anticonvulsant effects

DPDPE is selective δ-opioid receptor agonist peptide. Inhibits electrically stimulated contraction of mouse vas deferens in vitro (EC50 = 5.2 nM), and is antinociceptive in vivo.

(2R,4R)-APDC, a selective group II metabotropic glutamate receptors (mGluRs) agonist, exhibits anticonvulsant and neuroprotective effects.

Fluzinamide (AHR-8559) has anticonvulsant effects on ignited amygdala seizures.

γ-Aminobutyric acid belongs to natural products and functions as an agonist of GABAA and GABAB receptors, possessing central sedative effects, cell permeability, and the ability to modulate neuronal excitability. This compound is used in neuroscience research and exhibits anxiolytic, anticonvulsant, and neuroprotective activities.

3-Diethylamino-1-propanol exhibits anticonvulsant effects.

Phenprobamate (MH 532) is a relaxant that acts on central skeletal muscle and has anticonvulsant and psychostimulant effects.

Epoxylinalool (2-(2-Hydroxy-2-Propyl)-5-Methyl-5-Vinyltetrahydrofuran) is a naturally occurring monoterpene alcohol widely used in the production of perfumes and flavors.

Etifoxine hydrochloride (HOE 36-801 hydrochloride) is an anxiolytic and anticonvulsant drug. Unlike benzodiazepines, Etifoxine hydrochloride appears to produce its anxiolytic effects by binding to β2 and β3 subunits of the GABAA receptor complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines.

DCG-IV is an effective agonist of class II mGluR. DCG-IV has anticonvulsant and neuroprotective effects. The EC50 of mGlu2R and mGlu3R are 0.35 and 0.09 μM, respectively. DCG-IV is also a competitive antagonist of Group I (IC50: mGlu1 / 5R = 389/630 μM) a

N6-Cyclohexyladenosine (CHA) is a selective agonist of A1 receptor with EC50 of 8.2 Nm. N6-Cyclohexyladenosine exerts anticonvulsant effects and protects against neuronal death. CHA was also found to inhibit the pressor effects of lumbar sympathetic nerve stimulation in rats.

ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 is a potent and orally active KCNQ2/Q3 potassium channel opener (EC50: 0.38 μM). ICA-27243 also has antiepileptic and anticonvulsant effects.

LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with > 100 μM for mGlu5a, LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis.

Ciheptolane, a derivative of spirodibenzocycloalkanedioxalane, exhibits multiple pharmacological activities including analgesic, sedative, antihistamine, antiserotonin, anti-inflammatory, anticonvulsant, and antidepressant effects.

Profexalone is a derivative of oxazolidinone, exhibiting multiple pharmacological activities such as anticonvulsant, muscle relaxant, antidepressant, anti-inflammatory, and analgesic effects.

Clotizolam is a thienotriazolodiazepine derivative with PAF antagonistic properties, exhibiting sedative, anxiolytic, anticonvulsant, and muscle relaxant effects.

3-Methylnordiazepam (RO-5-2751) is a benzodiazepine compound that exhibits anticonvulsant effects in mice.

Nitrazolam is a benzodiazepine compound that may exhibit central nervous system depressant properties similar to traditional benzodiazepine drugs by acting on the GABA receptors (GABA receptor). These effects include sedation, hypnosis, anxiolytic, and anticonvulsant activities.

Anticonvulsant agent 10 (Compound 6d) is an inhibitor targeting the Keap1-Nrf2 interaction, with a strong activity showing an ED50 of 0.04 mmol/kg. By inhibiting the Keap1-Nrf2 binding, it activates the Nrf2/ARE pathway, providing anticonvulsant and neuroprotective effects, making it useful for research in epilepsy and neuroprotection.

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.

Kv7.2/Kv7.3 activator-2 is a blood-brain barrier-penetrating activator of Kv7.2/Kv7.3 channels with an EC50 of 0.25 μM. This compound exhibits excellent photostability and demonstrates potent anticonvulsant effects in acute epilepsy mouse models induced by maximal electroshock (MES) and sc-pentylenetetrazol (sc-PTZ).

Carbonic anhydrase inhibitor32 (compound 5B) is an orally active, selective inhibitor of hCA (carbonic anhydrase) II/VII, with Ki values of 6.3 nM for hCA II, 10.1 nM for hCA VII, and 681 nM for hCA I. It shows potential for neuroprotection and anticonvulsant effects by reducing mTOR activation and increasing hippocampal KCC2 levels.

AMPA-IN-2 is an orally effective AMPA inhibitor capable of crossing the blood-brain barrier. By suppressing intrinsic neuronal excitability and inhibiting glutamatergic transmission excitability, AMPA-IN-2 alleviates seizures. In the pentylenetetrazol (PTZ) model, it demonstrates anticonvulsant effects, positioning it as a promising candidate with high broad-spectrum antiepileptic potential.

mGluR2 modulator6 (Compound 25-a) acts as an mGluR2 modulator demonstrating anticonvulsant activity in the 6Hz epilepsy model, with enhanced effects when used in combination with Levetiracetam. This compound is valuable for epilepsy research.

Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active activator of Kv7.2/Kv7.3 channels and the TSPO. It activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). This compound protects motor neurons from degeneration caused by exposure to astrocyte-conditioned media from mice and humans with amyotrophic lateral sclerosis/frontotemporal dementia. Additionally, Kv7.2/Kv7.3 activator-3 stimulates axonal growth in dorsal root ganglia through TSPO and Kv7.2/3 activation and exhibits anticonvulsant effects in epilepsy models. It alleviates hyperalgesia in diabetic neuropathy patients, enhances the survival and regeneration of neurons after cervical neuropathy in rats, and accelerates the recovery of normal function in sensory and motor neurons.