Epilepsy

JNJ-61432059 is a blood-brain barrier-permeable, orally active TARP γ-8-associated AMPAR modulator with anticonvulsant activity. JNJ-61432059 negatively regulates GluA1 and positively modulates GluA2-containing AMPARs. JNJ-61432059 exerts potent protective effects in rodent epilepsy models. JNJ-61432059 is applicable for epilepsy-related research.

Sodium bromide (NSC 77384; Sanibrom 40) is a GABA-ergic system modulator that crosses the blood-brain barrier, and it effectively reduces and blocks epileptiform discharges. Sodium bromide exerts significant anticonvulsant effects by enhancing GABA-ergic inhibitory functions, such as increasing the amplitude of inhibitory postsynaptic currents and paired-pulse inhibition. Sodium bromide specifically enhances stimulation-induced extracellular alkalosis without affecting baseline pH or subsequent acidosis processes. Sodium bromide exhibits species-specific pharmacokinetic characteristics, competes with chloride ions for renal tubular reabsorption sites, and serves as a marker for extracellular fluid volume. Sodium bromide can be used in the research of epilepsy and related neurological diseases.

Avizafone (Pro-diazepam) dihydrobromide, a pro-drug of Diazepam, is an anticonvulsant agent. Avizafone dihydrobromide can be used as an antidote of nerve agent poisoning. In vivo, Avizafone dihydrobromide is rapidly hydrolyzed by aminopeptidase to produce lysine and diazepam. Avizafone dihydrobromide has research areas including neurological disease, such as epilepsy.

JW-65 is a selective TRPC3 channel inhibitor with favorable blood-brain barrier penetration. JW-65 directly binds to human TRPC3 protein and modulates calcium signaling to reduce seizure susceptibility. JW-65 reduces seizure incidence, severity, and duration while prolonging seizure latency in multiple seizure models. JW-65 alleviates Aβ‑induced neuronal damage. JW-65 serves as a valuable tool for research on epilepsy, seizure disorders, and Alzheimer’s disease.

CZL55 is a caspase-1 inhibitor. CZL55 can be used for the research of febrile seizures (FS).

Sclareol glycol is a blood-brain barrier-permeable, reversible adenylate cyclase (AC) activator. Sclareol glycol induces dose-dependent changes in body temperature, regulates convulsive seizures and spontaneous activity. Sclareol glycol interacts with GABAergic transmission, thereby affecting dopamine-related behaviors. Sclareol glycol can be used in studies related to convulsive seizures, aggressive responses, thermoregulation, etc.

Dipropofol is a dimeric derivative of Propofol (HY-B0649) with antioxidant and antibacterial activities. Dipropofol terminates free radical chain reactions, scavenges DPPH free radicals and inhibits lipid peroxidation. Dipropofol protects cells from death induced by glutamate, Aβ(25-35) and buthionine sulfoximine, and increases the survival rate of mice exposed to oxygen. Dipropofol selectively activates tonic GABAA currents, hyperpolarizes resting membrane potential, reduces action potential firing, and alleviates the severity of seizures induced by Kainic acid. Dipropofol can be used in the research of Gram-positive bacterial infections, Alzheimer's disease, cerebral ischemia-related neuronal injury, oxygen toxicity and temporal lobe epilepsy.

Dihydralazine sulfate is an antihypertensive hydrazine derivative and also a low-potency genotoxic agent. Dihydralazine sulfate is a direct-acting mutagen with a mixed gene mutation mechanism, which induces DNA fragmentation in the lung, kidney and spleen of mice, and induces sister chromatid exchange in mouse bone marrow cells. Dihydralazine sulfate specifically kills DNA repair-deficient bacteria. Dihydralazine sulfate is a vasodilator and antihypertensive agent that reduces systemic vascular resistance, increases cardiac output and heart rate, thereby lowering blood pressure. Dihydralazine sulfate can be used in research related to hypertension and severe early-onset preeclampsia.

Laniquidar is a non-competitive P-gp inhibitor with an IC₅₀ of 0.51 μM. Laniquidar binds to the P-gp transporter with high affinity and exhibits low activity as a substrate. Laniquidar is applicable to epilepsy-related research.

(R)-Safinamide (FCE 28073) is the enantiomer of Safinamide (HY-70057). (R)-Safinamide is an orally active, alanine-derived monoamine oxidase inhibitor with an IC₅₀ of 1.77 μM for rat MAO-B and an IC₅₀ of 50 μM for rat MAO-A. (R)-Safinamide regulates the activity of monoamine oxidase isoforms in brain homogenates. (R)-Safinamide is used in epilepsy research.

Carbonic anhydrase isoenzyme is an isoform of Carbonic anhydrase (HY-P1775). Carbonic anhydrase isoenzymes are a class of widely distributed metalloenzymes that catalyze the reversible hydration-dehydration reaction of the carbon dioxide-bicarbonate system, and also exhibit acetaldehyde hydration and ester hydrolysis activities. Carbonic anhydrase isoenzyme is associated with epithelial ion transport processes involving sodium, potassium, anions, and ammonia. Carbonic anhydrase isoenzyme can be used in research on cancer, glaucoma, obesity, and epilepsy.

