mGluR4
mGluR4 is a family C GPCR that modulates synaptic transmission and neuronal excitability[1]. Mechanistically, human mGlu2 and mGlu4 couple to heterotrimeric Gᵢ protein through a distinct intracellular-loop and helix III/IV binding site, supporting class C GPCR signaling studies[2]. In basal ganglia research, mGluR4 activation modulates neurotransmission and produces antiparkinsonian effects in rodent models[3]. Compared with related isoforms, α-synuclein preformed fibril binding was specific for mGluR4, while mGluR1, mGluR3, mGluR5, mGluR7, and mGluR8 were negative in the same assay[4]. In colorectal carcinoma, mGluR4 signaling may play a role in tumor biology, and overexpression associates with poor prognosis[5]. For experimental applications, VU0155041 acts as a mixed allosteric agonist/PAM, whereas ADX88178 is a potent, selective mGluR4 PAM useful for Parkinson’s disease model studies[3][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]. Lin S, et al. Structures of Gi-bound metabotropic glutamate receptors mGlu2 and mGlu4. Nature. 2021 Jun;594(7864):583-588. [Content Brief]
- [3]. Niswender CM, et al. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol. 2008 Nov;74(5):1345-58. [Content Brief]
- [4]. Perez-Canamas A, et al. mGluR4-NPDC1 complex mediates α-synuclein fibril-induced neurodegeneration. Nat Commun. 2025 Dec 25;17(1):994. [Content Brief]
- [5]. Chang HJ, et al. Metabotropic glutamate receptor 4 expression in colorectal carcinoma and its prognostic significance. Clin Cancer Res. 2005 May 1;11(9):3288-95. [Content Brief]
- [6]. Le Poul E, et al. A potent and selective metabotropic glutamate receptor 4 positive allosteric modulator improves movement in rodent models of Parkinson's disease. J Pharmacol Exp Ther. 2012 Oct;343(1):167-77. [Content Brief]
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mGluR4 Related Products (34)
Related Products (34)
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TCN238
0 ImagesTCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM.
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(1R,2S)-VU0155041
0 ImagesCat. No.: HY-14417ACAS No.: 1263273-14-8(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
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LSP4-2022
0 ImagesLSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity.
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L-AP4 monohydrate
0 ImagesSynonyms: L-APB monohydrateL-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
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VU0364770 hydrochloride
0 ImagesVU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
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VU6001376
0 ImagesCat. No.: HY-112814CAS No.: 1968546-34-0VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM.
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Foliglurax
0 ImagesCat. No.: HY-108703CAS No.: 1883329-51-8Synonyms: PXT002331Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM. Antiparkinsonian effect.
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mGlu4 receptor agonist 1
0 ImagesCat. No.: HY-144698CAS No.: 1678501-16-0mGlu4 receptor agonist 1 (compound 62) is a potent mGlu4 receptor positive allosteric modulator, with an EC50 of 308 nM. mGlu4 receptor agonist 1 shows significant anxiolytic- and antipsychotic-like effect.
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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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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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VU0155041 sodium
0 ImagesCat. No.: HY-14417BCAS No.: 1259372-69-4VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).
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VU0400195
0 ImagesCat. No.: HY-120567CAS No.: 1309434-83-0Synonyms: ML182VU0400195 (ML182) is a oral active and allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4) with the EC50 of 291 nM. VU0400195 can be used for study of antiparkinsonian animal model.
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PXT-012253
0 ImagesCat. No.: HY-167899CAS No.: 1835647-08-9PXT-012253 is a positron emission tomography (PET) ligand for mGluR4, as it binds to an allosteric site on mGluR4. PXT-012253 can be utilized in researches related to Parkinson's disease and levodopa-induced dyskinesia.
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