k(atp) channel

Glibornuride, a blocker of ATP-sensitive K+ channels (pKi: 5.75), inhibits high-affinity [3H]-glibenclamide binding with potencies corresponding to its K+ channel activity.

KRN 4884 is an opener of the K+ channel. KRN 4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM), in the presence of intracellular ATP (1 mM).

U-89232 is an opener of the cardioselective KATP channel.

Tifenazoxide is an effective and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has an anti-diabetic effect, can inhibit glucose-stimulated insulin release in vitro and in vivo.

1-((3R,4S)-3-hydroxy-2,2-dimethyl-6-(phenylsulfonyl)chroman-4-yl)pyrrolidin-2-one is an isomer of Rilmakalim, a potassium channel opener (PCO), which can activate ATP-sensitive K+ channels in the heart or other tissues

PCO 400 is an analog of comakalim that acts as a selective and potent ATP-sensitive K+ channel opener.

Isopulegol has antioxidant, and neuroactive properties. It also has gastroprotective effects induced by isopulegol appear to be mediated, at least in part, by endogenous prostaglandins, K+ATP channel opening and antioxidant proprieties related to GSH incr

Amiodarone hydrochloride is an anti-anginal agent and a class III antiarrhythmic drug that inhibits potassium channels (including wild-type hERG channels and their tail currents, with an IC₅₀ of approximately 45 nM) as well as voltage-gated sodium channels. This leads to prolonged action potential duration in ventricular and atrial myocytes, resulting in reduced heart rate and vascular resistance. It activates ERK1/2 and p38 MAPK signaling pathways in fibroblasts, promoting cell proliferation and myofibroblast differentiation. Amiodarone hydrochloride is widely used in the study of supraventricular and ventricular arrhythmias and can also be used to establish pulmonary fibrosis animal models.

Glipizide (CP 28720) is a short-acting, second-generation sulfonylurea with hypoglycemic activity.

Paxilline is an indole alkaloid mycotoxin from *Penicillium paxilli*, acting as a potent BK channel inhibitor via an almost exclusively closed-channel block mechanism. Paxilline possesses significant anticonvulsant activity.

Glisoxepide is a sulphonamide derivative and is an orally available nonselective K(ATP) channel blocker. It has antihyperglycemic activity and cardiovascular regulation effect.

Y-26763 is a K+ channel opener and active metabolite of Y-27152. This is an ATP-sensitive K+ (KATP) channel activator.

SKP-451 is an ATP-sensitive potassium (K+) channel agonist. It activates ATP-sensitive K+ channels, promoting the efflux of K+, leading to membrane hyperpolarization and inhibiting Ca2+ influx, which results in the relaxation of vascular smooth muscle. SKP-451 relaxes canine coronary arteries, rabbit basilar arteries, and vertebral arteries. Additionally, SKP-451 lowers mean arterial blood pressure in conscious spontaneously hypertensive rats (SHR). It holds potential for cardiovascular disease research.

Mitiglinide (KAD-1229) is an insulinotropic agent that is an ATP-sensitive K + (K ATP ) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K ATP channel). Mitiglinide is able to be used for the research of type 2 diabetes [1] [2].

Cromakalim (BRL 34915) is an ATP-dependent K(+) channel opener and a smooth muscle relaxant.Cromakalim has antiepileptic and anticonvulsant activity and may be useful in studies of asthma and disorders associated with vasodilation.

MCC-134 is an inverse agonist for the pancreatic-type ATP-sensitive K(+) channel. It also used as a vascular relaxing agent.

Iptakalim, 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. Iptakalim is also a K(ir) 6.1/SUR2B activator that can attenuate hypoxia-induced pulmonary arterial hypertension in rats by endothelial function protection.

KR-31378, a K(ATP) channel activator, is used potentially for the treatment of ocular hypertension and glaucoma.

Tilisolol is a nonselective blocker of beta-adrenergic. Tilisolol hydrochloride dilates coronary arteries through an ATP-sensitive K(+)-channel opening mechanism in dogs.

ZD-0947, a K(ATP) channel activator, is used potentially for the treatment of overactive bladder (OAB).

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

5-Hydroxydecanoate sodium is a selective ATP-sensitive K+ (KATP) channel blocker with an IC50 of approximately 30 μM and a substrate for mitochondrial outer membrane acyl-CoA synthetase, possessing antioxidant properties.

BMS 180448 is a prototype mitochondrial ATP-sensitive K+ (Mitok (ATP)) channel opener with cardioprotective and vasodilating properties.

Guanosine 5'-diphosphate (GDP) is a purine nucleotide and biosynthetic precursor of guanosine 5'-triphosphate .1It has been used to study the conformations of GTPases.2GDP (100 μM) activates sulfonylurea receptor 2B (SUR2B) linked to the inward-rectifier potassium channel 6.1 (Kir6.1) in HEK293T cells in a patch-clamp assay.3 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Biochemistry(2002) 2.Vetter, I.R., and Wittinghofer, A.The guanine nucleotide-binding switch in three dimensionsScience294(5545)1299-1304(2001) 3.Yamada, M., Isomoto, S., Matsumoto, S., et al.Sulphonylurea receptor 2B and Kir6.1 form a sulphonylurea-sensitive but ATP-insensitive K+ channelJ. Physiol.499(Pt 3)715-720(1997)