kainate receptor

Dasolampanel (NGX-426) 是一种可口服的离子型谷氨酸受体 AMPA 和 Kainate 受体拮抗剂，可用于研究慢性疼痛疾病，包括神经性疼痛和偏头痛。

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。

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

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。

cis-PDA (cis PDA) 是一种通用的离子型受体拮抗剂。 cis-PDA 通过阻断 NMDA、AMPA 和红藻氨酸介导的反应发挥作用。

GYKI 52466 dihydrochloride (GYKI 52466 2HCl) 是一种具有良好的血脑屏障通透性、口服活性和选择性的 AMPA Kainate 受体拮抗剂，具有抗惊厥活性，可用于研究帕金森和癫痫等神经系统疾病。

Fanapanel（ZK200775,法那帕奈）是一种喹草胺二酮衍生物和高效的AMPAR的竞争性拮抗剂，可用于脑血管相关研究。

(S)-Willardiine (L-willardiine) 存在于金合欢和含羞草的种子中。 (S)-Willardiine 是一种 AMPA 红藻氨酸受体激动剂 (EC50 = 44.8 μM)。

LY382884 是一种具有选择性和有效性的 GLU(K5)受体拮抗剂，具有抗焦虑活性。LY382884可阻断阻断苔藓纤维LTP的诱导。

IEM 1754 2HBr (IEM 1754 dihydrobromide) 是一种选择性 AMPA 红藻氨酸受体阻滞剂，作用于 GluR1 和 GluR3，IC50 为 6 μM。

DNQX disodium salt 是一种选择性、强竞争性的非 NMDA 谷氨酸受体 (non-NMDA glutamate receptor) 拮抗剂 (对 AMPA、kainate 和 NMDA 受体的 IC50分别为 0.5、2 和 40 μM)，是一种喹恶啉衍生物。

CP 465022 hydrochloride 是强效的、选择性的AMPA 受体非竞争性拮抗剂，具有抗惊厥活性。CP 465022 hydrochloride 在大鼠皮层神经元中抑制Kainate 诱导的反应 (IC50= 25 nM)。

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。

GluR5-subunit containing kainate receptor antagonist

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]

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。

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.

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).

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.

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。

NMDA and AMPA/kainate receptor antagonist

NS 3763 is a kainate receptor antagonist.

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