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
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2860 |
IEM 1754 2HBrIEM 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。 |
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| S4716 |
Evans BlueEvans 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 AcidXanthurenic acid, a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3). |
||
| S1614 |
RiluzoleRiluzole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。 |
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 2HClLatrepirdine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。 |
||
| S2809 |
MPEPMPEP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。 |
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，Ki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。 |
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. |
|
| S6266New |
(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。 |
||
| S2690 |
ADX-47273ADX-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 0357121VU 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 0364439VU 0364439是一种mGlu4正性变构调节剂（PAM)， EC50为19.8 nM。 |
||
| S5137 |
O-Phospho-L-serineO-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. |
||
| S3070 |
PiracetamPiracetam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 0364770VU 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 0361737VU 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。 |
||
| S6618New |
JNJ-42153605JNJ-42153605是一种有效的、选择性mGlu2受体正向别构调节剂，EC50为17 nM。 |
||
| S1893 |
D-glutamineD-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 2HBrIEM 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 BlueEvans 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 AcidXanthurenic 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 |
RiluzoleRiluzole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。 |
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 2HClLatrepirdine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。 |
||
| S2809 |
MPEPMPEP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。 |
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，Ki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。 |
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. |
|
| S6266New |
(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。 |
||
| S2690 |
ADX-47273ADX-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 0357121VU 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 0364439VU 0364439是一种mGlu4正性变构调节剂（PAM)， EC50为19.8 nM。 |
||
| S5137 |
O-Phospho-L-serineO-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. |
||
| S3070 |
PiracetamPiracetam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 0364770VU 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 0361737VU 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。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6618New |
JNJ-42153605JNJ-42153605是一种有效的、选择性mGlu2受体正向别构调节剂，EC50为17 nM。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1893 |
D-glutamineD-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。 |
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