potassium channel activator 1

Potassium Channel Activator 1 可用于治疗多巴胺能系统被破坏的疾病或病症的研究，例如情绪障碍 ADHD、精神分裂症和其他精神病状态。

KCNQ1 activator-1 是有效的 KCNQ1通道激活剂。它在研究长 QT 综合征中有研究的价值。

BL-1249 是一种具有选择性和有效性的非甾体钾通道激活剂，具有抗炎活性，可激活 K2P2.1 (TREK-1) 和 K2P10.1 (TREK-2)。

17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases in the spontaneous beating of NRCMs.3,4 1.Schwarz, D., Kisselev, P., Ericksen, S.S., et al.Arachidonic and eicosapentaenoic acid metabolism by human CYP1A1: Highly steroselective formation of 17(R), 18(S)-epoxyeicosatetraenoic acidBiochem. Pharmacol.67(8)1445-1457(2004) 2.Lauterbach, B., Barbosa-Sicard, E., Wang, M.H., et al.Cytochrome P450-dependent eicosapentaenoic acid metabolites are novel BK channel activatorsHypertension39(2 Pt. 2)609-613(2002) 3.Falck, J.R., Wallukat, G., Puli, N., et al.17(R),18(S)-Epoxyeicosatetraenoic acid, a potent eicosapentaenoic acid (EPA) derived regulator of cardiomyocyte contraction: Structure-activity relationships and stable analoguesJ. Med. Chem.54(12)4109-4118(2011) 4.Arnold, C., Markovic, M., Blossey, K., et al.Arachidonic acid-metabolizing cytochrome P450 enzymes are targets of omega-3 fatty acidsJ. Biol. Chem.285(43)32720-32733(2010)

Loureirin B 是从剑叶龙血树中分离到的一种黄酮，是 PAI-1抑制剂，IC50值为 26.10 μM。它抑制 KATP，以及 ERK 和 JNK 的磷酸化，具有抗糖尿病的功效。

Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B Kir6.2 over the SUR2A Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 = 4.4 µM). It decreases mean blood pressure, coronary resistance, and heart rate, as well as increases coronary sinus outflow, in dogs when administered intravenously at a dose of 1 mg kg. Nicorandil increases survival and decreases infarct size in a rabbit model of myocardial ischemia-reperfusion injury induced by left coronary artery occlusion. Formulations containing nicorandil have been used in the treatment of angina pectoris.

Ebio1, 选择性电压门控钾通道KCNQ2激活剂, 于饱和电压(+50 mV)下通过产生具有更大电导率的扩展通道门，激活KCNQ2。

KCNQ2 3 activator-1 是Kv7.2 Kv7.3(KCNQ2 3) 钾通道激活剂，详细信息来自专利 WO2021113757A1的化合物 A。