(R)-Nimodipine ((R)-BAY-e 9736) is an orally active, blood-brain barrier-permeable L-type calcium channel blocker with an IC₅₀ of 5 nM. (R)-Nimodipine inhibits corticosterone release by blocking calcium channels on the hypothalamic-pituitary-adrenal axis, thereby reversing immobilization stress-induced memory impairment and behavioral abnormalities. (R)-Nimodipine is widely used in studies related to aneurysmal subarachnoid hemorrhage, cerebral ischemia, epilepsy, age-related degenerative neurological diseases, and alcohol intoxication.

(R)-Amino-N-benzyl-3-methoxypropionamide is a key intermediate for the synthesis of the antiepileptic agent (R)-Lacosamide. To improve its chiral purity and chemical stability, (R)-Amino-N-benzyl-3-methoxypropionamide can react with phosphoric acid to form a phosphate salt. Detected by high performance liquid chromatography (HPLC), this phosphate salt exhibits extremely high chiral purity, with the content of the R-enantiomer reaching up to 99.37%.

Isopimaric acid is a coniferous tree defense compound. Isopimaric acid binds to AKT and inhibits mTOR phosphorylation, thereby regulating the AKT/mTOR pathway. Isopimaric acid inhibits oxidative stress, inflammation, microglial migration, apoptosis, autophagic flux, ornithine decarboxylase activity, breast cancer proliferation and metastasis, and fungal spore germination. Isopimaric acid also induces M2 microglial polarization, mitochondrial damage, ROS accumulation, starvation-induced colon cancer cell apoptosis, and breast cancer cell cycle arrest. Isopimaric acid activates potassium channels, regulates sodium channels and calcium channels, reduces myocardial excitability, and improves arrhythmia. Isopimaric acid acts as an oxidative substrate for CYP6BW1/3, down-regulates PINK1/Parkin, and regulates calcium homeostasis, oxidative phosphorylation, EMT, and the Wnt pathway. Isopimaric acid exhibits activity against drug-resistant Staphylococcus aureus, repels feeding, and promotes the growth of rice seedlings. Isopimaric acid is suitable for research related to epilepsy, tumors, drug-resistant bacterial infections, atrial fibrillation, hypertension, hyperlipidemia, pulmonary tuberculosis, etc.

Methsuximide (Mesuximide) is an orally active succinimide-derived antiepileptic agent. Methsuximide interacts with cytochrome P-450, increases the level of hepatic microsomal cytochrome P-450, and inhibits or competes with the cytochrome P-450 CYP 2C9/10 subtype. Methsuximide can be used in epilepsy-related research.

L-Aspartic acid disodium (disodium L-aspartate) is a NMDA receptor agonist and acidic amino acid. L-Aspartic acid disodium has no independent analgesic activity. L-Aspartic acid disodium can antagonize the analgesic effects of D-Aspartic acid and Morphine. L-Aspartic acid disodium regulates polymorph transformation, crystal growth/aggregation and nucleation processes of calcium carbonate, and can serve as a biomineralization template. L-Aspartic acid disodium promotes burst firing of central neurons. L-Aspartic acid disodium can be used in studies related to cerebral ischemia and epilepsy.

Hydantoin is an imidazolidine-2,4-dione and serves as the parent nucleus of the antiepileptic agent Phenytoin (HY-B0448).

Murine Thrombin is a murine serine protease that plays a central role in blood coagulation. Murine Thrombin stimulates macrophages to polarize into a unique phenotype characterized by anti-inflammatory and pro-repair properties. Murine Thrombin activates PAR1, induces the production of MCP-1, MMP3 and VEGF in mouse intervertebral discs, and causes degradation of the cartilage matrix and destruction of intervertebral disc structure. Murine Thrombin activity increases significantly in paraoxon-induced status epilepticus.

Quinpirole (LY 171555; (-)-LY 141865) is a D2/D3 dopamine receptor agonist and a CaV1.3 calcium channel modulator. Quinpirole normalizes dendritic spine density in dopamine-depleted striatum, upregulates the protein expression of BCL2 and GluR2, downregulates the protein expression of BAX, and delays the onset of seizures. Quinpirole enhances learning and memory, inhibits neuronal apoptosis (apoptosis), and induces anxiety-like, stereotyped, and compulsive behaviors. Quinpirole disrupts prepulse inhibition in rhesus monkeys, enhances the activity of paraventricular thalamic neurons to promote recovery from Isoflurane anesthesia, and alters the composition of the gut microbiota in rats. Quinpirole can be used in research related to dyskinesia, pain, epilepsy, and neurological disorders including anxiety disorder, obsessive-compulsive disorder, and schizophrenia.

(E)-KN-93 phosphate is a Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) inhibitor with IC₅₀ values of 9 μM and 3 μM against CaMKIIδ_Monomer and CaMKIIδ_Dodecamer, respectively. (E)-KN-93 phosphate can be used in research on epilepsy, depression, and arrhythmias..