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Results for "

mGluR

" in MCE Product Catalog:

By Targets:	mGluR (102) Akt (2) Aminopeptidase (2) CaSR (1) Endogenous Metabolite (5) ERK (2) iGluR (2) NF-κB (2) Phosphatase (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (2) Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (94)

102

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: mGluR

Cat. No.	Product Name	Target	Research Areas

HY-141832

mGluR5 modulator 1	mGluR	Neurological Disease
mGluR5 modulator 1 is a *mGluR5* positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments.

HY-147530

mGluR2 modulator 4	mGluR	Neurological Disease
mGluR2 modulator 4 (compound 47) is a potent *mGluR2* positive allosteric modulator with an EC₅₀ value of 0.8 μM. mGluR2 modulator 4 can be used for researching antipsychotic.

HY-147528

mGluR2 modulator 2	mGluR	Neurological Disease
mGluR2 modulator 2 (compound 2) is a potent, selective and orally bioavailable *mGluR2* positive allosteric modulator with an EC₅₀ value of 0.13 μM. mGluR2 modulator 2 can be used for researching antipsychotic.

HY-130630

mGluR2 modulator 1	mGluR	Neurological Disease
mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated *mGluR2* (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC₅₀ of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research.

HY-147529

mGluR2 modulator 3	mGluR	Neurological Disease
mGluR2 modulator 3 (compound 1) is a potent *mGluR2* positive allosteric modulator with an EC₅₀ value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice.

HY-133555

mGluR2 antagonist 1	mGluR	Neurological Disease
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of *mGluR2* negative allosteric modulator (IC₅₀ of 9 nM) with excellent brain permeability.

HY-15445

CTEP RO 4956371; mGluR5 inhibitor	mGluR	Neurological Disease
CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC₅₀ of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.

HY-100372

E4CPG (RS)-ECPG	mGluR	Neurological Disease
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.

HY-19434A

cis-ACPD	iGluR mGluR	Neurological Disease
cis-ACPD is a potent agonist of NMDA receptor, with an IC₅₀ of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC₅₀s of 13 μM and 50 μM for *mGluR2* and *mGluR4*, respectively.

HY-101332

EGLU (2S)-α-Ethylglutamic acid; (2S)-α-EGLU	mGluR	Neurological Disease
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 K_d value of 66 μM. EGLU is an antidepressant agent.

HY-100838A

L-CCG-I	mGluR	Metabolic Disease
L-CCG-I is an extended isomer of conformationally restricted glutamate analog. L-CCG-I also is a potent agonist for *mGluR2* with an EC₅₀ value of 0.3 nM. L-CCG-I can be used for the research of mGluR family.

HY-103572

MNI137	mGluR	Neurological Disease
MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC₅₀s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization.

HY-108546

L-AP3 3-Phosphono-L-alanine	mGluR	Neurological Disease
L-AP3, metabotropic glutamate receptor (mGluR) antagonist, inhibits D-phosphoserine and L-phosphoserine with IC₅₀s of 368 μM and 2087 μM, respectively.

HY-122255

LY487379	mGluR	Neurological Disease
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [³⁵S]GTPγS binding with EC₅₀ values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research.

HY-103552

LY487379 hydrochloride	mGluR	Neurological Disease
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [³⁵S]GTPγS binding with EC₅₀ values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research.

HY-15129

O-Phospho-L-serine L-Serine O-phosphate; L-SOP	mGluR Endogenous Metabolite	Neurological Disease
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*.

HY-100804

L-Cysteinesulfinic acid	mGluR Endogenous Metabolite	Neurological Disease
L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC₅₀s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.

HY-W017230

L-Cysteinesulfinic acid monohydrate	mGluR Endogenous Metabolite	Neurological Disease
L-Cysteinesulfinic acid monohydrate is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC₅₀s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.

HY-15129S

O-Phospho-L-serine-13C3,15N L-Serine O-phosphate-¹³C₃,¹⁵N; L-SOP-¹³C₃,¹⁵N	mGluR Endogenous Metabolite	Neurological Disease
O-Phospho-L-serine-¹³C₃,¹⁵N is the ¹³C- and ¹⁵N-labeled 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[1].

