Epilepsy

Kojic amine is an orally active γ-aminobutyric acid (GABA) analog. Kojic amine acts as a GABA mimic that inhibits sodium-independent [³H]GABA binding to rat brain cell membranes. Kojic amine reduces flexor spasms in chronic spinal rat and cat models. Kojic amine prevents tonic extensor convulsions in mice. Kojic amine produces a transient, dose-dependent analgesic effect in the mouse hot-plate test. Kojic amine can be used in research related to skeletal muscle spasm, epilepsy and analgesia^[1][2]

E0714 is a blood-brain barrier-permeable, selective Kv7.2 potassium channel activator, with EC₅₀ values of 1.90 μM and 0.021 μM for homotetrameric Kv7.2 channels and heterotetrameric Kv7.2/7.3 channels, respectively. E0714 exhibits anticonvulsant activity. E0714 can be used in research related to epilepsy.

Tetrantoin (Spirodon) is a spirocyclic hydantoin and anticonvulsant with an approximate ED₅₀ of 54 mg/kg.Tetrantoin inhibits and prevents convulsions induced by maximum electric shock test.Tetrantoin can be used for the research of epilepsy.

Ro 48-8587 is a selective AMPA receptor antagonist with an IC₅₀ of 8 nM. Ro 48-8587 functionally inhibits AMPA receptor activity, blocks AMPA-induced depolarization of rat cortical wedges. Ro 48-8587 can be used for the research of ischaemia and seizures.

CHF-2993 is an orally active anticonvulsant. CHF-2993 antagonizes Bicuculline (HY-N0219)- and Picrotoxin (HY-101391)-induced tonic convulsions in mice, shows no activity against Pentylenetetrazole-induced clonic convulsions in mice, and partially reduces Veratridine (HY-N6691)-induced aspartate efflux in rat cortical synaptosomes. CHF-2993 can be used in the research of epilepsy.

SePP is a blood-brain barrier-permeable NMDAR antagonist and dopamine/norepinephrine reuptake inhibitor, with a K_i of 28.7 nM for rat NMDAR. SePP exerts anticonvulsant effects. SePP can be used in research related to fragile X syndrome.

Abz-GFDPFRQ-EDDnp is a fluorogenic substrate for metallothionein oligopeptidase (λ_ex=320 nm, λ_em=420 nm). Abz-GFDPFRQ-EDDnp is used to determine the enzymatic activity of metallothionein oligopeptidase in tissue extracts and for research on temporal lobe epilepsy.

Naringenin 4',7-dimethyl ether, Naringenin (HY-N0100) derivative is an anti-seizure agent. Naringenin 4',7-dimethyl ether attenuates pentylenetetrazole-induced seizures in larval zebrafish and reduces seizures in the mouse 6-Hz psychomotor seizure model. Naringenin 4',7-dimethyl ether can be used for the research of epilepsy. Naringenin 4',7-dimethyl ether is an active agent against Leishmania mexicana (17.8 µM) and Trypanosoma brucei (17.5 µM).

TPH2 agonist-1 (compound 20e) is an orally active, blood-brain barrier permeable, 1,3,4-oxadiazol-2 (3H)-one-derived TPH2 agonist. TPH2 agonist-1 upregulates TPH2 expression, elevates 5-HT and GABA levels, and exhibits antiepileptic activity in SCN1A-deficient models. TPH2 agonist-1 stabilizes the electrophysiological activity of neuronal networks and inhibits abnormal spike and burst activities. TPH2 agonist-1 shows no significant hERG inhibition or cytotoxicity, and it can be used in studies related to severe myoclonic epilepsy of infancy (Dravet syndrome).

GABAA receptor modulator-13 is an orally active, blood-brain barrier-permeable α₄β₁δ GABA_A receptor modulator (IC₅₀ = 9.02 μM). GABAA receptor modulator-13 reduces GABA-induced currents, impairs the stability of the transmembrane domain M2-M3 loop of α₄β₁δ GABA_A receptors, and exhibits selectivity for γ₂-containing GABA_A receptor subtypes and α₆β₃δ GABA_A receptor subtypes. GABAA receptor modulator-13 is applicable to the research of nervous system diseases with altered tonic inhibition, such as neurodevelopmental disorders and epilepsy.

CAI-IN-6 (Compound 3F) is a carbonic anhydrase (CAI) inhibitor with a K_i of 902.1 nM against hCA I and a K_i of 86.1 nM against hCA II. CAI-IN-6 can be used for the research of diuresis, glaucoma, epilepsy, tumors, and other conditions.

Qingyangshengenin 3-O-β-D-cymaropyranosyl-(1→4)-β-D-digitoxopyranoside is a natural steroid.

(±)-U-50488 ((±)-trans-(1R,2R)-U-50488) is a selective kappa opioid receptor agonist. (±)-U-50488 can improve symptoms related to status epilepticus, but has no significant effect on spontaneous seizure episodes. (±)-U-50488 can be used for research of epilepsy.

CM304 free base (FTC-146) is a potent S1R antagonist. CM304 free base enhances the antinociceptive effects of the cannabinoid receptor agonists. CM304 free base inhibits convulsions in rats.

Fenimide is an antipsychotic agent. Fenimide shows sedative, anticonvulsant and anesthetic activity. Fenimide has also prevented formation of stress-induced gastric lesions in the rat.

Nicotinanilide (N-Phenylnicotinamide) (Compound 12) is an aquaporin 4 (AQP4) inhibitor. Nicotinanilide can be used for research on diseases associated with AQP4 dysfunction, such as epilepsy and migraine.

CAII-IN-12 (compound 6c) is a potent and selective carbonic anhydrase (CA) II and VII inhibitor (hCA II K_i = 47.8 nM, hCA VII K_i = 3.6 nM) with anti-epilepitic activity. CAII-IN-12 displays selectivity over hCA I (K_i = 370 nM). CAII-IN-12 exhibits potent anticonvulsant activity in both Pentylenetetrazol- and Pilocarpine (HY-B0726A)-induced seizure mouse models. CAII-IN-12 increases expression of KCC2 in the hippocampus, maintains neuronal integrity, and reduces mTOR activity. CAII-IN-12 can be used for epilepsy research.

(-)-Norfenfluramine (l-Norfenfluramine) is a Fenfluramine metabolite. (-)-Norfenfluramine effectively counteracts the zebrafish abnormal locomotor activity. (-)-Norfenfluramine can be used in epilepsy research.

(Rac)-UCB-J (Compound 23) is a ligand for synaptic vesicle protein 2A (SV2A), with a pIC₅₀ value of 8.2. (Rac)-UCB-J can be used as a PET tracer for SV2A to assist in the diagnosis of epilepsy research.

LY456236 free base is a selective, non-competitive and orally active antagonist of glutamate receptor 1 (mGlu1), which can inhibit phosphatidylinositol hydrolysis with an IC₅₀ of 0.145 μM. LY456236 free base can also inhibit EGFR, with an IC₅₀ of 0.918 μM. LY456236 free base blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A). LY456236 free base can be used in epilepsy research.