mGluR8 Agonist

L-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.

L-Cysteinesulfinic acid is a potent agonist at several 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.

L-Cysteinesulfinic acid monohydrate is a potent agonist at several 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.

VU6005649 is a blood-brain-barrier penetrant mGlu_7/8 receptor agonist with EC₅₀s of 0.65 μM and 2.6 μM for mGlu₇ receptor and mGlu₈ receptor, respectively.

DCG-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.

(S)-3,4-DCPG is a selective agonist of metabotropic glutamate receptor 8a (mGluR8a) with an EC₅₀ of 31 nM in AV12-664 cells expressing human mGluR8.

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

LSP4-2022 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.

L-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.

LBG30300 is a subtype-selective mGlu₂ receptor agonist EC₅₀ 0.6 nM. LBG30300 is blood-brain barrier permeable.