iGluR(离子型谷氨酸受体)
iGluR (ionotropic glutamate receptor) is a ligand-gated ion channel that is activated by the neurotransmitter glutamate. iGluR are integral membrane proteins compose of four large subunits that form a central ion channel pore. Sequence similarity among all known glutamate receptor subunits, including the AMPA, kainate, NMDA, and δ receptors.
AMPA receptors are the main charge carriers during basal transmission, permitting influx of sodium ions to depolarise the postsynaptic membrane. NMDA receptors are blocked by magnesium ions and therefore only permit ion flux following prior depolarisation. This enables them to act as coincidence detectors for synaptic plasticity. Calcium influx through NMDA receptors leads to persistent modifications in the strength of synaptic transmission.
Products for iGluR
- Cat.No. 产品名称 Information
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GC45776
LY404187
N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺
A positive allosteric modulator of AMPA receptors -
GC37821
Transcrocetin meglumine salt
trans-Crocetin meglumine salt
A natural apocarotenoid with diverse biological activities -
GC37703
Sunifiram
桑尼菲拉姆; DM-235
An Analytical Reference Standard -
GC37612
SDZ 220-581 Ammonium salt
(S)-ALPHA-氨基-2'-氯-5-(膦酰甲基)-[1,1'-联苯]-3-丙酸单铵盐
SDZ 220-581铵盐是NMDA谷氨酸受体竞争性拮抗剂。 -
GC36876
Perzinfotel
EAA-090
Perzinfotel (EAA-090) 是一种有效选择性的,竞争性的 NMDA 受体拮抗剂,具有神经保护作用。Perzinfotel (EAA-090) 对谷氨酸位点显示出高亲和力 (IC50=30 nM)。 -
GC36865
PEAQX tetrasodium hydrate
NVP-AAM077 tetrasodium hydrate
PEAQX (NVP-AAM077) is an effective and orally available human NMDA antagonist, which shows preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over hNMDA 1A/2B receptors (IC50=29,600 nM). -
GC36515
LY450108
N-[4-[(1R)-1-甲基-2-[[异丙基磺酰基]氨基]乙基]苯基]-3,5-二氟苯基甲酰胺
LY450108是AMPA受体增强剂。 -
GC36510
LY3130481
LY3130481 是一种跨膜 AMPA 受体调节蛋白 TARP γ-8 依赖性的 AMPA 受体拮抗剂,选择性抑制 AMPA/TARP γ-8 的 IC50 值为 65 nM。
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GC36411
Kynurenic acid sodium
Kynurenic acid sodium 是一种内源性色氨酸代谢物,是针对靶点 NMDA, glutamate, α7 nicotinic acetylcholine receptor 的光谱性拮抗剂。Kynurenic acid sodium 也是 GPR35/CXCR8 的激动剂。
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GC36060
Flupirtine
氟吡汀,D 9998
An activator of Kv7 channels -
GC36027
Fanapanel hydrate
ZK200775 hydrate; MPQX hydrate
Fanapanel hydrate (ZK200775 hydrate) 是高选择性AMPA拮抗剂。 -
GC35918
Dynorphin A 1-10
Dynorphin A (1-10) 是一种内源性的阿片样神经肽,与 κ 阿片受体 (κ-opioid receptor) 结合。Dynorphin A (1-10) 也阻断 NMDA 激活的电流,IC50 为 42.0 μM。
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GC35917
Dynorphin A (1-10) TFA
Dynorphin A (1-10) (TFA) 是一种内源性的阿片样神经肽,与 κ 阿片受体 (κ-opioid receptor) 结合。Dynorphin A (1-10) (TFA) 也阻断 NMDA 激活的电流,IC50 为 42.0 μM。
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GC34998
(S)-(-)-5-Fluorowillardiine hydrochloride
(5S)-Fluorowillardiine hydrochloride; (S)-5-Fluorowillardiine hydrochloride
(S)-(-)-5-Fluorowillardiine hydrochloride 是AMPAR高效选择性激动剂。 -
GC34828
Tat-NR2B9c TFA
Tat-NR2Bct TFA; NA-1 TFA
Tat-NR2B9c(TFA)是由20个氨基酸组成的多肽,为PSD-95的抑制剂,对PSD-95d2和PSD-95d1的EC50值分别为6.7nM和670nM。Tat-NR2B9c同时可降低NMDA诱导的p38的活化,具有神经保护作用。 -
GC34753
Radiprodil
RGH-896
An NMDA receptor antagonist
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GC34638
JNJ-61432059
JNJ-61432059是具有口服活性的、选择性的AMPAR的负向调节剂,其对GluA1/γ-8的pIC50值为9.7。在老鼠的海马体中显示出具有时间和剂量依赖性的AMPA受体占用情况,在角膜点燃癫痫动物模型中显示出较强的保护作用。
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GC34352
NMDAR antagonist 1
2,2,2-三氟-N-(丙-2-炔-1-基)乙酰胺
NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective antagonist of NMDAR. It has neuroprotective activity. -
GC33740
NT 13 (TPPT)
TPPT
NT 13 (TPPT) (TPPT) 是一种四肽,具有氨基酸序列 L-苏氨酰-L-脯氨酰-L-脯氨酰-L-苏氨酸酰胺。 -
GC33723
Becampanel (AMP 397)
AMP 397
Becampanel (AMP 397) (AMP397) 是第一个竞争性 AMPA 拮抗剂和抗癫痫剂。
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GC33701
Orphenadrine hydrochloride
盐酸奥芬那君;盐酸邻甲苯海拉明;奥芬那君盐酸盐
A muscarinic acetylcholine receptor antagonist -
GC33685
Tulrampator (CX-1632)
