mglur4

VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.

3-MATIDA is an effective mGluR-1 antagonist (IC50: 6.3 μM, rat mGluR-1a). Displays ≥ 40-fold selectivity over other receptors: mGluR-5, mGluR-2, mGluR-4 (mGluR-4a) (IC50 > 300 μM), NMDA and GluR (AMPA) (IC50 = 250 μM). 3-MATIDA act as a neuroprotectant in cultured murine cortical cells and rat hippocampal slice cultures in vitro.

VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of the mGlu4 receptor with an EC50 of 240 nM for human receptors and 110 nM for rat receptors. It exhibits weak activity at mGlu5 and mGlu8 receptors and is inactive at mGlu1, mGlu2, mGlu3, mGlu6, and mGlu7 receptors. The compound can penetrate the CNS.

Foliglurax monohydrochloride Antiparkinsonian effect. is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM.

Foliglurax is a highly selective brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) (EC50: 79 nM).

L-Cysteinesulfinic acid is an endogenous neurotransmitter with agonistic effects on a variety of metabotropic glutamate receptors (mGluRs), including mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, with a pEC50 = 2.7 to 4.0. L- Cysteinesulfinic acid is a pld-coupled agonist of metabotropic excitatory amino acid (EAA) receptors.

(1R,2S)-VU0155041 is the cis regioisomer of VU0155041 and a partial agonist of mGluR4.

GYKI 53655 hydrochloride (LY300168 hydrochloride) is an antagonist of AMPA and is used in the study of neurological disorders.

LY341495 is a potent metabotropic glutamate receptor antagonist that exhibits high activity against a wide range of glutamate receptor subtypes and can be used for the study of neurological disorders.

(E)-PHCCC, acting as a positive allosteric modulator (PAM) of the mGluR4, enhances the activity of the receptor's endogenous ligand (glutamate). It demonstrates activity in a calcium mobilization assay in CHO cells, with an EC50 of 3.2 μM.

PXT-012253 is a positron emission tomography (PET) ligand targeting mGluR4, designed to bind to its allosteric sites. This compound is useful for research related to Parkinson's disease and levodopa-induced movement disorders.

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases.

VU0155041 sodium is a positive allosteric modulator of mGluR4, promoting extinction in male rats and inhibiting the recovery of morphine-induced conditioned place preference. It alleviates hyperalgesia in nerve injury pain models, useful in neurodegenerative disease research.

VU-29 is a positive allosteric mGlu5 receptor modulator with an EC50 of 9 nM and a Ki of 244 nM for rmGluR5. It is selective for mGluR5 relative to other mGluR subtypes [EC50: rmGluR1 rmGluR2=557 nM 1.5 μM; hmGluR4=154 nM].

LSP4-2022, a mGlu4 selective agonist, increases behavioral despair in mouse models of antidepressant action.

VU0080241 is a positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4).

VU0359516 is a mGluR4 positive allosteric modulators.

VU0410150, a pyrrylarylsulfone containing compound, has been found to be a mGluR4-positive allosteric modulator and has been evaluated as a potential drug for the treatment of Parkinson's disease.

VU0422288 (ML396) is a potent orthosteric modulator of type III mGlu receptors (mGlus).VU0422288 shows inhibition of mGluR4, mGluR7, and mGluR8 in a calcium mobilization assay.VU0422288 can be used to study Rett syndrome (RTT).

PHCCC ((-) PHCCC) is a Group I metabotropic glutamate receptor antagonist and a positive allosteric modulator of mGluR4. It also is a potent to antagonism for mGluR2 and mGluR8.

trans-ACPD ((±)-trans-ACPD) is an equimolecular mixture of (1S, 3R)- and (1R, 3S)-ACPD. trans-ACPD is a selective agonist of the mGluR (metabotropic glutamate receptor); active at the group I II mGlu receptors (EC50: 2 15 23 800 μM, mGluR2 1 5 4).

Lu AF21934 is a brain-penetrant and selective mGlu4 receptor positive allosteric modulator (IC50: 500 nM, human).

VU0155041 is an effective and positive allosteric modulator allosteric agonist at mGlu4 receptors (EC50: 798 693 nM, at human rat).

L-Cysteinesulfinic acid monohydrate is a potent agonist at rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively [1].