GluR
特异性亚型抑制剂
GluR产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S6906New |
Capric acidCapric acid (DA, Decanoic acid, Decylic acid) 是在椰子油和棕榈油中天然存在的中链甘油三酯的成分,可通过直接抑制 AMPA receptor 来控制癫痫发作。癸酸还是 PPARs 的调节配体。由于其特殊的熔化范围,产品可能是固体、液体或半固体状态。 |
||
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 (Direct Blue 53) 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 (xanthurenate, 8-Hydroxykynurenic acid, 4,8-Dihydroxyquinaldic acid), a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3). |
||
S1614 |
RiluzoleRiluzole (RP-54274, PK 26124) 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。 |
||
S9686New |
NBQX (FG9202)NBQX (FG9202, NNC 079202) 是一种具有高选择性的 AMPA receptor (AMPAR) 的竞争性拮抗剂,具有抗癫痫的作用。 |
||
S2645New |
SIB 1757SIB 1757是一种高选择性、非竞争性的 metabotropic glutamate receptor type 5 (mGluR5) 的拮抗剂,对于hmGluR5的IC50值为0.4μM,而对于hmGluR1b,hmGluR2,hmGluR4,hmGluR6,hmGluR7和hmGluR7的IC50值均>30 µM。 |
||
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. |
|
S6803New |
1-BCP1-BCP (Piperonylic acid piperidide) 是一种记忆增强剂,可增强AMPA诱导的电流。 |
||
S0165New |
Ampalex (CX-516)Ampalex (CX-516, Ampakine CX 516, BDP-12, SPD 420) 是一种 AMPA receptor 的正向变构调节剂。Ampalex 对阿尔茨海默氏病,精神分裂症和轻度认知障碍(MCI)具有潜在的治疗作用。 |
||
S2690 |
ADX-47273ADX47273 (BA 94673139)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 (Dexfosfoserine), 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 (UCB 6215)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。 |
||
S6266 |
(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。 |
||
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。 |
||
S5222 |
ColuracetamColuracetam (BCI-540, MKC-231)是益智类药,具有增强认知和神经保护作用。 |
||
S4721 |
L-Glutamic acid monosodium saltL-Glutamic acid monosodium salt (Monosodium glutamate, MSG) 是谷氨酸的钠盐形式,天然存在于马铃薯、奶酪和其他食物中。 |
||
S6804New |
CX546CX546 是一种典型的安帕金药剂、选择性的 AMPA receptor 的阳性调节剂。 |
||
S2434New |
IDRA-21IDRA-21是一种 AMPA receptor 脱敏的部分变构调节剂。IDRA-21是一种有效的增强认知药物,几乎没有神经毒性作用。 |
||
S6618 |
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。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S6906New |
Capric acidCapric acid (DA, Decanoic acid, Decylic acid) 是在椰子油和棕榈油中天然存在的中链甘油三酯的成分,可通过直接抑制 AMPA receptor 来控制癫痫发作。癸酸还是 PPARs 的调节配体。由于其特殊的熔化范围,产品可能是固体、液体或半固体状态。 |
||
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 (Direct Blue 53) 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。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S4774 |
Xanthurenic AcidXanthurenic acid (xanthurenate, 8-Hydroxykynurenic acid, 4,8-Dihydroxyquinaldic acid), a molecule arising from tryptophan metabolism by transamination of 3-hydroxykynurenine, activates mGlu2/3 Metabotropic glutamate receptors (mGlu2 and mGlu3). |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1614 |
RiluzoleRiluzole (RP-54274, PK 26124) 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。 |
||
S9686New |
NBQX (FG9202)NBQX (FG9202, NNC 079202) 是一种具有高选择性的 AMPA receptor (AMPAR) 的竞争性拮抗剂,具有抗癫痫的作用。 |
||
S2645New |
SIB 1757SIB 1757是一种高选择性、非竞争性的 metabotropic glutamate receptor type 5 (mGluR5) 的拮抗剂,对于hmGluR5的IC50值为0.4μM,而对于hmGluR1b,hmGluR2,hmGluR4,hmGluR6,hmGluR7和hmGluR7的IC50值均>30 µM。 |
||
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)
|
目录号 | 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. |
|
S6803New |
1-BCP1-BCP (Piperonylic acid piperidide) 是一种记忆增强剂,可增强AMPA诱导的电流。 |
||
S0165New |
Ampalex (CX-516)Ampalex (CX-516, Ampakine CX 516, BDP-12, SPD 420) 是一种 AMPA receptor 的正向变构调节剂。Ampalex 对阿尔茨海默氏病,精神分裂症和轻度认知障碍(MCI)具有潜在的治疗作用。 |
||
S2690 |
ADX-47273ADX47273 (BA 94673139)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 (Dexfosfoserine), 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 (UCB 6215)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。 |
||
S6266 |
(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。 |
||
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。 |
||
S5222 |
ColuracetamColuracetam (BCI-540, MKC-231)是益智类药,具有增强认知和神经保护作用。 |
||
S4721 |
L-Glutamic acid monosodium saltL-Glutamic acid monosodium salt (Monosodium glutamate, MSG) 是谷氨酸的钠盐形式,天然存在于马铃薯、奶酪和其他食物中。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S6804New |
CX546CX546 是一种典型的安帕金药剂、选择性的 AMPA receptor 的阳性调节剂。 |
||
S2434New |
IDRA-21IDRA-21是一种 AMPA receptor 脱敏的部分变构调节剂。IDRA-21是一种有效的增强认知药物,几乎没有神经毒性作用。 |
||
S6618 |
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。 |
目录号 | 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。 |