GluR

亜型選択性的な製品

NMDA receptor AMPA receptor mGluR2 mGluR3 mGluR4 mGluR5

シグナル伝達経路

GluR製品

All (48)
GluR阻害剤 (4)
GluR活性剤(2)
GluR拮抗剤(8)
GluR作動薬(14)
GluRモジュレータ(4)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S1614	Riluzole	Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.	Neurotherapeutics, 2023, none J Endocr Soc, 2023, 7(10):bvad117 Front Bioeng Biotechnol, 2022, 10:855755
S6001	pomaglumetad (LY404039)	LY404039 is a potent agonist of recombinant human mGlu2/mGlu3 receptors with K_i of 149 nM/92 nM, shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3.	Schizophr Bull, 2021, sbab047 Neuropsychopharmacology, 2020, 10.1038/s41386-020-0764-2 Sci Rep, 2019, 9(1):14247
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.	Int J Mol Sci, 2022, 23(18)10551 Front Physiol, 2022, 13:1008073
S6266	(S)-Glutamic acid	(S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.	Cancer Sci, 2022, 113-6:1955-1967 CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S2251	(-)-Huperzine A (HupA)	(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with K_i of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.	Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4
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.	EBioMedicine, 2017, 20:120-126
S2690	ADX-47273	ADX47273 (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.	J Biol Chem, 2014, 289(41):28460-77
S2809	MPEP	MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.	Mol Neurobiol, 2017, 54(7):5286-5299
S8035	VU 0364439	VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.	Antioxidants (Basel), 2018, 10.3390/antiox7110150
S6906	Capric acid	Capric 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.	Pharmaceuticals (Basel), 2023, 16(5)692
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).	Cell Commun Signal, 2023, 21(1):141
S2645	SIB 1757	SIB 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.	MedComm (2020), 2023, 4(2):e242 MedComm (2020), 2023, 4(2):e242
S4716	Evans Blue	Evans Blue (Direct Blue 53,C.I.23860) is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.	Int J Nanomedicine, 2024, 19:6677-6692 J Biol Chem, 2022, 298(12):102699
S4721	L-Glutamic acid monosodium salt	L-Glutamic acid monosodium salt (Monosodium glutamate, MSG) is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods.	Heliyon, 2024, 10(1):e23945 Acta Biomater, 2022, 152:255-272
S1245	Latrepirdine 2HCl	Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.
S2795	VU 0357121	VU0357121 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.
S1893	D-glutamine	D-glutamine is a D type stereoisomer of glutamine which is one of the 20 amino acids encoded by the standard genetic code.
S2860	IEM 1754 2HBr	IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
E1257	(R,S)-3,5-DHPG Hydrochloride	(R,S)-3,5-DHPG hydrochloride (DHPG, Dihydroxy phenylglycine) is a salt of free amino acid dihydroxy phenylglycine (DHPG) which acts as a selective and potent agonist of group I metabotropic glutamate receptors (mGluR) (mGluR 1 and mGluR 5).
E0484	CNQX	CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) is an AMPA and kainate receptor antagonist with IC50 values are 0.3 μM and 1.5 μM for AMPA and kainate receptors, respectively. CNQX is also an antagonist at the glycine modulatory site on the NMDA receptor complex (IC50 = 25 μM). CNQX shows neuroprotective effects in models of ischemia and inhibits seizure-like activity in hippocampal neurons.
S3070	Piracetam	Piracetam (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
S6804	CX546	CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator.
S8143^New	Mavoglurant	Mavoglurant (AFQ056) is a structurally selective, non-competitive antagonist of mGlu5 receptor with an IC50 of 30 nM. It exhibits efficacy in treatment of L-dopa induced dyskinesia in Parkinson's disease and Fragile X syndrome.
E4619^New	Basimglurant	Basimglurant(RG7090, CTEP Derivative) is a potent and selective negative allosteric modulator of mGlu5, with a Kd of 1.1 nM, It inhibits the function of mGluR5, thereby regulating glutamatergic neurotransmission.
S1970	VU-29	VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor, with EC50 of 9 nM and Ki=244 nM for rat mGluR5, which is selective for mGluR5 relative to other mGluR subtypes.
S6618	JNJ-42153605	JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.
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 0364770	VU 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 0361737	VU 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.
S2434	IDRA-21	IDRA-21 is a partial allosteric modulator of AMPA receptor desensitization. IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability.
S9686	NBQX (FG9202)	NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
S6803	1-BCP	1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents.
E1773^New	Fasoracetam (NS 105)	Fasoracetam (NS 105) is a metabotropic glutamate receptor activator with a potential to treat vascular dementia.
S5222	Coluracetam	Coluracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects.
S6001	pomaglumetad (LY404039)	LY404039 is a potent agonist of recombinant human mGlu2/mGlu3 receptors with K_i of 149 nM/92 nM, shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3.	Schizophr Bull, 2021, sbab047 Neuropsychopharmacology, 2020, 10.1038/s41386-020-0764-2 Sci Rep, 2019, 9(1):14247
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.	Int J Mol Sci, 2022, 23(18)10551 Front Physiol, 2022, 13:1008073
S6266	(S)-Glutamic acid	(S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.	Cancer Sci, 2022, 113-6:1955-1967 CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S2690	ADX-47273	ADX47273 (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.	J Biol Chem, 2014, 289(41):28460-77
S8035	VU 0364439	VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.	Antioxidants (Basel), 2018, 10.3390/antiox7110150
S4721	L-Glutamic acid monosodium salt	L-Glutamic acid monosodium salt (Monosodium glutamate, MSG) is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods.	Heliyon, 2024, 10(1):e23945 Acta Biomater, 2022, 152:255-272
