kainate receptors

SYM 2081 是一种特异性红藻氨酸受体激动剂，对 [3H]-红藻氨酸结合的 IC50 值为 35 nM。 SYM 2081 使肌肉去极化并降低 EPSP 振幅。

Memantine hydrochloride (Memantine HCl) 是一种具有一些多巴胺能作用的金刚烷胺衍生物，是一种温和的 NMDA 受体非竞争性拮抗剂，能够抑制 CYP2B6 和 CYP2D6。它可作为抗帕金森剂。

Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。

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.

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].

AMPA receptor antagonist with weak activity at NMDA receptors and little activity at kainate receptors.This compound is unstable in powder form and other related salt forms are recommended.

UBP310 (UBP 310) 是选择性GluR5拮抗剂，Kd 值为 130 nM。

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.

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.

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]

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).

CNQX (FG9065) 是一种竞争性、非 NMDA 谷氨酸受体拮抗剂，对 AMPA 和红藻氨酸受体的IC50分别为 0.3 和 1.5 μM。

DNQX (FG 9041) 是喹恶啉衍生物，是一种选择性和强竞争性的非 NMDA 谷氨酸受体拮抗剂，对 AMPA、kainate 和 NMDA 受体的IC50分别为 0.5、2 和 40 μM。

CNQX disodium 是一种有效的、竞争性的 AMPA 海藻酸酯受体 (AMPA kainate receptor) 拮抗剂，IC50分别为 0.3 μM 和 1.5 μM。它能够阻止大鼠恐惧增强的表达，是一种竞争性的非 NMDA 受体拮抗剂。

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

BPAM344 是一种红藻氨酸受体亚基GluK1b、GluK2a 和GluK3a 的正变构调节剂。