potentials

4F 4PP oxalate 是一种选择性5-HT2A 拮抗剂。

Saclofen 是竞争性GABAB 受体拮抗剂(IC50:7.8 μM)。它可研究 GABAB 受体调节大脑中缓慢抑制性突触后电位的功能。

Helichrysetin 是从豆蔻果实中分离出的一种天然产物，是一种 DNA 结合抑制剂，可抑制原位导管癌DCIS 的形成。它抑制细胞生长，可诱导 A549 细胞凋亡。

Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。

UCL 2077 是癫痫相关 KCNQ 通道的亚型选择性阻滞剂，也是一种选择性慢后超极化通道阻滞剂，在培养的海马神经元中 IC50 为 500 nM，对 Ca2+ 通道、动作电位、输入电阻的影响小 ，以及超极化后的介质。

NMDAR antagonist 2 (compound 3I) 作为一种具有血脑屏障通透性的NMDAR拮抗剂，在hGluN1 hGluN2A的膜电位为-60 mV时的IC50值为4.42 μM，在40 mV时为214.75 μM。此外，该化合物能有效减轻海马损伤。

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。

Rovatirelin（亦称为S-0373）是一种新型合成化合物，其作用模仿甲状腺释放激素（TRH）。该化合物对人类TRH受体的亲和力（Ki=702nM）高于taltirelin（Ki=3877nM）。在大鼠蓝斑区（LC）急性分离的去甲肾上腺素神经元中，Rovatirelin能增加自发动作电位的发放。此外，Rovatirelin亦能增加运动活动。Rovatirelin可能作为口服治疗，对SCD患者具有潜在的治疗效果。

gamma-DGG TFA 是一种兴奋性氨基酸拮抗剂，能够阻断由 NMDA-、Kainate- 和 Quisqualate- 诱导的去极化，并在大鼠海马切片中对兴奋性突触后电位 (e.p.s.p.) 产生拮抗作用。

Risotilide is a voltage-dependent potassium channel inhibitor. It can prolong cardiac action potentials and refractory periods.

AHR-12234 affects cardiac action potentials.

Chlordene, as a polychlorinated flame retardant, has bioaccumulation and biomagnification potentials.

Ro 67-7476 是mGluR1的正变位调节剂，能增强表达 rat mGluR1a 的 HEK293 细胞中谷氨酸诱导的钙释放，EC50为 60.1 nM。它是 P-ERK1 2 激动剂，可以在没有外源添加谷氨酸的情况下激活 ERK1 2 磷酸化 (EC50=163.3 nM)。

Brevetoxin B is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. It binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50 = 15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively. Brevetoxin B is ichthyotoxic at nanomolar concentrations and is responsible for an illness described as neurotoxic shellfish poisoning.

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg kg, respectively). Zonisamide (40 mg kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

Ajmaline hydrochloride is an alkaloid found in the root of Rauwolfia serpentina, and other plant sources. It is a class of Ia antiarrhythmic agent that apparently works by changing the shape and threshold of cardiac action potentials.

Vasicine 是一种分离自Justicia adhatoda 中的喹唑啉类生物碱。它具有抗结核作用。

CT1-3 是一种有效的抗癌剂。CT1-3 能够调控 JNK Bcl-2 Bax XIAP 通路，进而诱导线粒体介导的细胞凋亡 (apoptosis)。CT1-3 可以调控 E-cadherin Snail 轴抑制人癌细胞 (HCCs) 的上皮间充质转化 (EMT) 电位，并抑制肿瘤发生。CT1-3 在小鼠模型中具有抗肿瘤作用，且没有表现出明显的肝、肾毒性。

Moricizine Hydrochloride (EN 313) 是一种口服具有活力的 I 类抗心律失常剂。Moricizine Hydrochloride 能够减少 0 相去极化的速率；提高 2 相和 3 相复极率，降低动作电位持续时间，减少有效不应期。

Asocainol hydrochloride ia an antiarrhythmic drug which inhibits slow Ca2+ influx. This is accompanied by alterations in normal Na+-carried action potentials. Therefore, Asocainol not only inhibits Ca2+ inflow but also interferes with the fast inward Na+ current.

Phenytoin-d10 is intended for use as an internal standard for the quantification of phenytoin by GC- or LC-MS. Phenytoin is an anticonvulsant agent and active metabolite of fosphenytoin. Phenytoin is formed from fosphenytoin by tissue phosphatases. It inhibits neuronal voltage-gated sodium channels in a voltage-dependent manner. Phenytoin reduces the neuronal firing frequency and decreases the amplitude of excitatory post-synaptic potentials (EPSPs) in electrically stimulated rat corticostriatal slices. It protects against seizures induced by maximal electroshock (MES) in mice. Formulations containing phenytoin have been used in the treatment of tonic-clonic seizures and status epilepticus.

ProTx-II TFA是选择性作用于Nav1.7钠通道的阻滞剂，具有0.3 nM的IC50值，选择性比其他钠通道亚型高出至少100倍。该化合物抑制钠离子通道，通过减少通道电导及使激活电压向更正的电位移动，从而阻断痛觉感受器中动作电位的传导。

Lotusine (hydroxide)为纯生物碱，源自Nelumbo nucifera Gaertn绿色种胚提取。该化合物能够影响心肌动作电位和心脏浦肯野纤维的缓慢内向电流。

CaMKIIα-PHOTAC是一种靶向Ca2+ 钙调蛋白依赖性蛋白激酶IIα（CaMKIIα）的光化学靶向嵌合体（PHOTAC）。该分子在特定波长光照射下实现靶蛋白的泛素化及通过蛋白酶体催化的降解。CaMKIIα-PHOTAC能在光照条件下显著降低小鼠海马区域的诱发LTP反应强度，减弱突触功能，并对维护亚细胞级别的树突结构域、长时程增强及记忆能力起到关键作用。