kainate receptor

(S)-Willardiine (L-willardiine) is present in the seeds of Acacia and Mimosa. (S)-Willardiine is an AMPA/kainate receptor agonist (EC50 = 44.8 μM).

Dasolampanel (NGX-426) is an orally available ionotropic glutamate receptor AMPA and Kainate receptor antagonist for the study of chronic pain disorders, including neuropathic pain and migraine.

Memantine hydrochloride (Memantine HCl) is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.

GYKI 52466 dihydrochloride (GYKI 52466 2HCl) is a highly potent, orally active and selective AMPA/Kainate receptor antagonist with good blood-brain permeability and anticonvulsant activity that can be used to study neurological diseases such as Parkinson's and epilepsy.

SYM 2081 is a specific kainate receptor agonist with an IC50 value of 35 nM for [3H]-kainate binding. SYM 2081 depolarizes the muscle and reduces the EPSP amplitude.

cis-PDA (cis PDA) is a general ionotropic receptor antagonist. cis-PDA acts by blocking NMDA, AMPA, and kainate-mediated responses.

BPAM344 is a potent positive allosteric modulator (PAM) of the KAR subunits GluK1b, GluK2a, and GluK3a.

Fanapanel (ZK200775) is a quinoxalinedione derivative and potent competitive antagonist of AMPAR for cerebrovascular-related studies.

UBP301 is a potent and selective kainate receptor antagonist with an IC₅₀ of 164 μM and a Kd of 5.94 μM. Its selectivity for kainate receptors is 30-fold higher than that for AMPA receptors, and it is structurally classified as a sophorose amino acid derivative.

YM90K (6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-) hydrochloride is an antagonist of AMPA receptor.

CNQX disodium is a competitive non-NMDA receptor antagonist and competitive AMPA/kainate receptor antagonist in neuronal cultures.

LY382884 is a selective and potent GluR5 kainate receptor antagonist with anxiolytic activity.LY382884 blocks blockade of mossy fibre LTP induction.

IEM 1754 2HBr (IEM 1754 dihydrobromide) is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.

CP 465022 hydrochloride is a potent, and selective noncompetitive antagonist of AMPA receptor with anticonvulsant activity. CP 465022 hydrochloride inhibits Kainate-induced response with an IC50 of 25 nM in rat cortical neurons.

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg/kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg/kg and prevents memory deficits induced by the AMPA/kainate glutamate receptor antagonist NBQX at 0.1 mg/kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

DNQX disodium salt is a water-soluble form of selective antagonist of non-NMDA receptor

UBP 302 is an effective and selective GLUK5-subunit-containing kainate receptor antagonist (apparent Kd=402 nM) and displays very little affinity on GluK2 kainate receptors.

GYKI-52466 is a selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >50 μM for AMPA-, kainate- and NMDA-induced responses, respectively) used as a Skeletal muscle relaxant, orally active anticonvulsant, neuroprotective and

CP-465022 Maleate is a potent, selective, noncompetitive AMPA receptor antagonist with anticonvulsant activity, effectively countering the Kainate-induced response in rat cortical neurons with an IC50 of 25 nM, making it a valuable instrument for studying the involvement of AMPA receptors in various physiological and pathophysiological processes [1] [2].

GluR5-containing kainate receptor antagonist

NS 3763 is a kainate receptor antagonist.

AMPA receptor antagonist with weak activity at NMDA receptors and little activity at kainate receptors

NMDA and AMPA/kainate receptor antagonist

5-Iodowillardiine is a selective agonist for specific kainate receptor subunits that robustly activates GluK1 (GluR5) and GluK5 (KA2)-containing receptors while displaying minimal activity at AMPA receptors and no measurable agonism toward GluK2 (GluR6) subunits. Despite its excitotoxic neurotoxic activity in vivo, 5-Iodowillardiine remains a powerful experimental tool for dissecting kainate receptor subtype distribution, synaptic function, and excitatory neurotransmission in the brain and spinal cord.