electroshock

Cyclamic acid sodium (Cyclohexylsulfamicacidsodium) is a carbonic anhydrase inhibitor and one of the most widely used artificial sweeteners in food and pharmaceuticals.Cyclamic acid sodium shows moderate anticonvulsant activity in a maximal electroshock convulsive seizure model.Cyclamic acid sodium is used in cancer research.

GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.

Lvguidingan is an Anticonvulsant agent.

Suclofenide is a benzenesulfonamide derivative that acts as an anticonvulsant and antiepileptic agent. In preclinical models, it showed potent anticonvulsant activity against electroshock and pentylenetetrazole-induced convulsions in mice. Sublethal toxicity was demonstrated by lethargy, myoclonic jerks and diarrhea.

(R)-AS-1 is a selective positive allosteric modulator of excitatory amino acid transporter 2 (EAAT2), with an EC50 of 11 nM. At doses of 60 and 90 mg kg, (R)-AS-1 enhances spontaneous locomotor activity in mice. It demonstrates anticonvulsant properties in mouse seizure models induced by maximal electroshock (MES), pentylenetetrazole (PTZ), or electric current stimulation (32 or 44 mA), with ED50 values of 66.3, 36.3, 15.6, and 41.6 mg kg, respectively. This compound is applicable in neurological disease research.

(S)-3-N-Cbz-Amino-succinimide (Compound 1d) is an antiepileptic agent that suppresses tonic convulsions in mice induced by pentylenetetrazole and maximal electroshock (MES).

Anticonvulsant agent 8 (compound D4) is a chemical used in treating epilepsy by inhibiting GABAA currents. In mouse models, its ED50 values are 2.23 mg kg for the maximal electroshock (MES) test and 24.60 mg kg for the pentylenetetrazol (PTZ) test.

Anticonvulsant agent 7 (Compound 19) is an orally active, broad-spectrum anticonvulsant demonstrating excellent anticonvulsant activity in the MES (maximum electroshock) and 6 Hz seizure models.

Carbamazepine 10,11-epoxide is an active metabolite of the anticonvulsant carbamazepine. It is formed by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C8 in microsomes from HepG2 cells expressing CYP3A4 or CYP2C8, respectively. Carbamazepine 10,11-epoxide exhibits anticonvulsant activity against maximal electroshock-induced seizures in mice and has been detected in wastewater effluent [1][2][3].

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, a derivative of the endogenous lipid amides (N-acylethanolamines), demonstrates anticonvulsant efficacy in electroshock-induced seizures in mice, exhibiting minimal toxicity [1].

Carbamazepine-10,11-epoxide-d10 (rings-d10) is a deuterated compound of Carbamazepine-10,11-epoxide. Carbamazepine-10,11-epoxide has a CAS number of 36507-30-9. Carbamazepine 10,11-epoxide is an active metabolite of the anticonvulsant carbamazepine[1][2].It is formed from carbamazepine by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C8 in microsomes prepared from HepG2 cells expressing CYP3A4 or CYP2C8, respectively[1].Carbamazepine 10,11-epoxide has anticonvulsant activity against maximal electroshock-induced seizures in mice.2It has been found in wastewater effluent[3].

Sodium cyclamate-d4 is a deuterated compound of Sodium cyclamate. Sodium cyclamate has a CAS number of 139-05-9. Cyclamic acid sodium is a carbonic anhydrase inhibitor and one of the most widely used artificial sweeteners in food and pharmaceuticals.Cyclamic acid sodium shows moderate anticonvulsant activity in a maximal electroshock convulsive seizure model.Cyclamic acid sodium is used in cancer research.