Metabotropic glutamate receptors (mGluR)

ADX-47273 is a drug used in scientific research which acts as a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5.

LY 341495 has been shown to be a highly potent and selective group II metabotropic glutamate receptor (mGluR-2) antagonist with Ki / IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGluR-2, mGluR-3, mGluR-8 , mGluR-7a, mGluR-1a, mGluR-5a and mGluR-4a.

VU 0361737 is a selective positive allosteric modulator at mGluR-4 (EC50 values are 240 and 110 nM at human and rat receptors respectively).

MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors.

VU 0364439 is a positive allosteric modulator (PAM) of mGlu4 receptors (EC50 = 19.8 nM in vitro for human mGlu4).

CPPHA is a selective positive allosteric modulator of mGluR5 receptor.

MTEP hydrochloride is a potent, selective and non-competitive mGlu5 antagonist with IC50 and Ki of 5 nM and 16 nM, respectively.

DL-AP3, a racemic preparation of D-AP3 and L-AP3, is an inhibitor of phosphoserine phosphatase and an antagonist of the metabotropic glutamate receptor (mGluR), blocking phosphoinositide turnover mediated by the mGluR.

Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).

O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.

TCN238 is a positive allosteric mGlu4 receptor modulator with an EC50 of 1 μM.

Ro0711401 is a mGlu1 receptor agonist.

YM 298198 Hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM).