convulsions

Vamicamide (FK 176) is a novel anticholinergic compound. Vamicamide increases spontaneous locomotor activity in mice at 32 mg kg (p.o.) or higher and inhibits cataleptic convulsions in mice at 100 mg kg.

(S)-Vamicamide is a novel anticholinergic compound.Vamicamide increases spontaneous locomotor activity in mice at 32 mg kg or higher (p.o.) and inhibits tonic convulsions in mice at 100 mg kg.13483-86-1

L-Allylglycine is an amino acid derivative that reduces glutamate decarboxylase (GAD) activity by 60% when administered at a dose of 39.8 μmol g per hour ex vivo in mouse brain preparations. L-Allylglycine (1.2 mmol kg, i.p.) induces convulsions and decreases GABA concentration throughout the cerebellum, pons, medulla, striatum, cortex, and hippocampus in mice. Chronic administration (3.2 μg 0.5 μl per hour for 13 days) of L-allylglycine in rats increases locomotor activity in an open field test and impairs attention in the 5-choice serial reaction time task (5CSRTT). In vitro, L-allylglycine inhibits GAD only when used at high concentrations (1-80 mM). The more potent in vivo activity can be attributed to metabolic conversion of L-allylglycine to 2-keto-4-pentanoic acid, a more potent convulsant and GAD inhibitor.

Nefiracetam (DM9384) are underway in Phase 2 trials. Nefiracetam, a GABAergic, cholinergic,and monoaminergic neuronal system enhancer, is used for Ro 5-4864-induced convulsions.

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

Modaline was a 2-methyl-3-piperidinopyrazine derivative found to inhibit monoamine oxidase (MAO) and showed a curative effect for the anti-depressant. Similar to other MAO inhibitors, it enhanced convulsions induced by tryptamine and hyperthermia induced

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.

UMB24 is an effective antagonist of the σ2 receptor, exhibiting dissociation constants (Ki values) of 170 nM for the σ2 receptor and 322 nM for the σ1 receptor. This compound mitigates cocaine-induced convulsions and hyperactivity without causing mortality.

(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).

DL-AP7, a competitive NMDA antagonist and anticonvulsant, blocks NMDA-induced convulsions and impairs learning performance in mice during a passive avoidance task [1].

high affinity agonist of the translocator protein

Allylglycine is a glutamate decarboxylase inhibitor and a GAMMA-AMINOBUTYRIC ACID antagonist. It is used to induce convulsions in experimental animals.

LY 81067 is a new anticonvulsive compound that effectively protects against pentylenetetrazole- and picrotoxin-induced convulsions in mice. It exerts its anticonvulsant effects by binding to or near picrotoxin binding sites.

Samandarine is the main steroidal alkaloid secreted by the fire salamander (Salamandra salamandra). The compound is extremely toxic and causes convulsions, respiratory paralysis, and eventual death.

ML 297 is a selective Kir3.1 3.2 (GIRK1 2) channel activator (IC50 values are 160, 887 and 914 nM for GIRK1 2, GIRK1 4 and GIRK1 3 respectively). ML 297 exhibits no effect on GIRK2, GIRK2 3, Kir2.1 and Kv7.4 channels, and has minimal effect on a panel of other ion channels, receptors and transporters.

Xanthine amine congener (XAC) hydrochloride, a non-selective adenosine receptor antagonist, induces convulsions in mice.

Hexylcaine HCl also called cyclaine or osmocaine, is a short-acting local anesthetic. It acts by inhibiting sodium channel conduction. Overdose can lead to headache, tinnitus, numbness and tingling around the mouth and tongue, convulsions, inability to breathe, and decreased heart function.

DDPM-2571 is a highly potent and in vivo active inhibitor of GABA transporter subtype 1 with anticonvulsant, anxiolytic, antidepressant and antinociceptive properties. DDPM-2571 was quickly distributed into the brain and was highly effective in the prevention of chemically-induced seizures (pentylenetetrazole and pilocarpine models) and 6-Hz convulsions. It demonstrated significant anxiolytic-like and antidepressant-like properties. DDPM-2571 had antinociceptive properties, both in the hot plate test and in the second phase of the formalin test.

PF05020182 is novel potent and selective Kv7.2 4 potassium channel opener. PF-05020182 (2) significantly inhibits convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 support further development as an adjunctive treatment of refractory epilepsy. Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in controlling spontaneous electrical activity during epileptic seizures.

Pifexole is the 1,2,4-oxadiazole derivative. It has a similar profile of muscle-relaxant activity in animals to that of chlorzoxazone. In rats, pifexole is reported to be seven times more potent than chlorzoxazone in inhibition of strychnine-induced convulsions.

Bicuculline methobromide, a selective GABAA Receptor antagonist with an IC50 value of 3 μM, induces tonic-clonic convulsions in mammals and blocks Ca2+ activated potassium channels. It is applicable in researching epilepsy and related psychiatric disorders.

Bicuculline methochloride ((+)-Bicuculline; d-Bicuculline), a selective GABAA receptor antagonist, exhibits an IC50 of 3 μM. It induces tonic-clonic convulsions in mammals and blocks Ca2+ activated potassium channels, making it useful for studying epilepsy and related psychiatric disorders [1] [2].

Polyphyllin H can be extracted from loblolly pine and rhizomes, has antitumor activity, and is used in studies of inflammation, fractures, and convulsions.

Isopulegol presents depressant- and anxiolytic-like effects, it also has anticonvulsant and bioprotective effects against PTZ-induced convulsions are possibly related to positive modulation of benzodiazepine-sensitive GABAA receptors and to antioxidant properties.Isopulegol presents significant gastroprotective effects in both ethanol- and indomethacin-induced ulcer models, which appear to be mediated, at least in part, by endogenous prostaglandins, K(ATP) channel opening, and antioxidant properties.