kainate

AMPA/kainate antagonist-2 acts as a non-competitive antagonist of AMPA/kainate receptors.

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.

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

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

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

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

DNQX (FG 9041) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.5 and 0.1 μM for AMPA and kainate receptors, respectively)

L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice.

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)

Topiramate lithium (McN 4853) is a wide-ranging antiepileptic compound with GluR5 receptor antagonistic properties. Its mechanism of action involves enhancing GABAergic activity, inhibiting kainate/AMPA receptors, voltage-sensitive sodium and calcium channels, and increasing potassium conductance. Additionally, this compound inhibits carbonic anhydrase. [1][2][3]

Topiramate (RWJ 17021) is a unique antiseizure medication that is used in the treatment of partial and generalized seizures. Topiramate has been rarely associated with hepatic injury and largely when used in combination with other anticonvulsant medications.

GluR5-subunit containing kainate receptor antagonist

CNQX (FG9065) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.3 and 1.5 μM for AMPA and kainate receptors, respectively)

L-Glutamic acid-15N is the 15N-labeled version of L-Glutamic acid, an excitatory neurotransmitter and an agonist at metabotropic, kainate, NMDA, and AMPA glutamate receptor subtypes. It directly activates the release of dopamine (DA) from dopaminergic terminals.

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

EGIS-8332 is a potent and selective non-competitive AMPA receptor antagonist. EGIS-8332 inhibits AMPA/kainate ion channels and cell death. EGIS-8332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA- and quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons (IC(50)=5.1-9.0 microM), in vitro. EGIS-8332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimental disease models, and on its low side effect potential.

AMPA and kainate receptor antagonist

NBQX, also known as FG9202, is an AMPA receptor antagonist. NBQX blocks AMPA receptors in micromolar concentrations (~10–20 µM) and also blocks kainate receptors. In experiments, it is used to counter glutamate excitotoxicity. NBQX was found to have anticonvulsant activity in rodent seizure models. As the disodium salt, NBQX is soluble in water at high concentrations (at least up to 100 mM).

Fanapanel hydrate is a highly selective antagonist of AMPA/kainate with little activity against NMDA(Ki of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively).

Fanapanel is a highly selective AMPA/kainate antagonist with little activity against NMDA. It also has Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.

NS 3763 is a kainate receptor antagonist.

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.

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

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

NMDA and AMPA/kainate receptor antagonist

UBP310 (UBP 310) is a GLUK5 kainate receptor antagonist

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.

hGluR5 kainate receptor agonist

LY339434 is a potent and selective agonist of the kainate receptor GluK1, GluR5.

GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of generalized tonic-clonic seizures induced by 4-aminopyridine (4-AP) when administered at doses of 25 and 50 mg/kg. GYKI 52466 (30 mg/kg) prevents neuronal damage in the CA1 region of the hippocampus in a rat model of global ischemia-reperfusion injury induced by four-vessel occlusion.

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

N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM). It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors. CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.

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.

CP-465022 Maleate is a potent, selective, noncompetitive AMPA receptor antagonist with anticonvulsant activity. It effectively counters the Kainate-induced response in rat cortical neurons, exhibiting an IC 50 of 25 nM. As such, CP-465022 Maleate presents a valuable instrument for studying the involvement of AMPA receptors in various physiological and pathophysiological processes [1] [2].

UBP301 is a kainate receptor antagonist.

RAD-140-Q (RAD-140) is a selective androgen receptor modulator that inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action. RAD-140-Q is neuroprotective in cultured neurons and kainate-lesioned

GluR5-containing kainate receptor antagonist

GYKI 52466 dihydrochloride is orally active and non-competitive kainate- and AMPA-activated currents antagonist (IC50s: 7.5 μM and 11 μM). It is inactive against NMDA or γ-aminobutyric acid responses. It is a muscle relaxant and anticonvulsant agent and h

L-Glutamic acid (Glutaminol) acts as an excitatory transmitter, shows a direct activating effect on the release of DA from dopaminergic terminals.

DL-Willardiine (2-amino-3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)propanoic acid) is an unnatural amino acid, a derivative of glutamate. It is an agonist of mGluR5, which regulates the activity of enzymes involved in neurotransmitter synthesis and catabolism, and affects the activity of ion channels and other membrane proteins.

L-Glutamic-5-14C acid is a bioactive chemical.

D-Glutamic acid ((R)-Glutamic acid), the enantiomer of L-glutamic acid, is widely used in medicine and food.

DL-Glutamic acid, monohydrate is a useful organic compound for research related to life sciences. The catalog number is T125469 and the CAS number is 19285-83-7.

L-Glutamic acid monosodium salt (MSG) (Monosodium glutamate) is an activator of mGlu1 receptor.