators: NS 1619, NS 11021, and rottlerin.CTIBD induced a reversible potentiation of macroscopic outward currents of the BKCa channel, CTIBD activates both rSlo/rβ1 and rSlo/rβ4 coexpressed channels mainly by decreasing the closing rate of the channel.CTIBD concentration-dependently reduced ACh-induced contractions in isolated rat urinary bladder strips. CTIBD effectively restored frequent voiding contraction and lowered voiding volume without affecting other bladder function parameters in acetic acid-induced overactive bladder (OAB) model (i.p. 20 mg/kg).

GAT1508 (GAT-1508) is a potent, specific activator for brain-expressed GIRK1/2 channels (EC50=75 nM), specifically activates the brain GIRK1/2 over the cardiac GIRK1/4; GAT1508 is an allosteric modulator of channel–phosphatidylinositol 4,5-bisphosphate interactions. GAT1508 effectively extinguished conditioned fear in rodents and lacked cardiac and behavioral side effects, suggesting its potential for use in pharmacotherapy for post-traumatic stress disorder.

KNa1.1 inhibitor 31 is a potent, selective, orally available inhibitor of sodium-activated potassium channel KNa1.1 (Slack, Slo2.2) with IC50 of 40 nM (hKNa1.1 WT).KNa1.1 inhibitor 31 reduced seizures and interictal spikes in a mouse model of KCNT1 GoF.

Kv2.1-syntaxin inhibitor 15 (Kv2.1-syntaxin-IN-15, Cpd5) is a small molecule Kv2.1-syntaxin-binding inhibitor (IC50=5.5 uM) with neuroprotective properties.Kv2.1-syntaxin inhibitor 15 competitively binds syntaxin against C1aB-containing Kv2.1 peptides with IC50 of 5.5 uM.Kv2.1-syntaxin inhibitor 15 (10 uM) significantly diminished threo-β-benzyloxyaspartate (TBOA, 75 uM)-induced toxicity neuronal cultures, ameliorated significant cellular damage, by preventing the expression of enhanced Kv2.1-mediated K+ currents.Kv2.1-syntaxin inhibitor 15 is a first-in-class inhibitor of Kv2.1 binding to Syntaxin, likely due to inhibition of the C1a region of Kv2.1 binding to syntaxin.Cpd5 (10 μM) does not affect evoked AMPAR EPSCs in layer 2/3 corticocallosal neurons in the mouse auditory cortex.

Lu AA41178 is a potent, pan-selective Kv7.2-7.5 opener with EC50 of 1.5, 0.6 20.5, and 37.0 uM for Kv7.2, Kv7.2/7.3, Kv7.4 and Kv7.5, respectively.Lu AA41178 displays no activity at Kv7.1 channels, has no potentiating impact on currents through GABAA ion channels, and a clean off-target profile against common cardiac ion channels.Lu AA41178 significantly increased the seizure thresholds in mice, demonstrating anticonvulsant efficacy in the maximum electroshock seizure threshold test and PTZ seizure threshold test.Lu AA41178 demonstrated antipsychotic-like activity by reducing amphetamine-induced hyperlocomotion in mice as well as lowering conditioned avoidance responses in rats, significantly reduced immobility in mouse model with antidepressant predictivity.

VU 0606170 is a selective sodium-activated potassium channel KNa1.1 (Slack, Slo2.2) inhibitor with EC50 of 1.84 and 1.16 uM for WT Slack and A934T Slack, repectively.VU0606170 did not modulate HEK293 channels expressing Slick, Slo1 α1/β1, Slo1 α1/β2, Slo1 α1/β3, Slo1 α1/β4, or Slo3 channels. also potently inhibits G288S and R428Q Slack channels.VU0606170 also proved effective at significantly decreasing the firing rate in overexcited, spontaneously firing cortical neuron cultures.

