GluR

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抑制剂选择性比较

特异性亚型抑制剂

GluR产品

所有产品(27) GluR抑制剂(3) GluR激活剂(1) GluR拮抗剂(6) GluR激动剂(13) GluR调节剂(3)

目录号	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。
S6906	Capric acid Capric 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。
S4716	Evans Blue Evans 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 Acid Xanthurenic 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	Riluzole (PK 26124) Riluzole (PK 26124, RP-54274)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。	Mol Genet Metab, 2021, S1096-7192(21)00826-X Cancer Res, 2019, 79(8):1799-1809 Neuropharmacology, 2019, 150:175-183	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 themost 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)
S9686	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。
S2645	SIB 1757 SIB 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。
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。	Schizophr Bull, 2021, sbab047 Neuropsychopharmacology, 2020, 10.1038/s41386-020-0764-2 Sci Rep, 2019, 9(1):14247	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.
S2690	ADX-47273 ADX47273 (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。	J Biol Chem, 2014, 289(41):28460-77
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。	Antioxidants (Basel), 2018, 10.3390/antiox7110150
S5137	O-Phospho-L-serine O-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	Piracetam Piracetam (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。	CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S0165	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。
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。
S6803	1-BCP 1-BCP (Piperonylic acid piperidide) 是一种记忆增强剂，可增强AMPA诱导的电流。
S5222	Coluracetam Coluracetam (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 salt L-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。
S6804	CX546 CX546 是一种典型的安帕金药剂、选择性的 AMPA receptor 的阳性调节剂。
S6618	JNJ-42153605 JNJ-42153605是一种有效的、选择性mGlu2受体正向别构调节剂，EC50为17 nM。
S2434	IDRA-21 IDRA-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。
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。

目录号

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。

S6906

Capric acid

Capric 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。

S4716

Evans Blue

Evans 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 Acid Xanthurenic 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

S4774

Xanthurenic 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	Riluzole (PK 26124) Riluzole (PK 26124, RP-54274)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。	Mol Genet Metab, 2021, S1096-7192(21)00826-X Cancer Res, 2019, 79(8):1799-1809 Neuropharmacology, 2019, 150:175-183	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 themost 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)
S9686	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。
S2645	SIB 1757 SIB 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。

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，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。	Schizophr Bull, 2021, sbab047 Neuropsychopharmacology, 2020, 10.1038/s41386-020-0764-2 Sci Rep, 2019, 9(1):14247	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.
S2690	ADX-47273 ADX47273 (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。	J Biol Chem, 2014, 289(41):28460-77
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。	Antioxidants (Basel), 2018, 10.3390/antiox7110150
S5137	O-Phospho-L-serine O-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	Piracetam Piracetam (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。	CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S0165	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。
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。
S6803	1-BCP 1-BCP (Piperonylic acid piperidide) 是一种记忆增强剂，可增强AMPA诱导的电流。
S5222	Coluracetam Coluracetam (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 salt L-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
S6804	CX546 CX546 是一种典型的安帕金药剂、选择性的 AMPA receptor 的阳性调节剂。
S6618	JNJ-42153605 JNJ-42153605是一种有效的、选择性mGlu2受体正向别构调节剂，EC50为17 nM。
S2434	IDRA-21 IDRA-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。

目录号

产品描述

文献引用

实验数据

S6804

目录号	产品描述	文献引用	实验数据
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。

产品描述

文献引用

实验数据

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。

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抑制剂选择性比较

特异性亚型抑制剂

GluR产品