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 관련 제품 (34)
관련 제품 (34)
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Cinnabarinic acid
0 ImagesCinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.
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L-AP4
0 ImagesSynonyms: L-APBL-AP4 (L-APB) 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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VU0422288
0 ImagesSynonyms: ML396VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice.
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ADX88178 TFA
0 ImagesCat. No.: HY-18654AADX88178 TFA is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC50 of 3.5 nM against hmGluR4. ADX88178 TFA modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 TFA reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 TFA can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease.
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Quisqualic acid
0 ImagesSynonyms: L-Quisqualic acid
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VU0483605
0 ImagesCat. No.: HY-100605CAS No.: 1623101-11-0VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively.
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Lu AF21934
0 ImagesLu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.
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DCG-IV
0 ImagesDCG-IV is a potent agonist of group II mGluRs with EC50s of 0.35 and 0.09 μM for mGlu2R and mGlu3R, reapectively. DCG-IV is also a competitive antagonist at group I (IC50: mGlu1R/5R=389/630 μM) and III receptors (IC50: mGlu4R/6R/7R/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects.
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VU0364770
0 ImagesVU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 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 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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VU0361737
0 ImagesSynonyms: ML-128VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.
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