kainic acid

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.

Generates large inward currents at resting membrane potential

(-)-(α)-Kainic Acid (hydrate) is an effective excitotoxic agent that acts as an agonist of ionotropic glutamate receptor subtypes, capable of inducing seizures and commonly used to establish animal models of epilepsy.

EAAT2(GLT1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake

NBQX disodium is a highly selective, competitive AMPA receptor antagonist with neuroprotective and anticonvulsant activity. NBQX disodium is a salt of NBQX. NBQX disodium is a potent and selective AMPA/rhodosinate receptor antagonist that can be used to antagonize the excitatory toxicity of glutamate. It has anticonvulsant effects in rodent models.

Domoic acid is a kainic acid analog.

GABAA receptor modulator-10 is an orally active and potent positive allosteric modulator (PAM) of the α1β2γ2GABAA receptor, exhibiting good blood-brain barrier permeability. It enhances the function of the α1β2γ2 GABAA receptor and increases GABA-induced currents. In mouse models of epilepsy induced by Pentetrazol (PTZ) and Kainic Acid (KA), GABAA receptor modulator-10 demonstrates strong antiepileptic efficacy. This compound shows potential for epilepsy research.

Irampanel hydrochloride (BIIR 561-CL) is an inhibitor of AMPA receptors and voltage-dependent sodium channels. It suppresses kainic acid-induced rat cortical neuronal currents.

Aspalatone is an anti-platelet aggregator (IC50 = 180 μM, in vitro) that prolongs bleeding time significantly in a rodent model of thromboembolism. Additionally at a minimal effective dose of 24 mg/kg, aspalatone generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy in rat hippocampus.

1. Decursin (Decursinol angelate) is able to attenuate kainic acid-induced seizures and could have potential as an antiepileptic drug. 2. Decursin exhibits hepatoprotective effects , potentially by inhibiting the TGF-β1 induced NOX activation and Smad signaling. 3. Decursin has anti-cancer activity , mediated suppression of the PKCα, MAPK and NF-κB pathways in MCF-7 cells. 4. Decursin exhibits cytotoxicity against various human cancer cells and to possess anti-amnesic activity in vivo through the inhibition of AChE activity.

(RS)-AMPA ((±)-AMPA) monohydrate, a potent and selective agonist of the excitatory neurotransmitter L-glutamic acid and a glutamate analogue, does not interact with the binding sites of kainic acid or NMDA receptors, highlighting its selectivity [1] [2].

Neuronotoxicity-IN-1 is a pyridothiazine derivative. Neuronotoxicity-IN-1 is an inhibitor of kainic acid neurotoxicity with neuroprotective activity[1].

3-ATA is a selective cyclin-dependent kinase 4 (Cdk4) inhibitor, attenuating kainic acid-induced apoptosis in neurons.

Compound 5c (Anticonvulsant agent 5) exhibits high affinity for GABAA receptors (GABAA receptor) and NaV1.3 receptors (NaV1.3 receptor). In the murine psychomotor seizure test, it demonstrated anticonvulsant activity with an ED50 of 107 mg/kg. Additionally, Compound 5c shows neuroprotective effects against Kainic acid with an IC50 of 113 μM and possesses blood-brain barrier (BBB) permeability.

Neuroprotectin B is a cyclic peptide that safeguards cultured chicken neurons from excitotoxicity induced by glutamate and kainic acid.

Neuroprotectin A (Complestatin A) is a cyclic peptide that safeguards cultured chicken brain neurons from excitotoxicity caused by glutamate and kainic acid.

S-(4-Hydroxybenzyl)glutathione was isolated as the major principle responsible for the inhibition of the in vitro binding of kainic acid to brain glutamate receptors by water extracts of the plant Gastrodia elata.