HY-50906

LY404039	mGluR	Neurological Disease
LY404039 is a potent, selective and orally active *mGluR2* and *mGluR3* agonist with K_is of 149 nM and 92 nM for recombinant human mGluR2 and *mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR*2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects.

HY-12598A

DHPG (RS)-3,5-DHPG	mGluR	Neurological Disease
DHPG ((RS)-3,5-DHPG) is an amino acid, which acts as a selective and potent agonist of group I mGluR (mGluR 1 and mGluR 5), shows no effect on Group II or Group III mGluRs. DHPG ((RS)-3,5-DHPG) is also an effective antagonist of mGluRs linked to phospholipase D.

HY-107507

Ro 01-6128
mGluR Neurological Disease

Ro 01-6128 is a positive allosteric modulator of mGluR1.

Ro 01-6128	mGluR	Neurological Disease
Ro 01-6128 is a positive allosteric modulator of *mGluR1*.

HY-100405

FTIDC	mGluR	Neurological Disease
FTIDC is an orally active, noncompetitive, selective allosteric *metabotropic glutamate receptor (mGluR) 1* antagonist with an IC₅₀ of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1.

HY-11095

NPS 2390	mGluR CaSR	Neurological Disease Cardiovascular Disease
NPS 2390 is a noncompetitive antagonist of mGluR1 and mGluR5. NPS 2390 is also a potent CaSR (calcium-sensing receptor) inhibitor.

HY-14612

CPPHA	mGluR	Neurological Disease
CPPHA is potent and selective positive allosteric modulator (PAM) of the *mGluR5* and *mGluR1* (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders.

HY-110190

VU0422288 ML396	mGluR	Neurological Disease
VU0422288 (ML396) is a positive allosteric modulator of group III *mGluRs. VU0422288 inhibits mGluRs* with EC₅₀s of 125 nM, 146 nM, and 108 nM for *mGluR4, mGluR7, and mGluR8*, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice.

HY-121848

VU0155094
ML397
mGluR Neurological Disease

VU0155094 is a positive allosteric modulator with differential activity at the various group III mGluRs.

VU0155094 ML397	mGluR	Neurological Disease
VU0155094 is a positive allosteric modulator with differential activity at the various group III mGluRs.

HY-107516

(S)-3,4-DCPG (S)-3,4-Dicarboxyphenylglycine	mGluR	Neurological Disease
(S)-3,4-DCPG is a selective agonist of metabotropic glutamate receptor 8a (mGluR8a) with an EC₅₀ of 31 nM in AV12-664 cells expressing human mGluR8.

HY-16766

Decoglurant
RO4995819
mGluR Neurological Disease

Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant.

Decoglurant RO4995819	mGluR	Neurological Disease
Decoglurant (RO4995819) is a negative allosteric modulator of *mGluR2* and *mGluR3*. Decoglurant is developed as an antidepressant.

HY-131286A

Talaglumetad hydrochloride LY-544344 hydrochloride	mGluR	Neurological Disease
Talaglumetad hydrochloride is a prodrug of thetype II metabotropic glutamate receptor (mGluR2/3) agonist Eglumegad for the treatment of anxiety.

HY-18654

ADX88178
mGluR Neurological Disease

ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC₅₀ of 4 nM for human mGluR4.
HY-101356

CPCCOEt
mGluR Neurological Disease

CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of metabotropic glutamate receptor 1b (mGluR1b).

ADX88178	mGluR	Neurological Disease
ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC₅₀ of 4 nM for human mGluR4.

CPCCOEt	mGluR	Neurological Disease
CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of metabotropic glutamate receptor 1b (mGluR1b).

HY-12598

(S)-3,5-DHPG	mGluR	Neurological Disease
(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with K_i values of 0.9 µM and 3.9 µM for mGluR1a and mGluR5a, respectively. (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia.

HY-103561

DCB	mGluR	Neurological Disease
DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB).

HY-110122

AZ 12216052	mGluR	Neurological Disease
AZ 12216052 is a *mGluR8* positive allosteric modulator, and helps *mGluR8* modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect.

