opener

Rilmakalim is a potassium channel opener. Rilmakalim shows antivasoconstrictor effect.

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

Aprikalim (RP 52891) is an adenosine triphosphate potassium channel (KATP) opener that protects against nerve damage in a rabbit model of spinal cord ischemia.Aprikalim inhibits vasoconstriction and inhibits the elevation of [Ca2+]i during myocardial paralysis, and can be used to study cardiovascular disease.

Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener.

SG 209 is an analog of nicorandil and acts as a K+ channel opener and nitrate-free coronary vasodilator.

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

NS 11021 (NS11021) , a novel opener of large-conductance Ca(2+)-activated K(+) channels

ICA 110381 is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy

Foslevcromakalim (QLS-101), an ATP-sensitive potassium channel opener, serves as a proagent for ocular hypotensive effects [1] [2].

ICA-105665 (PF-04895162) is a potent and orally active opener of neuronal Kv7.2 7.3 and Kv7.3 7.5 potassium channels. ICA-105665 had low cytotoxic potential in human hepatocytes but inhibited liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the central nervous system (CNS) and has antiseizure effects [1][2][3][4].

Flupirtine HCl is the salt form of Flupirtine, also known as W-2964, an aminopyridine that functions as a centrally acting non-opioid analgesic. It first became available in Europe in 1984, and is sold mainly under the names Katadolon, Trancolong, Awegal, Efiret, Trancopal Dolo, and Metanor. Like nefopam, it is unique among analgesics in that it is a non-opioid, non-NSAID, non-steroidal centrally acting analgesic. Flupirtine is a selective neuronal potassium channel opener that also has NMDA receptor antagonist and GABAA receptor modulatory properties.

PF05020182 is novel potent and selective Kv7.2/4 potassium channel opener. PF-05020182 (2) significantly inhibits convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 support further development as an adjunctive treatment of refractory epilepsy. Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in controlling spontaneous electrical activity during epileptic seizures.

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.

ZM 226600 is an ATP-sensitive potassium channel opener with an EC50 value of 500 nM. ZM226600 has an inhibitory effect on spontaneous bladder activity.

Flupirtine-d4 (D 9998-d4) hydrochloride, the deuterium-labeled version of Flupirtine (D 9998) hydrochloride, is a selective neuronal potassium channel opener with NMDA receptor antagonist properties [1] [2].

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

Y-27152 is a prodrug of the KATP (Kir6) channel opener Y-26763 and is a long-acting K+ channel opener.

QO-58 is a Kv7 channel opener with EC50 values of 7.0, 1.0, 5.2, 0.6 μM for Kv7.1, Kv7.2, Kv7.3/7.5, Kv7.4 respectively. QO-58 increases the pain threshold of neuropathic pain in a sciatic nerve CCI in vivo.

Flupirtine (D 9998) is a selective neuronal potassium channel opener and exhibits properties of an NMDA receptor antagonist.

NC00075159 is an opener of human KCNQ4 (Kv7.4) potassium channel.

KCO-912 is a potent and selective opener of ATP-dependent potassium (K ATP) channels. KCO-912 suppresses airways hyperreactivity at doses devoid of cardiovascular effects.

Naminidil is an opener of cyanoguanidine KATP.

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.

Ro 31-7837 is an opener of potassium channel.

ZM 260384 is a potassium channel opener.

NS004 is a large-conductance K+ channel opener, it inhibits mitochondrial function in glioma cells.

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

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

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).

ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 is a potent and orally active KCNQ2/Q3 potassium channel opener (EC50: 0.38 μM). ICA-27243 also has antiepileptic and anticonvulsant effects.

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.

TREK1 and TREK2 channel activator (EC50 = 0.76 μM in Rb efflux assay in TREK1-expressing CHO cells). Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Hyperpolarizes membrane potential of dorsal root ganglion neurons and depresses neuronal activity in vitro. Loucif et al (2018) GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. Br.J.Pharmacol. 175 2272 PMID:29150838