GluR

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

GluR产品

所有产品 GluR抑制剂(2) GluR激活剂(1) GluR拮抗剂(4) GluR激动剂(9) GluR化学产品(1) 新GluR产品

产品目录	产品描述	文献引用	实验数据
S2860	IEM 1754 2HBr IEM 1754 2HBr是一种选择性AMPA/kainate受体抑制剂，作用于GluR1和GluR3，IC50为6 μM。
S4716	Evans Blue Evans Blue是突触泡谷氨酸吸收的有效抑制剂，同时也是一种AMPA/kainate受体拮抗剂。
S4774	Xanthurenic Acid Xanthurenic acid, a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3).
S1614	Riluzole Riluzole是谷氨酸盐释放抑制剂，具有神经保护、抗癫痫、抗焦虑以及麻醉作用。	Int J Mol Sci, 2016, 17(3):357 J Neuroimmune Pharmacol, 2013, 8(5):1098-105	Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (p≤0.036). c Swim Speed. Aged rats swam the most slowly (p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (p<0.001).
S1245	Latrepirdine 2HCl Latrepirdine具有口服活性及神经活性，可以作为包括histamine receptors, GluR, 和5-HT receptors在内的多个药物靶点的拮抗剂，用作抗组织胺的药物。
S2861	CTEP (RO4956371) CTEP (RO4956371)是一种新型，长效的，口服生物有效的，mGlu5受体变构拮抗剂，IC50为2.2 nM，比作用于其他mGlu受体选择性高1000倍以上。	EBioMedicine, 2017, 20:120-126
S2809	MPEP MPEP是一种选择性mGlu5受体拮抗剂，IC50为36 nM，对mGlu1b/2/3/4a/7b/8a/6受体几乎没有作用活性。	Mol Neurobiol, 2017, 54(7):5286-5299	The expression of mGluR5 and Homer were detected by Western blot and analysed by ImageJ. a–c Cells were treated with various concentrations of pu-erh tea for 12 h. d–f Cells were treated with 62.5 μg/mL pu-erh tea for 3, 6, 9, 12 h. g-i Cells were treated with 62.5 μg/mL pu-erh, black, or green teas for 12 h. Data were analysed using GraphPad Prism software (*p < 0.001 vs. vehicle control, p < 0.01 vs. vehicle control, n = 3)
S6001	pomaglumetad (LY404039) LY404039是一种有效的重组人类mGlu2/mGlu3受体激动剂，K_i为149 nM/92 nM，比作用于其他离子型谷氨酸受体，谷氨酸转运体及其他受体选择性高100倍以上。Phase 3。	Synapse, 2015, 70:45–48 Neuropharm, 2012, 62(7):2184-91 PLoS One, 2011, 6(7):e22235	LY404039 avoids reduction in phospho-Akt levels caused by DETA/NO. Total cellular proteins were extracted as described in Materials and Methods from astrocytes exposed to 1 mM DETA/NO6100 mM LY40403961 mM db-cAMP for 30 min, and 50 mg of protein extracts were assayed for phospho-Akt by western-blot. (A) Specificity of the western-blot was analyzed by incubating astrocytes with the PI3K/Akt pathway inhibitor, 20 mM LY294002, which completely prevented LY404039-induced Akt phosphorylation, and LPS/IFNc was used as positive control of Akt activation. Membranes were stripped and incubated with anti-total Akt antibody, which was considered loading control. (B) Data were expressed as phospho-Akt/ total Akt ratio and related to control group. Bars represent the mean 6 SEM of 4 independent experiments. p,0.05, **p,0.001 versus control, ‘‘p,0.01 versus LY404039.
S6266^New	(S)-Glutamic acid (S)-Glutamic acid (L-Glutamic acid)是一种内源性的、非选择性的谷氨酸受体（glutamate receptor）激动剂。
S5137^New	O-Phospho-L-serine O-Phospho-L-serine, a molecule that mimics the phosphatidylserine head group and partially blocks microglial phagocytosis of apoptotic cells, is a specific group III metabotropic glutamate receptor (mGluR) agonist.
S2690	ADX-47273 ADX-47273是一种有效的，特异性的mGlu5正变构调节剂(PAM)EC50为0.17 μM，对其他亚型没有作用活性。
S2795	VU 0357121 VU 0357121是一种新型的mGlu5正变构调节剂（PAM），EC50为33 nM，抑制其他mGlu受体亚型活性或使其活性非常低。
S8035	VU 0364439 VU 0364439是一种mGlu4正性变构调节剂（PAM)， EC50为19.8 nM。
S3070	Piracetam Piracetam是神经递质氨基丁酸(GABA)的一种环状衍生物,用于治疗一系列认知障碍。
S2862	VU 0364770 VU 0364770是一种mGlu4正变构调节剂(PAM)，EC50为1.1 μM，对68种其他受体，包括其他mGlu亚型，几乎没有作用活性。
S2892	VU 0361737 VU 0361737是一种选择性(PAM)mGlu4受体正变构调节剂(PAM)，作用于人类和大鼠受体，EC50分别为240 nM和110 nM，对mGlu5和mGlu8受体具有微弱的作用活性，抑制mGlu1， mGlu2， mGlu3， mGlu6 and mGlu7受体活性，可以渗透进入CNS。
S1893	D-glutamine D-glutamine是谷氨酰胺的D型立体异构，是标准遗传密码所编码的20个氨基酸之一。

产品目录

产品描述

文献引用

实验数据

S2860

IEM 1754 2HBr

IEM 1754 2HBr是一种选择性AMPA/kainate受体抑制剂，作用于GluR1和GluR3，IC50为6 μM。

S4716

Evans Blue

Evans Blue是突触泡谷氨酸吸收的有效抑制剂，同时也是一种AMPA/kainate受体拮抗剂。

产品目录	产品描述	文献引用	实验数据
S4774	Xanthurenic Acid Xanthurenic acid, a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3).