HY-110254

AZD 9272
mGluR Neurological Disease

AZD 9272 is a brain penetrant mGluR5 antagonist.

AZD 9272	mGluR	Neurological Disease
AZD 9272 is a brain penetrant *mGluR5* antagonist.

HY-100382

FPTQ	mGluR	Others
FPTQ is potent *mGluR₁* antagonist with IC₅₀ values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo.

HY-100786

DL-AP3	Endogenous Metabolite mGluR Phosphatase	Cancer Neurological Disease
DL-AP3 is a competitive *mGluR1* and *mGluR5* antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect.

HY-114863

PHCCC(4Me) THCCC	mGluR	Neurological Disease
PHCCC(4Me) (THCCC), a PHCCC analog, is a dual *mGluR2* (IC₅₀ of 1.5 μM) negative allosteric modulator and *mGluR3* (EC₅₀ of 8.9 μM) positive allosteric modulator.

HY-103575A

MFZ 10-7 hydrochloride	mGluR	Neurological Disease
MFZ 10-7 hydrochloride is a highly potent and selective *mGluR5* NAM (negative allosteric modulator), with a K_i of 0.67 nM for rat mGluR5. MFZ 10-7 hydrochloride inhibits cocaine-taking and cocaine-seeking behavior in rats.

HY-14417

VU0155041	mGluR	Neurological Disease
VU0155041 is a potent, selective positive allosteric modulator (PAM) of *mGluR4, with EC₅₀s of 798 nM and 693 nM for human and rat mGluR*4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).

HY-14417B

VU0155041 sodium	mGluR	Neurological Disease
VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of *mGluR4, with EC₅₀s of 798 nM and 693 nM for human and rat mGluR*4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD).

HY-12597

Quisqualic acid L-Quisqualic acid	iGluR mGluR	Neurological Disease
Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and *mGluR) of excitatory amino acid (EAA) agonist with an EC₅₀* of 45 nM and a K_i of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis indica.

HY-100406

(S)-MCPG (+)-MCPG	mGluR	Neurological Disease
(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.

HY-107457

AZD-8529	mGluR	Neurological Disease
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of *mGluR2, with an EC₅₀* of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

HY-103565

AMN082	mGluR	Neurological Disease
AMN082, a selective, orally active, and brain penetrant *mGluR7* agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC₅₀ values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.

HY-101247

MTPG	mGluR	Neurological Disease
MTPG is a potent *mGluR2* and *mGluR3* antagonist. MTPG can block the induction of brain ischemic tolerance induced by cerebral ischemic preconditioning. MTPG also significantly attenuates the inhibitory effect of L-CCG-1 on the KCl-evoked dopamine release.

HY-14569

CDPPB	mGluR	Neurological Disease
CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC₅₀ of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.

HY-107457A

AZD-8529 mesylate	mGluR	Neurological Disease
AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of *mGluR2, with an EC₅₀* of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

HY-110304

NPEC-caged-LY379268
mGluR Neurological Disease

NPEC-caged-LY379268 is a type II mGluR agonist.

HY-103565A

AMN082 free base	mGluR	Neurological Disease
AMN082 free base, a selective, orally active, and brain penetrant *mGluR7* agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC₅₀ values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.

HY-101164

MAP4
mGluR Neurological Disease

MAP4 is a selective group III mGluR antagonist in some electrophysiological systems.

HY-141848A

(S,S)-BMS-984923	mGluR	Neurological Disease
(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC₅₀ >1μM for mGluR5 receptor. BMS-984923 is a potent mGluR5 silent allosteric modulator.

HY-103111

MMPIP hydrochloride	mGluR	Neurological Disease
MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (K_B values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.

HY-107503

MMPIP	mGluR	Neurological Disease
MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (K_B values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.

HY-13058B

(R)-ADX-47273
mGluR Neurological Disease

(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC₅₀ of 168 nM for potentiation .

HY-122559

BMS-984923	mGluR	Neurological Disease
BMS-984923, a potent *mGluR5* silent allosteric modulator (SAM), with exquisite binding affinity (K_i = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling.

