mGluR
Metabotropic glutamate receptors (mGluRs) are class C G protein-coupled receptors that bind glutamate and regulate synaptic transmission, neuronal excitability, and activity-dependent plasticity throughout the central nervous system[1][2]. Mechanistically, mGluRs transduce extracellular glutamate signals through intracellular signaling pathways that modulate ion channels, second messengers, and downstream neuronal responses, thereby influencing learning, memory, and network function[1][3]. The mGluR family comprises eight receptor subtypes organized into three groups based on sequence homology, pharmacology, and G-protein coupling properties[2][4]. Group I receptors (mGluR1 and mGluR5) primarily activate phospholipase C-dependent signaling and are predominantly localized postsynaptically, whereas Group II (mGluR2/3) and Group III (mGluR4/6/7/8) receptors generally inhibit cyclic AMP signaling and are frequently associated with presynaptic modulation of neurotransmitter release[2][4]. Dysregulation of mGluR signaling has been implicated in multiple neurological and neuropsychiatric disorders, including schizophrenia, Parkinson’s disease, epilepsy, anxiety disorders, and neurodegenerative conditions, making these receptors important experimental and therapeutic targets[1][5]. Compared with related glutamate receptor families, mGluRs mediate slower but longer-lasting modulatory effects through metabotropic signaling rather than direct ion channel gating, providing distinct control over neuronal circuit activity[3][4]. For experimental applications, subtype-selective agonists, antagonists, and allosteric modulators have become essential tools for dissecting receptor-specific functions, with particularly extensive pharmacological development focused on mGluR5 because of its central role in higher-order brain functions and disease-relevant signaling pathways[5][6].
References:
- [1]. Niswender CM, et al. Metabotropic glutamate receptors: physiology, pharmacology, and disease. Annu Rev Pharmacol Toxicol. 2010;50:295-322. [Content Brief]
- [2]. Conn PJ, et al. Pharmacology and functions of metabotropic glutamate receptors. Annu Rev Pharmacol Toxicol. 1997;37:205-37. [Content Brief]
- [3]. Gerber U, et al. Metabotropic glutamate receptors: intracellular signaling pathways. Curr Opin Pharmacol. 2007 Feb;7(1):56-61. [Content Brief]
- [4]. Database: Guide to pharmacology.
- [5]. Ishiwata S, et al. Contractile system of muscle as an auto-oscillator. Prog Biophys Mol Biol. 2011 May;105(3):187-98. [Content Brief]
- [6]. Kos JA, et al. Pharmacology, Signaling and Therapeutic Potential of Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators. ACS Pharmacol Transl Sci. 2024 Nov 5;7(12):3671-3690. [Content Brief]
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mGluR Related Products (207)
Related Products (207)
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BMS-984923
0 ImagesBMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling.
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LY487379
0 ImagesLY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research.
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Roemerine
0 ImagesRoemerine is an alkaloid that has been identified from the leaves of Fibraurea recisa Pierre. Roemerine exhibits antibacterial, anticancer, and antidepressant activities, can reverse the multidrug resistance phenotype in cultured cells, and exerts antibacterial effects by regulating the cAMP signaling pathway. Additionally, Roemerine influences neuronal activity by increasing BDNF protein expression and modulating the serotonergic and glutamatergic systems. Roemerine holds promise for research in the fields of cancer, infections, and neurological diseases.
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XAP044
0 ImagesXAP044 is a potent and selective antagonist of mGlu7. The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms.
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Kainic acid hydrate
0 ImagesKainic acid hydrate is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid hydrate induces seizures.
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L-Glutamine-5-13C
0 ImagesSynonyms: L-Glutamic acid 5-amide-5-13CL-Glutamine-5-13C is the 13C-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na+-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.
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JNJ-46356479
0 ImagesJNJ-46356479 is a selective and orally bioavailable mGlu2 receptor positive allosteric modulator (PAM), with the EC50 of 78 nM. JNJ-46356479 shows active in vivo.
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(-)-Camphoric acid
0 Images(-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid induces glutamate receptor expression. Camphoric acid also significantly induces the activation of NF-κB and AP-1. Camphoric acid significantly stimulates the differentiation of mouse osteoblastic MC3T3-E1 subclone 4 cells. Camphoric acid has weak regulatory function towards glutamate receptors. Camphoric acid can induce mRNA expression of glutamate signaling molecules and activate transcription factors, thereby stimulating osteoblast differentiation.
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VU0155094
0 ImagesSynonyms: ML397VU0155094 is a positive allosteric modulator with differential activity at the various group III mGluRs.
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trans-ACPD
0 ImagesSynonyms: Trans-(±)-ACPtrans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
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L-Glutamine-13C5,15N2,d5
0 ImagesSynonyms: L-Glutamic acid 5-amide-13C5,15N2,d5L-Glutamine-13C5,15N2,d5 is the deuterium, 13C-, and 15N-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na+-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.
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(S,S)-BMS-984923
0 Images(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC50 >1μM for mGluR5 receptor. BMS-984923 is a potent mGluR5 silent allosteric modulator. (S,S)-BMS-984923 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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LSN2463359
0 ImagesLSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model. LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Naftazone
0 ImagesNaftazone is a naphthoquinone derivative, it can be used for the research of venous insufciency. Naftazone protects blood vessels, increases venous tonicity and capillary resistance, and improves lymphatic and venous circulation.
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Fasoracetam
0 ImagesSynonyms: NS 105Fasoracetam (NS 105) is the activator of metabotropic glutamate receptor (mGluR). Fasoracetam (NS 105) has the potential for the research of attention-deficit hyperactivity disorder (ADHD) and Alzheimer's disease (AD).
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O-Phospho-L-serine (Standard)
0 ImagesO-Phospho-L-serine (Standard) (L-Serine O-phosphate (Standard)) is the analytical standard of O-Phospho-L-serine (HY-15129). This product is intended for research and analytical applications. O-Phospho-L-serine is the immediate precursor to L-cystein in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8). O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
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Eglumegad hydrochloride
0 ImagesCat. No.: HY-18941CSynonyms: LY354740 hydrochloride; Eglumetad hydrochlorideEglumegad (LY354740) hydrochloride is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively. Eglumegad hydrochloride protects neurons from NMDA toxicity. Eglumegad hydrochloride has anxiolytic- and antipsychotic-like effects.
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ZJ43
0 ImagesZJ43 is a NAAG peptidase inhibitor and glutamate carboxypeptidase II/III (GCP II/III) inhibitor with human GCP II IC50 of 2.4 nM and Ki of 0.8 nM. ZJ43 blocks N-acetylaspartylglutamate hydrolysis, elevates extracellular N-acetylaspartylglutamate levels, and activates group II metabotropic glutamate receptors (mGluR). ZJ43 can be used for the research of schizophrenia, inflammatory pain, neuropathic pain, and traumatic brain injury.