VU0468554 (VU 0468554) is a nove potent, selective inhibitor of GIRK channel with IC50 of 0.85 and 2.6 uM for GIRK1/GIRK4 and GIRK1/GIRK2 in cellular assays.VU0468554 more effectively inhibits the cardiac GIRK channel than the neuronal GIRK channel, inhibits Gβγ-activated GIRK channels in noncompetitive and potentially uncompetitive fashion.VU0468554 competitively inhibits GIRK-channel activation by ML297, a GIRK-channel activator.In the isolated heart model, VU0468554 partially reversed carbachol-induced bradycardia in hearts from wild-type mice but not Girk4-/- mice.

VU6036720 (VU 6036720) is the first potent, selective inhibitor of heteromeric Kir4.1/Kir5.1 (KCNJ10/KCNJ16) with IC50 of 0.24 uM.VU6036720 displays >30-fold selective for Kir4.1/5.1 over homomeric Kir4.1 channels, Kir1.1, Kir2.1, Kir2.2, Kir2.3, Kir4.2, Kir6.2/SUR1, Kir6.1/SUR2b and Kir7.1.VU6036720 inhibits Kir4.1/5.1 activity through a reduction of channel open-state probability and single-channel current amplitude, does not induce diuresis in vivo.VU6036720 showwd an IC50 in 3 uM in Tl+ flux assays, approximately 7-times more potent at inhibiting Kir4.1/5.1 than fluoxetine and amitriptyline.VU6036720 represents the current state-of-the-art Kir4.1/5.1 inhibitor that should be useful for probing the functions of Kir4.1/5.1 in vitro and ex vivo.

XAF-1407 (XAF1407) is a novel putatively potent and highly specific IK,Ach (Kir3.1/3.4 and Kir3.4/3.4) inhibitor (IC50 of 1.1 and 3.2 nM, respectively).XAF-1407 displays highly selectivity other relevant cardiac ion channels, with selectivity ratios for Kir3.1/3.4 of >2,000–8,000 fold up to >27,000 fold for Nav1.5 and Kir2.1, respectively.XAF-1407 potently and selectively inhibited Kir 3.1/3.4 and Kir 3.4/3.4, underlying the IK,ACh current.XAF-1407 treatment in horses prolonged atrial effective refractory period as well as decreased atrial fibrillatory rate significantly and successfully cardioverted atrial fibrillation (AF), although with a decreasing efficacy over time. XAF-1407 shortened atrioventricular-nodal refractoriness, without effect on QRS duration.

GAL-021 sulfate is a potent BKCa-channel blocker. GAL-021 sulfate inhibits KCa1.1 in GH3 cells. GAL-021 sulfate is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 sulfate increases minute ventilation in rats and non-human primates.

HN37 as a potent and chemically stable antiepileptic drug candidate, with an EC50 of 37 nM for KCNQ2.

DDO-02005 is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine.

DDO-02001 is a moderately potent Kv1.5 potassium channel inhibitor with an IC50 value of 17.7 μM. DDO-02001 can be used for researching anti-arrhythmia.

DDO-02005 (free base) is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 (free base) has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine.

Dendrotoxin K is a Kv1.1 channel blocker. Dendrotoxin K determines glutamate release in CA3 neurons in a time-dependent manner through the control of the presynaptic spike waveform.

PBFI-AM is a useful tool to determine intracellular K+ content.

Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes.

N-Bromoacetamide can irreversibly remove sodium channel inactivation in the cytoplasmic face of the membrane, also decreasing K current rapid inactivation.

NS-8, a pyrrole derivative, activates the Ca2+-sensitive k+-channel. NS-8 can suppress the micturition reflex by decreasing afferent pelvic nerve activity. NS-8 can be used in the research of urinary frequency and incontinence.

Clobutinol is a compound that has anti-tussive effects. Clobutinol affects heart rate and blood pressure, it can be used for cough related research.

TRAM-39 is a selective blocker of intermediate conductance Ca2+-activated K+ (IKCa) channels. TRAM-39 inhibits KCa3.1 channel with an IC50 value of 60 nM. TRAM-39 can be used for the research of ataxia, epilepsy, memory disorders, schizophrenia and Parkinson’s disease.

β-Bag cell peptide is a neuroactive peptide. β-Bag cell peptide elevates cyclic AMP levels in the bag cell neurons. β-Bag cell peptide decreases the amplitudes of the voltage-dependent potassium currents.

