BCC4596
VU 0361737
VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.
BCC6975
(RS)-PPG
(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.
BCC7755
CHPG Sodium salt
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..
BCC6610
(RS)-MCPG
(RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.
BCC5691
DCG IV
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: mGlu1/5R=389/630 μM) and III receptors (IC50: mGlu4/6/7/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects.
BCC6611
(S)-MCPG
(S)-MCPG is the active isomer of (RS)-MCPG (Cat.
BCC6969
(2R,4R)-APDC
(2R,4R)-APDC is a selective group II metabotropic glutamate receptors (mGluRs) agonist. (2R,4R)-APDC has anticonvulsant and neuroprotective effects.
BCC6910
CHPG
CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.
BCC6888
E4CPG
E4CPG is a novel group I/group II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG .
BCC6871
EGLU
EGLU ((2S)-α-Ethylglutamic acid; (2S)-α-EGLU) is a potent and competitive mGluR-2 receptor antagonist. EGLU interacts with (lS,3S)-ACPD-sensitive site with a Kd value of 66 μM. EGLU is an antidepressant agent.
BCC7614
LY 354740
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
BCC6895
PHCCC
PHCCC is a Group I metabotropic glutamate receptor antagonist with EC 50 of 6 uM and a positive allosteric modulator of mGluR4. Also as a potent to antagonism for mGluR2 and mGluR8.
BCC6872
CPPG
CPPG ((RS)-CPPG) is a potent group II/III mGlu receptor antagonist. CPPG exhibits some selectivity (approximately 20 fold) for group III (IC50=2.2 nM) over group II (IC50=46.2 nM) mGlu receptors in the rat cerebral cortex. CPPG has weak effects at group I mGlu receptors.
BCC7368
LY 379268
Highly selective group II mGlu agonist
BCC6983
LY 367385
LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects.
BCC6550
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.
BCC4589
Ifenprodil Tartrate
Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM.
BCC5915
Bay 36-7620
Non-competitive mGlu<sub>1</sub> antagonist with inverse agonist activity
BCC7754
Kynurenic acid sodium salt
Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
BCC6578
O-Phospho-L-serine
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.
BCC7332
JNJ 16259685
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.
BCN2228
Kynurenic acid
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
BCC7345
Fenobam
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). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity.
BCC7866
Xanthurenic acid
Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus.
BCC4597
VU 0364770
VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
BCC4590
NMDA (N-Methyl-D-aspartic acid)
NMDA is a specific agonist for NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor.
BCC6801
MSOP
MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
BCC6557
γDGG
gamma-DGG is a competitive AMPA receptor blocker.
BCC6567
(±)-trans-ACPD
trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
BCC4591
MK-801 (Dizocilpine)
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux.