HY-100728

BMT-145027
mGluR Neurological Disease

BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC₅₀ of 47 nM.
HY-15442

Biphenylindanone A
BINA
mGluR Neurological Disease

Biphenylindanone A (BINA) is a selective human mGluR2 (hmGluR2) potentiator for the treatment of many neurological disorders.
HY-103573

VU 0360223
mGluR Neurological Disease

VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC₅₀ of 61 nM.

HY-14418

VU0361737 ML-128	mGluR	Neurological Disease
VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR₄ PAM), with EC₅₀s of 240 nM and 110 nM for human and rat mGluR₄ receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.

HY-15257

Mavoglurant AFQ056	mGluR	Neurological Disease
Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active *mGluR5* antagonist, with an IC₅₀ of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinson's disease.

HY-110255

AZD 2066
mGluR Neurological Disease

AZD 2066 is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 has antinociception effects.
HY-110255A

AZD 2066 hydrate
mGluR Neurological Disease

AZD 2066 hydrate is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 hydrate has antinociception effects.

HY-130553

β-Spaglumic acid β-NAAG; β-N-Acetylaspartylglutamic acid	Aminopeptidase mGluR	Neurological Disease
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.

HY-119078

VU0080241
mGluR Neurological Disease

VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC₅₀ of 4.6 μM.
HY-101375

(RS)-APICA
mGluR Neurological Disease

(RS)-APICA is a selective group II metabotropic glutamate receptor (mGluR II) antagonist. (RS)-APICA shows potential neuroprotective effect.
HY-101226

MSOP
mGluR Neurological Disease

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

HY-107508

VU-29	mGluR	Neurological Disease
VU-29 is a positive allosteric modulator of *metabotropic glutamate 5 (mGlu5) receptor* (EC₅₀=9 nM and K_i=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC₅₀: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).

HY-16951

VU-1545
mGluR Neurological Disease

VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a K_i of 156 nM and an EC₅₀ of 9.6 nM.
HY-100409

PHCCC
mGluR Cancer

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

HY-100403

Ro 67-7476	mGluR	Cancer
Ro 67-7476 is a potent positive allosteric modulator of *mGluR₁* and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC₅₀ of 60.1 nM. Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC₅₀=163.3 nM).

HY-14417A

(1R,2S)-VU0155041
mGluR Neurological Disease

(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC₅₀ of 2.35 μM.
HY-101387

rel-ACPT-I
mGluR

rel-ACPT-I is an agonist of group III mGluRs with diverse biological activities including neuroprotective, anticonvulsant, and anxiolytic-like effects.

HY-103559

HexylHIBO	mGluR	Neurological Disease
HexylHIBO is a potent group I mGluR antagonist with Kbs of 140 and 110 μM at mGlu_1a and mGlu_5a receptors, respectively. HexylHIBO decreased sEPSC in rat.

HY-100402

CFMTI
mGluR Cancer

CFMTI inhibits L-glutamate-induced intracellular Ca²⁺ mobilization in CHO cells expressing human and rat mGluR1a, with IC₅₀s of 2.6 and 2.3 nM, respectively.

HY-110141

ABP688	mGluR	Others
ABP688 is a high affinity human mGluR5 antagonist with anK_i of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor.

HY-108703

Foliglurax PXT002331	mGluR	Neurological Disease
Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC₅₀ of 79 nM. Antiparkinsonian effect.

HY-14859

Dipraglurant ADX48621	mGluR	Neurological Disease
Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant *mGluR5* negative allosteric modulator (NAM), with an IC₅₀ of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo.

HY-103568

YM-298198 hydrochloride	mGluR	Neurological Disease
YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders.

HY-108703A

Foliglurax monohydrochloride PXT002331 (monohydrochloride)	mGluR	Neurological Disease
Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC₅₀ of 79 nM. Antiparkinsonian effect.

HY-13206

MTEP hydrochloride	mGluR	Neurological Disease
MTEP hydrochloride is a potent, non-competitive and highly selective *mGluR5* antagonist, with an IC₅₀ of 5 nM and a K_i of 16 nM. MTEP hydrochloride shows antidepressant and anxiolytic-like effects. MTEP hydrochloride can be used for Parkinson's disease research.