产品目录

产品描述

文献引用

实验数据

S4774

Xanthurenic Acid

Xanthurenic acid, a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3).

产品目录	产品描述	文献引用	实验数据
S1614	Riluzole Riluzole是谷氨酸盐释放抑制剂，具有神经保护、抗癫痫、抗焦虑以及麻醉作用。	Int J Mol Sci, 2016, 17(3):357 J Neuroimmune Pharmacol, 2013, 8(5):1098-105	Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (p≤0.036). c Swim Speed. Aged rats swam the most slowly (p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (p<0.001).
S1245	Latrepirdine 2HCl Latrepirdine具有口服活性及神经活性，可以作为包括histamine receptors, GluR, 和5-HT receptors在内的多个药物靶点的拮抗剂，用作抗组织胺的药物。
S2861	CTEP (RO4956371) CTEP (RO4956371)是一种新型，长效的，口服生物有效的，mGlu5受体变构拮抗剂，IC50为2.2 nM，比作用于其他mGlu受体选择性高1000倍以上。	EBioMedicine, 2017, 20:120-126
S2809	MPEP MPEP是一种选择性mGlu5受体拮抗剂，IC50为36 nM，对mGlu1b/2/3/4a/7b/8a/6受体几乎没有作用活性。	Mol Neurobiol, 2017, 54(7):5286-5299	The expression of mGluR5 and Homer were detected by Western blot and analysed by ImageJ. a–c Cells were treated with various concentrations of pu-erh tea for 12 h. d–f Cells were treated with 62.5 μg/mL pu-erh tea for 3, 6, 9, 12 h. g-i Cells were treated with 62.5 μg/mL pu-erh, black, or green teas for 12 h. Data were analysed using GraphPad Prism software (*p < 0.001 vs. vehicle control, p < 0.01 vs. vehicle control, n = 3)

产品目录	产品描述	文献引用	实验数据
S6001	pomaglumetad (LY404039) LY404039是一种有效的重组人类mGlu2/mGlu3受体激动剂，K_i为149 nM/92 nM，比作用于其他离子型谷氨酸受体，谷氨酸转运体及其他受体选择性高100倍以上。Phase 3。	Synapse, 2015, 70:45–48 Neuropharm, 2012, 62(7):2184-91 PLoS One, 2011, 6(7):e22235	LY404039 avoids reduction in phospho-Akt levels caused by DETA/NO. Total cellular proteins were extracted as described in Materials and Methods from astrocytes exposed to 1 mM DETA/NO6100 mM LY40403961 mM db-cAMP for 30 min, and 50 mg of protein extracts were assayed for phospho-Akt by western-blot. (A) Specificity of the western-blot was analyzed by incubating astrocytes with the PI3K/Akt pathway inhibitor, 20 mM LY294002, which completely prevented LY404039-induced Akt phosphorylation, and LPS/IFNc was used as positive control of Akt activation. Membranes were stripped and incubated with anti-total Akt antibody, which was considered loading control. (B) Data were expressed as phospho-Akt/ total Akt ratio and related to control group. Bars represent the mean 6 SEM of 4 independent experiments. p,0.05, **p,0.001 versus control, ‘‘p,0.01 versus LY404039.
S6266^New	(S)-Glutamic acid (S)-Glutamic acid (L-Glutamic acid)是一种内源性的、非选择性的谷氨酸受体（glutamate receptor）激动剂。
S5137^New	O-Phospho-L-serine O-Phospho-L-serine, a molecule that mimics the phosphatidylserine head group and partially blocks microglial phagocytosis of apoptotic cells, is a specific group III metabotropic glutamate receptor (mGluR) agonist.
S2690	ADX-47273 ADX-47273是一种有效的，特异性的mGlu5正变构调节剂(PAM)EC50为0.17 μM，对其他亚型没有作用活性。
S2795	VU 0357121 VU 0357121是一种新型的mGlu5正变构调节剂（PAM），EC50为33 nM，抑制其他mGlu受体亚型活性或使其活性非常低。
S8035	VU 0364439 VU 0364439是一种mGlu4正性变构调节剂（PAM)， EC50为19.8 nM。
S3070	Piracetam Piracetam是神经递质氨基丁酸(GABA)的一种环状衍生物,用于治疗一系列认知障碍。
S2862	VU 0364770 VU 0364770是一种mGlu4正变构调节剂(PAM)，EC50为1.1 μM，对68种其他受体，包括其他mGlu亚型，几乎没有作用活性。
S2892	VU 0361737 VU 0361737是一种选择性(PAM)mGlu4受体正变构调节剂(PAM)，作用于人类和大鼠受体，EC50分别为240 nM和110 nM，对mGlu5和mGlu8受体具有微弱的作用活性，抑制mGlu1， mGlu2， mGlu3， mGlu6 and mGlu7受体活性，可以渗透进入CNS。