k+ currents

Cloperastine fendizoate (Hustazol) 是 hERG K+ 电流的抑制剂，IC50 为 27 nM。

8-Bromo-cGMP sodium 是一种 PKG 激活剂， 是 cGMP 的膜渗透性类似物。8-Bromo-cGMP sodium 具有缓解疼痛和血管舒张作用，可显着抑制 Ca2+ 宏观电流，抑制高 K+ 刺激的胰岛素释放。

Bisaramil hydrochloride (Bisaramil) 是一种新型二氮双环壬烷抗心律失常化合物，抑制自由基生成。Bisaramil hydrochloride 可阻断钠电流，抑制异丙肾上腺素在 K（+） 去极化肌上诱导的缓慢 Ca（2+） 动作电位。

Quinidine hydrochloride monohydrate 是一种抗心律失常剂，也是 K+通道 (K+channel) 的有效阻断剂，其IC50值为 19.9 μM。它是一种有效且选择性的细胞色素 P450db (cytochrome P450db) 抑制剂，也可用作疟疾的研究。

Verapamil (CP-16533-1) 是一种非二氢吡啶类钙通道阻滞剂，一种 P-gp 抑制剂，也是一种 CYP3A4 抑制剂，具有口服活性。Verapamil 可以用于治疗高血压、心绞痛、心肌梗塞等。

Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity (IC50: 3.3 nM). Zaldaride maleate is an effective and selective inhibitor of calmodulin. Zaldaride maleate prevents estrogen-induced transcription activation by ER, re

AUT2是一种Kv3.1通道调节剂，具有治疗FXS患者感觉过敏的潜力，通过将高阈值电流的激活转移到更负的电位上。此转变降低了高阈值K+电流，并增加了神经元中的低阈值K+电流，恢复了ABR的IV波。由于其调节神经元兴奋试活性的能力，AUT2还有望用于治疗听力障碍。

Doxapram (Dopram) 是一种呼吸兴奋剂，抑制 TASK-1，TASK-3 和 TASK-1 TASK-3 异二聚体通道，可用于研究早产儿呼吸暂停和慢性阻塞性肺疾病恶化引起的通气衰竭。

inhibitor of outward K+ currents

Tedisamil is a blocker of K+ currents in cardiac tissues, exerts bradycardic effects. It is an antiarrhythmic drug with predominantly class III activity. It has shown clinical efficacy in angina pectoris.

Nerispirdine is a acetylcholine release enhancer, sodium channel blocker and K(V) 2.1 channel blocker. Nerispirdine inhibits voltage-dependent Na(+) channel currents recorded from human SH-SY5Y cells with an IC(50) of 11.9 micromol L when measured from a

Water-soluble salt of lamotrigine . Displays anticonvulsant effects and inhibits glutamate release, possibly through inhibition of Na+, K+ and Ca2+ currents. Leach et al (1991) Neurochemical and behavioral aspects of lamotr. Epilepsia 32 S4 PMID:1685439 |Smith and Meldrum (1995) Cardioprotective effect of lamotr. after focal ischemia in rats. Stroke 26 117 PMID:7839380 |Zona and Avoli (1997) Lamotrigine reduces voltage-gated sodium currents in rat central neurons in culture. Epilepsia 38 522 PMID:9184596 |Grunze et al (1998) Modulation of calcium and potassium currents by lamotr. Neuropsychobiology 38 131 PMID:9778600

Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg kg twice daily.3 Alaproclate (40 mg kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988). Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg kg twice daily.3 Alaproclate (40 mg kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4 References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988).

N-Salicyloyltryptamine(STP) 是一种色胺类似物，具有抗惊厥、抗炎、镇痛和血管舒张的作用。N-Salicyloyltryptamine 作为电压依赖性离子通道（包括Na+、Ca2+、K+离子通道）抑制剂，可抑制 K+电流，IC50值为 34.6 μM ( to)。

Quinine hemisulfate hydrate，一种从金鸡纳树皮提取的生物碱，具有抗疟疾效果。作为钾离子通道 (potassium channel) 抑制剂，它能够抑制由电压脉冲触发的MT mSlo3 (KCa5.1) 通道在+100 mV下的电流活动，其IC50值达169 μM。

ShK toxin 是从加勒比海葵（Stichodactylu helianthus）的全身提取物中分离出的一种蛋白，能够阻断电压依赖性钾通道(Kv1.3 通道)。在竞争实验中，ShK toxin 与树突毒素 I 及α-树突毒素相互竞争，以与大鼠脑突触体膜结合，从而促进乙酰胆碱的释放。此外，ShK toxin 抑制培养的大鼠背根神经节神经元中的K+ 电流，并且能够抑制T淋巴细胞的增殖。

Tamapin为靶向小电导Ca(2+)激活的K(+) (SK)通道的毒液肽，尤以钾通道SK2为选择性阻断剂。该化合物能够抑制海马锥体神经元SK通道介导的电流，来源于印度红蝎(Mesobuthus tamulus)。

Tamapin TFA为靶向小电导Ca(2+)激活的K(+) (SK)通道的毒液肽，特异性抑制SK2（钾通道）并阻断海马锥体神经元中SK通道介导的电流。该化合物可从印度红蝎(Mesobuthus tamulus)毒液中提取。

VU 0546110 是一种针对精子特异性钾通道 SLO3 的选择性抑制剂（IC50= 64 μM），相较于 SLO1 显示出 40 倍的选择性。它能完全阻断异源性 SLO3 电流和内源性 K+ 电流。VU 0546110 抑制精子超极化并阻止其超活跃移动。

Guangxitoxin 1E acts as a gating modifier since it shifts the voltage-dependence of Kv2.1 K+ currents towards depolarized potentials.

Potent and selective μ opioid receptor antagonist (Ki values are 0.96 and >10,000 nM for μ and δ receptors respectively). Causes behavioral effects on central administration in vivo. Also increases K+ currents in rat locus ceruleus neurons in vitro via a

Melanostatin, frog TFA 是一种高效性的 α-黑素细胞刺激激素 (α-MSH) 释放抑制剂，是从青蛙大脑中分离出的一种 36 个氨基酸的肽，通过调节 K+、Na+ 和 Ca2+ 电流抑制青蛙黑素营养素的电活性。

(S)-(-)-Bay-K-8644 ((S)-(-)-Bay K 8644) 是 L 型 Ca2+ 通道的激动剂，可激活 Ba2+ 电流，其EC50 为 32 nM。

(R)-(+)-Bay-K-8644 是一种 Ca2+ 通道抑制剂，也能抑制 Ba2+电流 (IBa)，诱导猫的中枢性呼吸抑制，通过竞争性拮抗血栓素 A2-前列腺素 H2 受体抑制血小板活化。