mGluR Antagonist

CPPG ((RS)-CPPG) is a potent group II/III mGlu receptors 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.

(S)-MCPG ((+)-MCPG) is a potent group I/II metabotropic glutamate receptor (mGluRs) antagonist and the active isomer of (RS)-MCPG (HY-100371). (S)-MCPG can be used for the study of the function of mGluRs in spatial learning.

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

DL-AP4 (2-Amino-4-phosphonobutyric acid) is a glutamate antagonist. DL-AP4 behaves as a competitive inhibitor of glutamate binding with an apparent K_d of 66 μM. DL-AP4 can be used for the research of central nervous system and visual system.

β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (K_i=1 µM) that protects spinal cord neurons from excitotoxicity and hypoxic damage. β-Spaglumic acid is also a selective mGluR3 antagonist (mGluR3 receptor functions to regulate activity-dependent synaptic potentiation in the hippocampus). β-Spaglumic acid can be used in neuroprotection-related studies.

(E/Z)-SIB-1893 is a racemic compound of (E)-SIB-1893 and (Z)-SIB-1893 isomers. (E)-SIB-1893 is a selective non-competitive metabotropic glutamate subtype 5 receptor (mGluR5) antagonist.

(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.

XAP044 is a potent and selective antagonist of mGlu7. The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms.

PHCCC is a Group I mGluR antagonist with an IC₅₀ of 3 μM. PHCCC is a selective positive modulator of mGlu4 receptor. Antiparkinsonian effect.

LY456066 is a selective non-competitive metabotropic glutamate receptors (mGluR1) antagonist with an IC₅₀ value of 52.0 nM. LY456066 is effective in rodent models of anxiolysis and nociception. LY456066 reduces hyperalgesia and the amount of licking and flinching following formalin injection, which is promising for research of analgesics for chronic pain.

mGluR5 antagonist-1 is an orally active mGluR5 antagonist with an IC₅₀ value of 11.5 nM. mGluR5 antagonist-1 has anti-depressant effect. mGluR5 antagonist-1 can be used for the study of depressive disorder.

E4CPG ((RS)-ECPG) is a Group I/Group II metabotropic glutamate receptor (mGluR) antagonist. E4CPG can inhibit the paired-pulse ratio of monosynaptic inhibitory postsynaptic currents (IPSC) potentiation.

ACDPP is a specific mGluR5 antagonist. ACDPP partially bolcks the increase of fragile X mental retardation protein (FMRP) caused by DHPG (HY-12598A) (group I mGluR Agonist).

VU0285683 is a selective mGluR5 positive allosteric modulator (PAM). VU0285683 has anxiolytic-like activity in rodent models for anxiety.

(±)-LY367385 is the racemate of LY367385. 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.

(RS)-4CPG ((RS)-4-Carboxyphenylglycine) is a type I metabotropic glutamate receptor antagonist with activity in blocking LTP induction. In mice lacking IP3R1, (RS)-4CPG (500μM) nearly blocked long-term potentiation (LTP) induced by type I metabotropic glutamate receptor activation, with LTP of 117.6±1.7% (n = 8) in IP3R1(-/-) mice and 116.9±1.8% (n = 5) in IP3R1(+/+) mice.

L-AP3, metabotropic glutamate receptor (mGluR) antagonist, inhibits D-phosphoserine and L-phosphoserine with IC₅₀s of 368 μM and 2087 μM, respectively.

IEM-1925 bromide is an orally active glutamate receptor antagonist, increases the latent period and decreases the duration of status epilepticus in rats in a lithium-pilocarpine model of epilepsy.

Desmethyl-YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC₅₀: 16 nM). Desmethyl-YM-298198 hydrochloride has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice.

UBP 1112 is a selective group III mGluR antagonist, with a K_d of 5.1 μM.UBP 1112 shows 96-fold affinity for group III over group II mGlu receptor (K_d, 488 μM), and shows no significant activity at group I mGlu receptor or iGlu receptor.