mGluR2
Metabotropic glutamate receptor 2 (mGluR2) functions as a presynaptic inhibitory receptor regulating glutamatergic neurotransmission through Galpha inhibitory subunits[1]. Mechanistically, mGluR2 modulates synaptic plasticity at hippocampal mossy fiber-CA3 synapses, mediating transient suppression of transmission, long-term depression (LTD), and inhibition of long-term potentiation (LTP)[1]. Compared with its closely related isoform mGluR3, mGluR2 exhibits distinct presynaptic localization and does not directly promote neural progenitor proliferation via ERK1/2 or JNK2 signaling[2]. In disease models, mGluR2 contributes to fear extinction in the lateral amygdala through long-term weakening of presynaptic release probability[3], while peripheral mGluR2 activation reduces prostaglandin E2-induced nociceptive sensitization[4]. In COVID-19 patients, anti-mGluR2 autoantibodies have been identified, indicating immune system cross-reactivity and potential neurological implications[5]. Pharmacologically, mGluR2-selective agonists, such as LY395756, modulate NMDA receptor expression and function, whereas positive allosteric modulators like (+)-TFMPIP selectively attenuate stress-induced phasic glutamate release without affecting tonic levels[6][7]. These findings highlight mGluR2 as a target for studies of synaptic plasticity, neuropsychiatric disorders, inflammatory pain, and allosteric modulation in experimental models.
References:
- [1]. Nicholls RE, et al. mGluR2 acts through inhibitory Galpha subunits to regulate transmission and long-term plasticity at hippocampal mossy fiber-CA3 synapses. Proc Natl Acad Sci U S A. 2006 Apr 18;103(16):6380-5. [Content Brief]
- [2]. Wu Z, et al. Identifying Neurological Autoantibodies in COVID-19: mGluR2 as a Marker of Immune Dysregulation During the Omicron Outbreak in China. J Med Virol. 2025 May;97(5):e70381. [Content Brief]
- [3]. Guo J, et al. mGluR3 promotes proliferation of human embryonic cortical neural progenitor cells by activating ERK1/2 and JNK2 signaling pathway in vitro. Cell Mol Biol (Noisy-le-grand). 2014;60(2):42-49.
- [4]. Yang D, et al. Peripheral group II metabotropic glutamate receptors (mGluR2/3) regulate prostaglandin E2-mediated sensitization of capsaicin responses and thermal nociception. J Neurosci. 2002 Aug 1;22(15):6388-93. [Content Brief]
- [5]. Li ML, et al. LY395756, an mGluR2 agonist and mGluR3 antagonist, enhances NMDA receptor expression and function in the normal adult rat prefrontal cortex, but fails to improve working memory and reverse MK801-induced working memory impairment. Exp Neurol. 2015 Nov;273:190-201. [Content Brief]
- [6]. Hascup ER, et al. An allosteric modulator of metabotropic glutamate receptors (mGluR₂), (+)-TFMPIP, inhibits restraint stress-induced phasic glutamate release in rat prefrontal cortex. J Neurochem. 2012 Aug;122(3):619-27. [Content Brief]
- [7]. Kim J, et al. mGluR2/3 in the Lateral Amygdala is Required for Fear Extinction: Cortical Input Synapses onto the Lateral Amygdala as a Target Site of the mGluR2/3 Action. Neuropsychopharmacology. 2015 Dec;40(13):2916-28. [Content Brief]
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mGluR2 Related Products (58)
Related Products (58)
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mGluR2 modulator 2
0 ImagesCat. No.: HY-147528CAS No.: 1004614-86-1mGluR2 modulator 2 (compound 2) is a potent, selective and orally bioavailable mGluR2 positive allosteric modulator with an EC50 value of 0.13 μM. mGluR2 modulator 2 can be used for researching antipsychotic.
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LY3027788 hydrochloride
0 ImagesCat. No.: HY-117606ACAS No.: 1377615-55-8LY3027788 hydrochloride, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 hydrochloride has antidepressant efficacy.