HY-13206A

MTEP	mGluR	Neurological Disease
MTEP is a potent, non-competitive and highly selective *mGluR5* antagonist, with an IC₅₀ of 5 nM and a K_i of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research.

HY-13058

ADX-47273	mGluR	Neurological Disease
ADX-47273 is a potent, selective and brain-penetrant *mGluR5* positive allosteric modulator (PAM), with an EC₅₀ of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities.

HY-102091

(2R,4R)-APDC	mGluR	Neurological Disease
(2R,4R)-APDC is a selective group II metabotropic glutamate receptors *(mGluRs)* agonist. (2R,4R)-APDC has anticonvulsant and neuroprotective effects.

HY-103575

MFZ 10-7	mGluR	Neurological Disease
MFZ 10-7 is a potent *mGluR5* antagonist. Intraperitoneal administration of MFZ 10-7 inhibits intravenous cocaine self-administration, cocaine-induced reinstatement of drug-seeking behavior and cocaine-associated cue-induced cocaine-seeking behavior in rats..

HY-102094

(E/Z)-SIB-1893	mGluR	Neurological Disease
(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.

HY-135464

(±)-LY367385	mGluR	Neurological Disease
(±)-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.

HY-103344

ZJ43	Aminopeptidase mGluR	Inflammation/Immunology Neurological Disease
ZJ43 is a potent NAAG peptidase inhibitor, with an IC₅₀ of 2.4 nM and a K_i of 0.8 nM. ZJ43 sufficiently activates group II mGluR and reduces some of the behavioral effects of PCP. ZJ43 shows an analgesic effect in neuropathic and inflammatory and pain models.

HY-100371

(RS)-MCPG alpha-MCPG	mGluR	Neurological Disease
(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.

HY-100781B

L-AP4 monohydrate L-APB monohydrate	mGluR	Neurological Disease
L-AP4 (L-APB) monohydrate 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.

HY-107515

LY367385	mGluR	Neurological Disease
LY367385 is a highly selective and potent *mGluR1a* antagonist. LY367385 has an IC₅₀ of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects.

HY-100781A

L-AP4 L-APB	mGluR	Neurological Disease
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.

HY-107515A

LY367385 hydrochloride	mGluR	Neurological Disease
LY367385 hydrochloride is a highly selective and potent *mGluR1a* antagonist. LY367385 hydrochloride has an IC₅₀ of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 hydrochloride has neuroprotective, anticonvulsant and antiepileptic effects.

HY-107514

(RS)-PPG	mGluR	Neurological Disease
(RS)-PPG is a potent and selective agonist for group III *mGluRs. The EC₅₀*s of 5.2 μM, 4.7 μM, 185 μM, and 0.2 μM for hmGluR4a, hmGluR6, hmGluR7b, and hmGluR8a, respectively. Anticonvulsive and neuroprotective activity.

HY-14611

3,3'-Difluorobenzaldazine DFB	mGluR	Neurological Disease
3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of *mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu*5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC₅₀s in the 2 to 5 μM range.

HY-70059

LY341495	mGluR	Neurological Disease
LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC₅₀s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively.

HY-101364A

CHPG sodium salt	mGluR NF-κB ERK Akt	Inflammation/Immunology Neurological Disease
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..

HY-101478

Fenobam	mGluR	Neurological Disease
Fenobam is a selective, orally active, and brain-penetrant *mGluR5* antagonist acting at an allosteric modulatory site (K_ds of 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.

HY-101364

CHPG	mGluR NF-κB ERK Akt	Inflammation/Immunology Cardiovascular Disease
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.

HY-107506

Ro 67-4853	mGluR	Neurological Disease
Ro 67-4853 is a positive allosteric modulator (PAM) of *mGluR1* (pEC₅₀=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation.

HY-101335

DCG-IV	mGluR	Neurological Disease
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: mGlu1R/5R=389/630 μM) and III receptors (IC₅₀: mGlu4R/6R/7R/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects.

Cat. No.	Product Name

HY-L006

GPCR/G Protein Compound Library

1973 compounds

GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery.

MCE provides a unique collection of 1973 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

Cat. No.	Product Name	Target	Category