CX-1632; S-47445
Tulrampator (CX-1632) (CX-1632) 是一种口服生物可利用的阳性 AMPAR(AMPA 受体的变构调节剂)。 -
GC33673
24-Hydroxycholesterol
24-羟基胆固醇
24-Hydroxycholesterol是一种天然的固醇类物质,是n-甲基-d-天门冬氨酸受体(NMDA)和转录因子LXR的激活剂。
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GC33668
Naspm (1-Naphthylacetyl spermine)
1-Naphthylacetyl spermine
Naspm (1-Naphthylacetyl semimine) (1-Naphthyl acetyl semimine) 是 Joro 蜘蛛毒素的合成类似物,是一种钙渗透性 AMPA (CP-AMPA) 受体拮抗剂。 -
GC33492
Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate)
GLYX-13 Trifluoroacetate
A partial agonist of the NMDA receptor -
GC33341
Transcrocetin (trans-Crocetin)
藏红花酸; trans-Crocetin
A natural apocarotenoid with diverse biological activities -
GC32755
DNQX (FG 9041)
二硝基喹酮; FG 9041
A non-NMDA glutamate receptor antagonist -
GC32553
CNS-5161 hydrochloride (CNS 5161A)
CNS 5161A
CNS-5161 hydrochloride (CNS 5161A) 是一种新型 NMDA 离子通道拮抗剂,可与 NMDA 受体/离子通道位点相互作用,对谷氨酸的作用产生非竞争性阻断。 -
GC32447
Transcrocetinate disodium (Disodium trans-crocetinate)
藏红花酸二钠盐,Disodium trans-crocetinate
从藏红花 (Crocus sativus L.) 中提取的 Transcrocetinate disodium (Disodium trans-crocetinate) 作为 NMDA 受体拮抗剂具有高亲和力。 -
GC31309
6-Methoxy-2-naphthoic acid (Naproxen impurity O)
6-甲氧基-2-萘甲酸,Naproxen impurity O
An active metabolite of nabumetone -
GC31270
GNE 0723
GNE0723是一种可透过血脑屏障的NMDAR的正向调节剂,对GluN2A的EC50值为21nM,对GluN2C和GluN2D的EC50值分别为7.4和6.2μM。
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GC31153
UK-240455
UK-240455是一个有效且有选择性的N-甲基D-天冬氨酸(NMDA)甘氨酸位点上的拮抗剂。
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GC31076
GNE 5729
GNE5729是一种可透过血脑屏障的NMDAR的正向调节剂,对GluN2A的EC50值为37nM,对GluN2C和GluN2D的EC50值分别为4.7和9.5μM。
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GC31039
RPR104632
RPR104632是一种特异性的NMDAreceptor拮抗剂,具有神经保护的作用。
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GC31036
MRZ 2-514
MRZ2-514是一种NMDAreceptor(glycineB)的拮抗剂,Ki值为33μM。
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GC31019
GV-196771A
GV-196771A是GV196771的钠盐形式。是NMDA受体拮抗剂。
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GC30973
Mephenesin
甲酚甘油醚
Mephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist. -
GC30951
MDL 105519
3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸
MDL105519是有效和选择性的甘氨酸与NMDA受体结合的拮抗剂。 -
GC30946
Procyclidine hydrochloride ((±)-Procyclidine hydrochlorid)
丙环定盐酸盐; Tricyclamol hydrochloride; (±)-Procyclidine hydrochloride
A muscarinic acetylcholine receptor antagonist -
GC30911
Apimostinel (NRX-1074)
NRX-1074; AGN-241660
Apimostinel (NRX-1074) (NRX-1074; AGN-241660) 是一种具有口服活性的 NMDA 受体部分激动剂。
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GC30860
Neu2000
Salfaprodil free base; Neu2000
Neu2000 (Salfaprodil free base) 是 N-甲基-D-天冬氨酸 (NMDA) 的 NR2B 选择性和非竞争性拮抗剂。 -
GC30852
Org-26576
Org26576是AMPA受体的正变构调节剂。
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GC30847
IC87201
An inhibitor of the nNOS-PSD-95 protein-protein interaction
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GC30839
Traxoprodil
曲索罗地
An antagonist of NR2B subunit-containing NMDA receptors
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GC30835
Rislenemdaz (MK-0657)
MK-0657; CERC-301
Rislenemdaz (MK-0657) (CERC-301) 是一种口服生物可利用的选择性 N-甲基-D-天冬氨酸 (NMDA) 受体亚基 2B (GluN2B) 拮抗剂,其 Ki 和 IC 50 分别为 8.1 nM 和 3.6 nM。
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GC30818
ZL006
An nNOS/PSD-95 interaction inhibitor
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GC30788
L-Glutamic acid monosodium salt (Monosodium glutamate)
谷氨酸单钠盐
L-Glutamic acid monosodium salt is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods. L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals. -
GC30774
Tat-NR2B9c
Tat-NR2Bct; NA-1
Tat-NR2B9c 旨在通过阻止突触后密度蛋白 95 (PSD-95) 与 N-甲基-D-天冬氨酸 (NMDA) 受体和神经元一氧化氮结合来阻止一氧化氮 (NO) 的产生氧化物合成酶。 -
GC30457
Zonampanel (YM 872)
唑南帕奈; YM 872
Zonampanel (YM 872) (YM 872) 是谷氨酸受体亚型 α;-氨基-3-羟基-5-甲基异恶唑-4-丙酸 (AMPA) 受体的选择性拮抗剂。 -
GC30212
(S)-Willardiine ((-)-Willardiine)
尿嘧啶基丙氨酸; (-)-Willardiine
(S)-Willardiine ((-)-Willardiine) 是一种有效的 AMPA/红藻氨酸受体激动剂,EC50 为 44.8 uM。