JNJ16259685 is a selective antagonist at the mGlu1 receptors, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.

LY404039 is an inhibitor for mGluR1 (Ki=149 nM) and mGluR2 (Ki= 92 nM), which can also inhibit dopamine receptor.

MPEP HCl is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype with IC50 of 36 nM.

SIB-1757 is a highly selective antagonist for the mGlu5 metabotropic glutamate receptor subtype. SIB-1757 displays an IC50 value of 0.4 μM at hmGlu5 compared with > 30 μM at hmGlu1b, hmGlu2, hmGlu4, hmGlu6, hmGlu7 and hmGlu8.

VU 0364770 is a brain-penetrant and positive allosteric modulator of mGlu4 receptors with EC50 values of 290 nM. It also exhibits affinity for MAO-B and MAO-A with Ki values of 0.72 μM and 8.5 μM, respectively.

LY354740 is a highly potent, efficacious and selective group II (mGlu2/3) receptor agonist, produces > 90% suppression of forskolin-stimulated cAMP formation with an EC50 of 5.1 ± 0.3 nM.

GET-73 is a mGlu5 receptor allosteric modulator potentially for the treatment of alcoholism.

LY 2389575 HCl is a selective negative allosteric modulator of mGlu3 with IC50 of 190 nM.

VU 0361737 is a brain-penetrant and selective positive allosteric modulator of mGlu4 receptors with EC50 values of 240 nM.

JNJ-40411813 is a positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM.

Mavoglurant is a structurally non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5.

CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5.

ABP 688 is a high affinity human mGlu5 receptor antagonist with Ki of 1.7 nM.

NPS 2390 is a Group I mGlu antagonist.

RG7090 is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.

AZD-8529 is a a positive allosteric modulator at the mGluR2 receptor. AZD8529 decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. AZD8529 potentiated agonist-induced activation of mGluR2 in the membrane-binding assay and in primate cortex, hippocampus, and striatum. In monkeys, AZD8529 decreased nicotine self-administration at doses (.3-3 mg/kg) that did not affect food self-administration. AZD8529 also reduced nicotine priming- and cue-induced reinstatement of nicotine seeking after extinction of the drug-reinforced responding. In rats, AZD8529 decreased nicotine-induced accumbens dopamine release. The positive allosteric modulators of metabotropic glutamate receptor 2 should be considered for relapse prevention.

Dipraglurant is a mGluR5 antagonists with IC50 of 0.021 μM.

MPEP HCl is both a selective non-competitive mGlu5 receptor antagonist with IC50 value of 36 nM, and a mGlu4 receptor positive allosteric modulator.

VU 0357121 is a positive allosteric mGlu5 receptors modulator with EC50 value of 33 nM.