S2795	VU 0357121	VU0357121 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.
E1257	(R,S)-3,5-DHPG Hydrochloride	(R,S)-3,5-DHPG hydrochloride (DHPG, Dihydroxy phenylglycine) is a salt of free amino acid dihydroxy phenylglycine (DHPG) which acts as a selective and potent agonist of group I metabotropic glutamate receptors (mGluR) (mGluR 1 and mGluR 5).
S3070	Piracetam	Piracetam (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
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 0364770	VU 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 0361737	VU 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-BCP	1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents.
S5222	Coluracetam	Coluracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects.
S6906	Capric acid	Capric 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.	Pharmaceuticals (Basel), 2023, 16(5)692
S4716	Evans Blue	Evans Blue (Direct Blue 53,C.I.23860) is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist.	Int J Nanomedicine, 2024, 19:6677-6692 J Biol Chem, 2022, 298(12):102699
S2860	IEM 1754 2HBr	IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.
E4619^New	Basimglurant	Basimglurant(RG7090, CTEP Derivative) is a potent and selective negative allosteric modulator of mGlu5, with a Kd of 1.1 nM, It inhibits the function of mGluR5, thereby regulating glutamatergic neurotransmission.
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).	Cell Commun Signal, 2023, 21(1):141
E1773^New	Fasoracetam (NS 105)	Fasoracetam (NS 105) is a metabotropic glutamate receptor activator with a potential to treat vascular dementia.
S1614	Riluzole	Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.	Neurotherapeutics, 2023, none J Endocr Soc, 2023, 7(10):bvad117 Front Bioeng Biotechnol, 2022, 10:855755
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.	EBioMedicine, 2017, 20:120-126
S2809	MPEP	MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.	Mol Neurobiol, 2017, 54(7):5286-5299
S2645	SIB 1757	SIB 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.	MedComm (2020), 2023, 4(2):e242 MedComm (2020), 2023, 4(2):e242
S1245	Latrepirdine 2HCl	Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.
E0484	CNQX	CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) is an AMPA and kainate receptor antagonist with IC50 values are 0.3 μM and 1.5 μM for AMPA and kainate receptors, respectively. CNQX is also an antagonist at the glycine modulatory site on the NMDA receptor complex (IC50 = 25 μM). CNQX shows neuroprotective effects in models of ischemia and inhibits seizure-like activity in hippocampal neurons.
S8143^New	Mavoglurant	Mavoglurant (AFQ056) is a structurally selective, non-competitive antagonist of mGlu5 receptor with an IC50 of 30 nM. It exhibits efficacy in treatment of L-dopa induced dyskinesia in Parkinson's disease and Fragile X syndrome.
S9686	NBQX (FG9202)	NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
S6001	pomaglumetad (LY404039)	LY404039 is a potent agonist of recombinant human mGlu2/mGlu3 receptors with K_i of 149 nM/92 nM, shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3.	Schizophr Bull, 2021, sbab047 Neuropsychopharmacology, 2020, 10.1038/s41386-020-0764-2 Sci Rep, 2019, 9(1):14247
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.	Int J Mol Sci, 2022, 23(18)10551 Front Physiol, 2022, 13:1008073
S6266	(S)-Glutamic acid	(S)-Glutamic acid (L-Glutamic acid) is an endogenous, non-selective glutamate receptor agonist.	Cancer Sci, 2022, 113-6:1955-1967 CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S2690	ADX-47273	ADX47273 (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.	J Biol Chem, 2014, 289(41):28460-77
S8035	VU 0364439	VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.	Antioxidants (Basel), 2018, 10.3390/antiox7110150
S4721	L-Glutamic acid monosodium salt	L-Glutamic acid monosodium salt (Monosodium glutamate, MSG) is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods.	Heliyon, 2024, 10(1):e23945 Acta Biomater, 2022, 152:255-272
S2795	VU 0357121	VU0357121 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.
E1257	(R,S)-3,5-DHPG Hydrochloride	(R,S)-3,5-DHPG hydrochloride (DHPG, Dihydroxy phenylglycine) is a salt of free amino acid dihydroxy phenylglycine (DHPG) which acts as a selective and potent agonist of group I metabotropic glutamate receptors (mGluR) (mGluR 1 and mGluR 5).
S3070	Piracetam	Piracetam (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
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 0364770	VU 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 0361737	VU 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-BCP	1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents.
S5222	Coluracetam	Coluracetam (BCI-540, MKC-231) is a nootropic belonging to the racetam family of drugs with cognitive enhancing and neuroprotective effects.
S6804	CX546	CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator.
S1970	VU-29	VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor, with EC50 of 9 nM and Ki=244 nM for rat mGluR5, which is selective for mGluR5 relative to other mGluR subtypes.
S6618	JNJ-42153605	JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.
S2434	IDRA-21	IDRA-21 is a partial allosteric modulator of AMPA receptor desensitization. IDRA-21 is a potent cognition-enhancing drug virtually devoid of neurotoxic liability.
S8143^New	Mavoglurant	Mavoglurant (AFQ056) is a structurally selective, non-competitive antagonist of mGlu5 receptor with an IC50 of 30 nM. It exhibits efficacy in treatment of L-dopa induced dyskinesia in Parkinson's disease and Fragile X syndrome.
E4619^New	Basimglurant	Basimglurant(RG7090, CTEP Derivative) is a potent and selective negative allosteric modulator of mGlu5, with a Kd of 1.1 nM, It inhibits the function of mGluR5, thereby regulating glutamatergic neurotransmission.
E1773^New	Fasoracetam (NS 105)	Fasoracetam (NS 105) is a metabotropic glutamate receptor activator with a potential to treat vascular dementia.

GluR阻害剤の選択性比較