Foslevcromakalim (QLS-101) is a ATP-sensitive potassium channel opener. Foslevcromakalim is the prodrug used for ocular hypotensive effect.

Etidocaine (hydrochloride) is a long aminoamide local anaesthetic that inhibits flicker potassium channel with an IC50 of 8.6 µM.

ML213 is a novel potent, selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) activator with EC50 of 230 and 510 nM, respectively. ML213 displays >80-fold selectivity over other related potassium channels (KCNQ1/3/5). ML213 causes significant hyperpolarization in mesenteric artery smooth muscle cells, shows potent vasorelaxant effects in different blood vessels.

3hi2one-G4 is a highly selective small molecule activator targeting GIRK4 homomeric channels, does not activate GIRK2, GIRK1/2 or GIRK1/4 channels.

ACOU001 (ACOU 001) is a potent small-molecule agonist of Kv7.4 (KCNQ4) channel with potential effect against ge-related hearing loss (ARHL) and other hearing impairments related to compromised KV7.4 function.

ACOU085 (ACOU 085) is a potent small-molecule agonist of Kv7.4 (KCNQ4) channel with higher potency than ML-213 in the nanomolar range.

AUT00201 is a potent, selective Kv3 potassium channel modulator with potential for the treatment of rare epilepsy syndromes.

BK channel modulator BC5 is an allosteric modulator of BK type Ca2+-activated K+ channels, interacts with the CTD-VSD interface and specifically modulates the Ca2+ dependent activation mechanism.

C101248 is the first selective small-molecule inhibitor of tandem pore domain halothane-inhibited K+ channel 1 (THIK-1) with IC50 of 50 nM for both mouse and human THIK-1.

Ebio1 is a selective voltage-gated potassium channel KCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channel gate with greater conductance at a saturation voltage (+50 mV).

LAKI (Light Activated K+ channel Inhibitor) is a specific photoswitchable inhibitor of the pain-related two-pore-domain potassium (K2P) TREK and TRESK channels.

ML308 (ML 308) is a potent, selective inhibitor of two-pore domain potassium channel KCNK9 (TASK-3, K2P9.1) with IC50 of 130 nM in thallium influx fluorescent assays and 413 nM in automated electrophysiology assays, respectively.

NIP-142 (NIP142) is an anti-arrhythmic agent by targeting cardiac K+ channel Kv1.5 (Kv1.5) currents, inhibits the steady-state phase with IC50 of 4.75 uM.

NPBA is a potent, selective pharmacological activator for K2P channel TASK-3 with EC50 of 6.7 uM (TASK-3 whole-cell currents), shows good selectivity between TASK channels.

NPBA-4 is a potent selective TWIK2 channel inhibitor with IC50 of 8.41 uM. shows little to no effects on TWIK1 channel.

SCR2682 is a potent, selective neuronal voltage-gated potassium Kv7/KCNQ/M channel opener (activator) with EC50 of 9.8 nM (Kv7.2/Kv7.3), 100-fold more potency than retigabine.

Tamapin TFA salt is a venom peptide from the Indian red scorpion (Mesobuthus tamulus), potent and selective inhibitor of small conductance calcium-activated potassium channel 2 (SK2, KCNN2) with IC50 of 24 pM.

TTQC-1 is a potent activator of the large-conductance Ca2+-activated K+ channel (BKCa channel), directly and reversibly activates the macroscopic current of BKCa channels expressed in Xenopus oocytes from both sides of the cellular membrane, increases the

VU0542270 is the first selective inhibitor of vascular Kir6.1/SUR2B KATP channel with IC50 of 129 nM, >300-fold selective over other members of the Kir channel family.

VU0546110 (VU 0546110) is a potent, selective inhibitor of the sperm-specific potassium channel SLO3 with IC50 of 1.29 uM, impairs sperm function.

VU0935685 is a potent, selective inhibitor of SLACK potassium channels with IC50 of 0.32 uM in in whole-cell, voltage-clamp electrophysiology (EP) assays, demonstrates selectivity versus hERG.

ZVS-08 is a selective inhibitor of the voltage-gated potassium channel KV10.1 with IC50 of 3.7 uM.