electroshock

GABAA receptor agent 1 是GABAA 受体的高亲和力配体，有抗惊厥活性。

Cyclamic acid sodium (Cyclohexylsulfamicacidsodium) 是一种碳酸酐酶抑制剂，是食品和药品中使用最广泛的人工甜味剂之一。Cyclamic acid sodium 在最大电休克惊厥发作模型显示出中等的抗惊厥活性。Cyclamic acid sodium 可用于研究癌症。

Lvguidingan 是一种抗惊厥药。

Suclofenide 是一种苯磺酰胺衍生物，可作为抗惊厥和抗癫痫剂。在临床前模型中，它对小鼠电击和戊四唑诱导的惊厥表现出强大的抗惊厥活性。亚致死毒性表现为嗜睡、肌阵挛抽搐和腹泻。

(R)-AS-1 是一种选择性激动性氨基酸转运体2 (EAAT2) 的正向异构调节剂，其EC50为11 nM。(R)-AS-1 以60和90 mg kg剂量显著增加小鼠的自发运动活动。在最大电休克 (MES)、戊四氮 (PTZ) 和电流刺激 (32或44 mA) 所引发的小鼠癫痫模型中，(R)-AS-1 显示出抗癫痫活性，ED50分别为66.3、36.3、15.6和41.6 mg kg。此化合物可应用于神经疾病的研究。

(S)-3-N-Cbz-Amino-succinimide (Compound 1d) 是一种抗癫痫化合物，能够抑制小鼠中由戊四氮 (pentylenetetrazole) 和最大电休克 (MES) 所引发的强直性惊厥。

抗癫痫剂 8 (compound D4) 为一种抗癫痫试剂，能有效抑制 GABAA 电流。在小鼠模型的最大电休克 (MES) 和戊四氮 (PTZ) 测试中，其 ED50 值为 2.23 mg kg 和 24.60 mg kg。

Anticonvulsant agent 7 (Compound 19) 是一种口服活性广谱抗惊厥剂，在MES (最大电休克) 和6 Hz癫痫模型中展现了卓越的抗惊厥活性。

Carbamazepine 10,11-epoxide 是抗惊厥药卡马西平 (carbamazepine) 的活性代谢物。它由卡马西平通过微粒体中的细胞色素 P450 (CYP) 同种型 CYP3A4 和 CYP2C8 形成，微粒体分别由表达 CYP3A4 或 CYP2C8 的 HepG2 细胞制备。它对小鼠电击诱发的癫痫发作具有抗惊厥活性。

5α-Androst-16-en-3α-ol is a steroid pheromone that has been found in boar testes and human male axillary sweat and has diverse biological activities.1,2It enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50= 0.4 μM).25α-Androst-16-en-3α-ol (0.1-1 μM) increases the amplitude of GABA-activated currents in HEK293 cells expressing human α1β2γ2and α2β2γ2subunit-containing GABAAreceptors.In vivo, 5α-androst-16-en-3α-ol (5-10 mg kg) decreases immobility time in the forced swim test in mice. It increases time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity, when administered at doses ranging from 30 to 50 mg kg. 5α-Androst-16-en-3α-ol protects against seizures induced by pentylenetetrazole or electroshock in mice (ED50s = 48.9 and 21.9 mg kg, respectively). 1.Brooksbank, B.W., Brown, R., and Gustafsson, J.A.The detection of 5α-androst-16-en-3α-ol in human male axillary sweatExperientia30(8)864-865(1974) 2.Kaminski, R.M., Marini, H., Ortinski, P.I., et al.The pheromone androstenol (5α-androst-16-en-3α-ol) is a neurosteroid positive modulator of GABAA receptorsJ. Pharmacol. Exp. Ther.317(2)694-703(2006)

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).

2-(Isopentylamino)naphthalene-1,4-dione is a vitamin K analog.1It inhibits spasms induced by pentylenetetrazole and tonic hindlimb extension induced by maximal electroshock (MES) in mice (ED50s = 349.2 and 108.1 mg/kg, respectively). It also protects mice against seizures in the 6 Hz psychomotor seizure test (ED50s = 152.7 and 263.7 mg/kg at stimulus intensities of 32 and 44 mA, respectively). 1.Li, X., Himes, R.A., Prosser, L.C., et al.Discovery of the first vitamin K analogue as a potential treatment of pharmacoresistant seizuresJ. Med. Chem.63(11)5865-5878(2020)

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.

Methazolamide-d6 is intended for use as an internal standard for the quantification of methazolamide by GC- or LC-MS. Methazolamide is a carbonic anhydrase inhibitor. It reduces intraocular pressure and cerebrospinal fluid flow in a rat model of glaucoma. Methazolamide reduces electroshock-induced seizures in rats with an ED50 value of 19.2 mg kg. It also inhibits production of reactive oxygen species (ROS) in a primary cortical neuron (PCN) cellular model of subarachnoid hemorrhage (SAH) and reduces cerebral edema in a mouse model of SAH.3 Methazolamide is larvicidal, with a 50% larvicidal concentration (LC50) value of 724 ppm, but has no activity when administered in the diet to adult A. aegypti. Formulations containing methazolamide have been used in the treatment of glaucoma.

Pentadecanoyl ethanolamide，一种N-acylethanolamine的内源性脂质酰胺衍生物，对电击休克的小鼠展现出抗惊厥效果，同时无明显毒性。

Carbamazepine-10,11-epoxide-d10 (rings-d10) 是 Carbamazepine-10,11-epoxide 的氘代化合物。Carbamazepine-10,11-epoxide 的 CAS 号为 36507-30-9。Carbamazepine 10,11-epoxide是抗惊厥药卡马西平 (carbamazepine) 的活性代谢物。它由卡马西平通过微粒体中的细胞色素 P450 (CYP) 同种型 CYP3A4 和 CYP2C8 形成，微粒体分别由表达 CYP3A4 或 CYP2C8 的 HepG2 细胞制备。它对小鼠最大电击诱发的癫痫发作具有抗惊厥活性。

Sodium cyclamate-d4 是 Sodium cyclamate 的氘代化合物。Sodium cyclamate 的 CAS 号为 139-05-9。Cyclamic acid sodium是一种碳酸酐酶抑制剂，是食品和药品中使用最广泛的人工甜味剂之一。Cyclamic acid sodium在最大电休克惊厥发作模型显示出中等的抗惊厥活性。Cyclamic acid sodium可用于研究癌症。