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MGS0028
0 ImagesCat. No.: HY-131287CAS No.: 321963-33-1MGS0028 is a selective metabotropic glutamate 2/3 (mGlu2/3) receptor agonist. MGS0028 can be used for psychiatric disorders research.
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BAY 36-7620
0 ImagesBAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research.
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LBG30300
0 ImagesCat. No.: HY-162117CAS No.: 3086973-64-7LBG30300 is a subtype-selective mGlu2 receptor agonist EC50 0.6 nM. LBG30300 is blood-brain barrier permeable.
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LY 541850
0 ImagesCat. No.: HY-103551ACAS No.: 852679-76-6LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells. LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.
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VU6001192
0 ImagesCat. No.: HY-115782CAS No.: 1821325-29-4VU6001192 is a potent and selective mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator. VU6001192 has potent inhibitory activity against the mGlu2 receptor (IC50 = 207 nM), but no activity against the mGlu3 receptor and the other 6 mGlu subtypes. VU6001192 can be used for the research of neurological disease, such as depression.
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Pomaglumetad methionil anhydrous
0 ImagesCat. No.: HY-14554CAS No.: 635318-55-7Synonyms: LY2140023Pomaglumetad methionil anhydrous (LY2140023) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. LY2140023 has the potential for schizophrenia research.
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MGS0008
0 ImagesCat. No.: HY-131293CAS No.: 234085-20-2MGS0008 is an orally active and brain-penetrant metabotropic glutamate receptor 2/3 (mGlu2/3) agonist with EC50 values of 29.4 nM and 45.4 nM for mGluR2 and mGluR3, respectively. MGS0008 is promising for research of central nervous system disorders, including schizophrenia, anxiety, and neurodegenerative diseases.
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cis-ACPD
0 ImagesCat. No.: HY-19434ACAS No.: 477331-06-9cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively.
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mGluR2 modulator 3
0 ImagesCat. No.: HY-147529CAS No.: 1004614-58-7mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice.
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mGluR2 modulator 4
0 ImagesCat. No.: HY-147530CAS No.: 2582758-47-0mGluR2 modulator 4 (compound 47) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.8 μM. mGluR2 modulator 4 can be used for researching antipsychotic.
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1-Benzyl-APDC
0 ImagesCat. No.: HY-169835CAS No.: 171336-76-8
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LY459477
0 ImagesCat. No.: HY-113981CAS No.: 635318-20-6LY459477 is a potent, selective and orally active metabotropic glutamate 2/3 receptor (mGluR2/3) agonist. LY459477 can effectively suppress Phencyclidine-evoked locomotor activity at doses that do not impair neuromuscular coordination. LY459477 can be used for the research of neurological disease.
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LY2934747
0 ImagesCat. No.: HY-131288CAS No.: 1448707-43-4LY2934747 is a selective and blood-brain barrier-permeable dual mGlu2/mGlu3 receptor agonist, with Ki values of 260 nM and 177 nM, and EC50 values of 8.4 nM and 62.4 nM against human receptors, respectively. LY2934747 exhibits antipsychotic and analgesic activities in in vivo animal models. LY2934747 can be used in studies related to psychosis and pain.
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L-CCG-I
0 ImagesCat. No.: HY-100838ACAS No.: 117857-93-9
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Oxomemazine hydrochloride
0 ImagesOxomemazine hydrochloride is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine hydrochloride is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki= 84 nM, M1 receptor) and low (Ki= 1.65 μM, M2 receptor) affinity sites[1]. Oxomemazine hydrochloride an antihistamine and anticholinergic agent used for the study of cough treatment.
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(RS)-4C3HPG
0 ImagesCat. No.: HY-100840ACAS No.: 134052-66-7Synonyms: 4-Carboxy-3-hydroxyphenylglycine(RS)-4C3HPG (4-Carboxy-3-hydroxyphenylglycine) is an effective competitive antagonist at the metabotropic glutamate receptor 1 (mGluR1) in the central nervous system, and it is also an agonist at mGluR2/3. (RS)-4C3HPG exhibits neuroprotective effects in an acute global ischemia rat model.
