GluR
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
GluR Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2860 |
IEM 1754 2HBrIEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM. |
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| S6906 |
Capric acidCapric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt. |
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| S4716 |
Evans BlueEvans Blue (Direct Blue 53) is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist. |
||
| 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 |
Riluzole (PK 26124)Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities. |
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 is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug. |
||
| S2861 |
CTEP (RO4956371)CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors. |
||
| S2809 |
MPEPMPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors. |
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)
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|
| S9686 |
NBQX (FG9202)NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect. |
||
| S2645 |
SIB 1757SIB 1757 is a highly selective, noncompetitive antagonist of metabotropic glutamate receptor type 5 (mGluR5) with IC50 of 0.4 μM at hmGluR5 compared with >30 µM at hmGluR1b, hmGluR2, hmGluR4, hmGluR6, hmGluR7 and hmGluR8. |
||
| S6001 |
pomaglumetad (LY404039)LY404039 is a potent agonist of recombinant human mGlu2/mGlu3 receptors with Ki of 149 nM/92 nM, shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. 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. |
|
| S2690 |
ADX-47273ADX47273 (BA 94673139) is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes. |
||
| S2795 |
VU 0357121VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes. |
||
| S8035 |
VU 0364439VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 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) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders. |
||
| S6266 |
(S)-Glutamic acid(S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist. |
||
| S0165 |
Ampalex (CX-516)Ampalex (CX-516, Ampakine CX 516, BDP-12, SPD 420) is a positive allosteric modulator of AMPA receptor. Ampalex exhibits potential treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI). |
||
| S2862 |
VU 0364770VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes. |
||
| S2892 |
VU 0361737VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS. |
||
| S6803 |
1-BCP1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents. |
||
| S5222 |
ColuracetamColuracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects. |
||
| S4721 |
L-Glutamic acid monosodium saltL-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. |
||
| S6804 |
CX546CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator. |
||
| S6618 |
JNJ-42153605JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM. |
||
| S2434 |
IDRA-21IDRA-21 is a partial allosteric modulator of AMPA receptor desensitization. IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability. |
||
| S1893 |
D-glutamineD-glutamine is a D type stereoisomer of glutamine which is one of the 20 amino acids encoded by the standard genetic code. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2860 |
IEM 1754 2HBrIEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM. |
||
| S6906 |
Capric acidCapric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt. |
||
| S4716 |
Evans BlueEvans Blue (Direct Blue 53) is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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). |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1614 |
Riluzole (PK 26124)Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities. |
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 is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug. |
||
| S2861 |
CTEP (RO4956371)CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors. |
||
| S2809 |
MPEPMPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors. |
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) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect. |
||
| S2645 |
SIB 1757SIB 1757 is a highly selective, noncompetitive antagonist of metabotropic glutamate receptor type 5 (mGluR5) with IC50 of 0.4 μM at hmGluR5 compared with >30 µM at hmGluR1b, hmGluR2, hmGluR4, hmGluR6, hmGluR7 and hmGluR8. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S6001 |
pomaglumetad (LY404039)LY404039 is a potent agonist of recombinant human mGlu2/mGlu3 receptors with Ki of 149 nM/92 nM, shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. 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. |
|
| S2690 |
ADX-47273ADX47273 (BA 94673139) is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes. |
||
| S2795 |
VU 0357121VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes. |
||
| S8035 |
VU 0364439VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 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) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders. |
||
| S6266 |
(S)-Glutamic acid(S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist. |
||
| S0165 |
Ampalex (CX-516)Ampalex (CX-516, Ampakine CX 516, BDP-12, SPD 420) is a positive allosteric modulator of AMPA receptor. Ampalex exhibits potential treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI). |
||
| S2862 |
VU 0364770VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes. |
||
| S2892 |
VU 0361737VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS. |
||
| S6803 |
1-BCP1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents. |
||
| S5222 |
ColuracetamColuracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects. |
||
| S4721 |
L-Glutamic acid monosodium saltL-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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S6804 |
CX546CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator. |
||
| S6618 |
JNJ-42153605JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM. |
||
| S2434 |
IDRA-21IDRA-21 is a partial allosteric modulator of AMPA receptor desensitization. IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1893 |
D-glutamineD-glutamine is a D type stereoisomer of glutamine which is one of the 20 amino acids encoded by the standard genetic code. |
