channel modulator

KCa2 channel modulator 1 (compound 2o) 是有效的亚型选择性的K Ca 通道的正调节剂，其增强大鼠 KCa2.2 通道亚型的EC50值为 0.99 μM 和人KCa2.3 通道亚型的EC50值为 0.19 μM。

KCa2 channel modulator 2 (compound 2q) 是有效的亚型选择性KCa2通道的正调节剂，对人KCa2.3 通道和大鼠 KCa2.2 通道亚型显示出相似的效力，EC50值分别为 0.6 μM 和 0.64 μM。

Calcium channel-modulator-1是钙离子通道调节剂(IC50:0.8 μM)，具有阻塞主动脉收缩的专业化。

Kv3 modulator 1 是一种电压门控钾通道 Kv3 调节剂，可用于研究神经系统级疾病。

SAK3 是一种新型的 nAChR 活性调节剂，可增强 T 型电压门控 Ca2+ 通道 (T-VGCC) 的活性，对 Cav3.1 和 Cav3.3 T 型 Ca2+ 通道电流均有增强作用。SAK3 对人神经母细胞瘤 SH-SY5Y 细胞中东莨菪碱诱导的胆碱能功能障碍有神经保护作用。SAK3 可用于研究记忆缺陷和阿尔茨海默病。

GAL-021新型静脉内BKCa-channel 阻滞剂。

Niguldipine Free Base is a calcium channel blocker and a₁-adrenergic receptor antagonist and a clinical modulator of multidrug resistance.

HC-056456 (3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide) 是一种有效但不完全选择性的 CatSper 通道阻断剂。它能够减慢 [Na+]i 上升(IC50:3 µM)。

Flindokalner (BMS-204352) 是一种钾离子通道调节剂。它是大电导钙激活 K 通道正向调节剂。它是在 HEK293 细胞中表达的所有神经元 Kv7通道亚型的正调节剂。它在 Kv7.1 通道 (Ki=3.7 μM) 处显示负调节活性，并充当 GABAA 受体的负调节剂。它在体内显示出抗焦虑功效。

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。

AP30663是一种KCa2通道的负向异构调节剂。

D3 5-HT receptor modulator-1 (compound 5i) 是一种具有选择性抑制多巴胺D3受体和5-HT2A受体的拮抗剂，同时也是部分激动5-HT1A受体的化合物。该化合物对多巴胺D3、5-HT2A和5-HT1A受体的Ki值分别为4.5 nM、11.9 nM和15.3 nM。相比之下，它对多巴胺D2受体、5-HT2C受体和hERG通道的亲和力较低，具有非典型抗精神病特性。

Kv7.2/Kv7.3 modulator-2 (compound 7d) 是一种 Kv7.2/Kv7.3 调节剂，具有打开 Kv7.2/3 通道活性，pEC50 值为 7.42。Kv7.2/Kv7.3 modulator-2 适用于癫痫、抑郁、脑损伤及疼痛的研究。

P-gp modulator-7（Compound 9e）是一种P-糖蛋白（P-gp）抑制剂。它通过其独特的T形结构占据P-gp通道入口，阻碍TM12和TM9跨膜结构域的蠕动挤出机制，从而抑制P-gp将药物泵出细胞，以此逆转肿瘤细胞的多药耐药性（MDR）。P-gp modulator-7 有望用于癌症研究。

Lifarizine methanesulfonate is a modulator of sodium-calcium channel that reduces ischemic brain damage.

BDF 9148, a Na(+)-channel modulator, increases the contractile force of guinea-pig atria and papillary muscles.

PZ-II-029 是 α6β3γ2 选择性 GABAA 通道的调节剂。

VU0405601是KV11.1通道的高效药理激活剂，通过hERG激动作用保护心肌组织免受多非利特（Dofetilide）等hERG抑制剂诱发的心律失常与室性心动过速。

Dexmecamylamine( TC-5214, NIH-11008) is used as a nicotinic channel modulator with antidepressant activity.

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

KCa2 (small conductance Ca2+-activated potassium) channel negative allosteric modulator (IC50 = 1.1 μM). Increases the EC50 of Ca2+ on KCa2.3 channels by ~3-fold. Prolongs atrial effective refractory period (AERP) in rats. Reduces atrial fibrillation (AF) duration and prolongs atrial refractoriness without affecting ventricular refractory period in an animal AF model. Diness et al (2017) Termination of vernakalant-resistant atrial fibrillation by inhibition of small-conductance Ca2+-activated K+ channels in pigs. Circ.Arrhythm.Electrophysiol. 10 e005125 PMID:29018164 |Simó-Vicens et al (2017) A new negative allosteric modulator, AP14145, for the study of small conductance calcium-activated potassium (KCa2) channels. Br.J.Pharmacol. 174 4396 PMID:28925012

AP14145 hydrochloride is a potent negative allosteric modulator of K Ca 2 (SK) channels, specifically targeting K Ca 2.2 (SK2) and K Ca 2.3 (SK3) channels with an IC 50 of 1.1 μM. Inhibition of AP14145 hydrochloride is highly influenced by S508 and A533 amino acids present in the channel. This compound effectively extends the atrial effective refractory period (AERP) in rats and exhibits antiarrhythmic properties in a Vernakalant-resistant porcine model of atrial fibrillation (AF).

SK3 Channel-IN-1 (compound 7a) is a powerful and selective modulator of the SK3 channel. It demonstrates significant efficacy in inhibiting breast cancer MDA-MB-435 cell migration while maintaining low cytotoxicity in other cell lines. Furthermore, SK3 Channel-IN-1 exhibits the ability to modulate ion channel activity in cancer cells [1].

Azidopine is a photoactive dihydropyridine channel blocker which may also act as a multidrug resistant (MDR) modulator.