Catalog No.

Product Name

Application

Product Information

Product Citation

A11382

Dipraglurant

mGluR5 antagonists

Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM.

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A11484

LY341495

mGluR-2 antagonist

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.

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A12589

MPEP

mGlu5 receptor antagonist

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.

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A12705

PHCCC

mGluR antagonist

PHCCC is a group I metabotropic glutamate receptor antagonist (IC50 ~ 3 μM).

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A13236

MPEP HCl

mGlu5 receptor antagonist

MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 uM.

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A13758

SIB 1757

mGluR antagonist

SIB 1757 is a highly selective antagonist for the mGlu5 metabotropic glutamate receptor subtype.

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A13759

SIB 1893

mGluR antagonist

SIB 1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype.

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A13854

A-841720

mGluR-1 antagonist

A 841720 is a potent, non-competitive mGluR-1 antagonist that displays 34-fold selectivity over mGluR-5 (IC50 values are 10 and 342 nM respectively).

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A15174

MTEP hydrochloride

mGlu5 antagonist

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

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A15378

DL-AP3

mGluR1 antagonist

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.

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A19152

LY3020371 hydrochloride

mGlu2/3 antagonist

LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM.

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A19729

AZD 2066

mGluR5 antagonist

AZD 2066 is a selective, orally active and brain-penetrant mGluR5 antagonist, with analgesia activity.

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A19738

AZD 9272

mGluR5 antagonist

AZD 9272 is a brain penetrant mGluR5 antagonist.

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A20372

Fenobam

mGluR5 antagonist

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).

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A20495

MSOP

group III mGluR antagonist

MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.

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A20545

JNJ16259685

mGlu1 receptor antagonist

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

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A20549

(S)-MCPG

group I/group II mGluR antagonist

(S)-MCPG is the active isomer of (RS)-MCPG, non-selective group I/group II metabotropic glutamate receptor antagonist.

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A20554

FTIDC

mGluR 1 antagonist

FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a.

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A20567

CFMTI

mGluR 1 allosteric antagonist

CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist with IC50 of 2.6 nM.

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A20674

FPTQ

mGluR1 antagonist

FPTQ is mGluR1 antagonist with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1 respectively.

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A20804

E4CPG

group I/group II mGluR antagonist

E4CPG is a novel group I/group II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG .

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A20818

(RS)-MCPG

group I/group II mGluR antagonist

(RS)-MCPG is a non-selective group I/group II metabotropic glutamate receptor antagonist.

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A20958

Auglurant

mGlu5 antagonist

Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.

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A21223

Mavoglurant

mGlu5 receptor antagonist

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

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A21651

LY 541850

mGlu2 agonist/mGlu3 antagonist

LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.

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A21799

Mavoglurant racemate

mGlu5 receptor antagonist

Mavoglurant (racemate) is the racemate of mavoglurant. Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist.

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A21899

Methoxy-PEPy

mGlu5 receptor antagonist

Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.

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A22629

CPCCOEt

mGluR1b antagonist

CPCCOEt is a low affinity, selective, non-competitive antagonist of the metabotropic glutamate receptor subtype mGluR1b.

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A22631

NPS2390

group I mGlu antagonist

NPS2390 is a group I mGlu antagonist. It displays noncompetitive antagonist activity at both mGlu1 and mGlu5 receptors. NPS2390 is thought to act on a site separate from the glutamate binding pocket.

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Metabotropic glutamate receptors (mGluR)