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).

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.

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

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

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

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

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.

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

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.

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.

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.

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.

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.

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.

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.

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

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

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).

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

RPR260243 was the first reported hERG 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.

Nicorandil is potassium channel activator.

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

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.

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.

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.