seizure

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing [hGlyT1a].

(RS)-(Tetrazol-5-yl)glycine is a potent and selective N-methyl-D-aspartate (NMDA) receptor agonist that can induce seizure models and Fos expression in mice. Its EC50 values for GluN1/GluN2D and GluN1/GluN2A are 99 nM and 1.7 μM, respectively.

Penicillamine (Artamine), possessing antineoplastic properties, induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. Artamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, Artamine chelates with heavy metals and increases their urinary excretion.

Kainic acid is an excitatory amino acid receptor agonist (EC50=16.2 μM). Kainic acid is an effective excitatory toxic agent. Kainic acid induces epileptic seizures.

CFM-2, a potent and selective non-competitive antagonist of AMPAR (AMPAR), exhibits anticonvulsant activity across various seizure models.

Inflachromene (ICM) is an inhibitor of HMGB1 and HMGB expression with anti-inflammatory activity.Inflachromene reduces seizure severity in a mouse model of epilepsy by inhibiting HMGB1 translocation, inhibits endothelial proliferation through the HMGB1/2-regulated TLR4-NF-κB pathway, and inhibits autophagy by regulating Beclin 1 activity. Inflachromene can be used to study epilepsy.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Clidinium bromide (Ro 2-3773) , a synthetic anticholinergic agent, has been shown in experimental and clinical researchers to have a pronounced antisecretory and antispasmodic effect on the gastrointestinal tract. It can inhibit muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites. It is used for the treatment of peptic ulcer disease and also to help relieve cramps or stomach spasms or abdominal due to colicky abdominal diverticulitis, pain, and irritable bowel syndrome.

Phenytoin (5,5-Diphenylhydantoin) is a hydantoin derivative and a non-sedative antiepileptic agent with anticonvulsant activity. It potentially acts by promoting sodium efflux from neurons in the motor cortex, reducing post-tetanic potentiation at synapses. This prevents cortical seizure foci from spreading to adjacent areas and stabilizes the threshold against hyperexcitability. Additionally, it appears to reduce muscle spindle sensitivity to stretch, causing muscle relaxation.

Rufinamide (E 2080), a triazole derivative, is used as voltage-gated sodium channel blocker for the treatment of seizure disorders.

3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.

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.

D-Leucine ((R)-Leucine) potently terminates seizures even after the onset of seizure activity. D-leucine reduces long-term potentiation but had no effect on basal synaptic transmission in vitro.

(E)-3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) is a natural compound derived from the roots and rhizomes of Notopterygium incisum.

Qingyangshengenin B (Otophylloside B) is a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic and anti-aging effects, it can extend lifespan, increase heat stress-resistance, delay body paralysis, and increase the chemotaxis response in C. elegans models of Alzheimer's disease. Otophylloside B can suppress the seizure-like locomotor activity caused by pentylenetetrazole in zebrafish.

L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, demonstrating over 280-fold selectivity compared to other growth inhibitory receptors. L-803087 induces AMPA-mediated synaptic responses in the hippocampus in vitro and increases seizures in alginate-induced seizure-busting mice in vivo.

Lvguidingan is an Anticonvulsant agent.

4-Deoxypyridoxine (4-DPD) is a vitamin B6 antimetabolite with diverse biological activities. It inhibits transport of pyridoxine , pyridoxal, and pyridoxamine in and reduces growth of S. carlsbergensis cells. 4-DPD inhibits sphingosine-1-phosphate (S1P) lyase and reduces cyclic stretch-induced apoptosis in alveolar epithelial MLE-12 cells. 4-DPD (5 mg, i.p.) reduces lysyl oxidase activity by 26% and reduces collagen and elastin crosslinking, resulting in limb abnormalities in chick embryos. It decreases latency to first seizure in mice (ED50 = 1 mmol kg) and increases the occurrence and duration of myoclonic responses in baboons with photosensitive epilepsy. 4-DPD reduces TNF-α and IL-6 production in mice infected with T. spiralis.

Talampanel (LY-300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptor antagonist with anti-seizure activity. Talampanel (IVAX) has neuroprotective effects in rodent stroke models.

Z944 is a T-type calcium channel antagonist with potential applications in pain management. In both epileptic and non-epileptic rats, Z944 disrupts prepulse inhibition. Additionally, it corrects cross-modal sensory and visual recognition memory deficits in Strasbourg genetic absence epilepsy rats. In a neuropathic pain rat model, Z944 restores cortical synchrony and thalamocortical connectivity. In the amygdala kindling model, it delays seizure progression.

(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.

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.

Nav1.2-IN-1 (compound 5i) is a 3-(1,2,3,6-tetrahydropyridine)-4-azaindole derivative that acts as a potent and selective Nav1.2 inhibitor. It effectively reduces the peak current of Nav1.2 with an IC50 of 7.79 μM. Nav1.2-IN-1 demonstrates antiepileptic activity and shows strong anticonvulsant effects with low neurotoxicity in a subcutaneous pentylenetetrazol (sc-PTZ) induced seizure model.