mglu4

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].

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.

L-APB is an effective and specific agonist for the group III mGluRs (EC50s: 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6, and mGlu7 receptors, respectively).

Valiglurax (VU2957), also known as VU0652957 and VU2957, is a potent, selective, CNS penetrant, and orally bioavailable mGlu4 PAM. VU2957 possessed attractive in vitro and in vivo pharmacological and DMPK properties across species. VU2957 was evaluated as a preclinical development candidate for the treatment of Parkinson's disease.

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

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.

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

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).

VU0364770 hydrochloride is a potent and selective mGlu4 positive allosteric modulator (PAM) (EC50s: 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively).

VU6001376 is an effective and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (EC50: 50.1 nM).

VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively.

mGlu4 receptor agonist

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.

VU0415374 is a positive allosteric modulator of mGlu4.

FP0429 is an agonist of mGlu4.

LSP1-2111 is a mGlu4 receptor subtype agonist.

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).

VU0418506 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGlu4).

VU0477886 is a potent mGlu4 positive allosteric modulator (PAM) with robust efficacy in a standard preclinical Parkinson's disease model, haloperidol-induced catalepsy (HIC).

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

L-AP4 (L-APB) monohydrate is a potent and specific agonist for group III mGluRs, with EC50s of 0.13, 0.29, 1.0, and 249 μM for mGlu4, mGlu8, mGlu6, and mGlu7 receptors, respectively [1][2].

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