|Description||Dipraglurant is a mGlu5 receptor negative allosteric modulator. It is currently in phase II for the treatment of dyskinesia in Parkinson's disease.|
Mavoglurant is a structurally novel, non-competitive mGlu5 receptor antagonist (IC50=30 nM), as a a selective non-competitive antagonist.
MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibiting no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.
Potent and selective antagonist for metabotropic glutamate receptor subtype 5 (mGluR5); Systemically active in vivo.
(±)-LY367385 is a selective mGlu1a antagonist.
ML337 is a Selective negative allosteric modulator of mGlu3 with IC50 value of 593 nM. It shows no activity at mGlu1, mGlu2 or mGlu4-8 at concentrations up to 3...
JNJ-42153605 is a selective positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor (EC50= 17 Nm) with an acceptable pharmacokinetic prof...
FITM is a potent mGlu1 inhibitor (Ki = 2.5 nM) with great selectivity that does not disrupt mGlu5.
CTEP is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor (IC50=2.2 nM), showing >1000-fold selectivity over other mGlu receptor...
LY-404,039, also known as pomaglumetad, is an amino acid analog drug that acts as a highly selective agonist for the metabotropic glutamate receptor group II su...
Lu AF21934 is a selective and brain-penetrating positive allosteric modulator (PAM) of mGlu4 receptors (IC50= 500 nM) on the harmaline-induced tremor and other ...
A 841720 is a potent non-competitive mGlu1 receptor antagonist (IC50 = 10 nM) exhibiting 34-fold selectivity over mGluR5 and inactive to other mGluR receptors, ...
TCN238 is an orally available, brain penetrant and positive allosteric mGlu4 receptor modulator (EC50= 1 μM) with 30-fold selectivity over mGluR5 using human re...
(1R,2S)-VU0155041 is a partial mGluR4-positive allosteric modulator (EC50= 2.35 μM) that dependently attenuated hyperalgesia in neuropathic pain model rats.
BAY 36-7620 elective mGlu1 receptor non-competitive antagonist (IC50 = 0.16 μM) with inverse agonist activity.
Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist.
Glutamate, the major excitatory neurotransmitter in the brain, acts on both ionotropic and metabotropic glutamate receptors. Excessive metabotropic glutamate re...
JNJ-40411813 is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM.
VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.
Topiramate is a kainate GluR5 receptor antagonist,originally used as an anticonvulsant.