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.

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

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

VU 0364439 is an mGlu4 positive allosteric modulator (C50: 19.8 nM).

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.

ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4.

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

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.

LSP4-2022 is a selective, blood-brain barrier-permeable mGlu4 orthosteric agonist (EC50 = 0.11 μM) capable of inhibiting neurotransmission in wild-type mouse cerebellar slices, exhibiting pro-depressive activity.

DCG-IV is an effective agonist of class II mGluR. DCG-IV has anticonvulsant and neuroprotective effects. The EC50 of mGlu2R and mGlu3R are 0.35 and 0.09 μM, respectively. DCG-IV is also a competitive antagonist of Group I (IC50: mGlu1 / 5R = 389/630 μM) a

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.

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.

(S)-3,5-DHPG is a weak but selective agonist of group I metabotropic glutamate receptors with Ki values of 0.9 μM for mGluR1a and 3.9 μM for mGluR5a. (S)-3,5-DHPG demonstrates anxiolytic activity in hypoxia-exposed rats, supporting its application in neuropharmacological studies of glutamatergic signaling, stress responses, and anxiety-related behaviors.

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].

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).

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).

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].

mGlu4 receptor agonist 1 (compound 62) is a potent positive allosteric modulator of mGlu4 receptors, with an EC50 of 308 nM, and exhibits significant anxiolytic and antipsychotic properties [1].

Quisqualic acid is a natural glutamate analog and a potent, non-selective agonist for two subsets of excitatory amino acid (EAA) receptor subtypes, namely iGluR and mGluR.

TCN238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4with an EC50 of 1 μM).

(RS)-PPG is a potent and selective group III mGluRs agonist (EC50s of 5.2 μM, 4.7 μM, 185 μM, and 0.2 μM for hmGluR4a, hmGluR6, hmGluR7b, and hmGluR8a, respectively), with neuroprotective and anticonvulsive activity.