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Isoforms Recommended:	mGluR5

Results for "

mGluR5

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (2) Apoptosis (2) CaSR (1) Endogenous Metabolite (1) ERK (2) mGluR (37) NF-κB (2)
By Research Areas:	Cancer (2) Cardiovascular Disease (2) Inflammation/Immunology (2) Neurological Disease (35)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-155352

mGluR5 antagonist-1	mGluR	Others
mGluR5 antagonist-1 (compound 10) is a high-affinity *mGluR5* antagonist, with an IC₅₀ value of 11.5 nM. mGluR5 antagonist-1 has anti-depressant effect .

HY-15445

CTEP 2 Publications Verification 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. CTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-110255

AZD 2066 1 Publications Verification	mGluR	Neurological Disease
AZD 2066 is a selective, orally active and brain-penetrant antagonist of *mGluR5*. AZD 2066 has antinociception effects .

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-125717

VU0029251	mGluR	Neurological Disease
VU0029251 is a *mGluR5* partial antagonist (K_i: 1.07 μM). VU0029251 inhibits glutamate induced calcium mobilization in HEK293 cell membranes expressing rat mGluR5 (IC₅₀: 1.7 μM) .

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 .

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-14569

CDPPB 1 Publications Verification	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-103571

VU0285683

mGluR Neurological Disease

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

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

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 . (S,S)-BMS-984923 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-103574

Raseglurant hydrochloride ADX-10059 hydrochloride	mGluR	Neurological Disease
Raseglurant hydrochloride is a negative allosteric modulator of *mGluR5*. Raseglurant hydrochloride can be used in study migraine .

HY-13058

ADX-47273 1 Publications Verification	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-15257

Mavoglurant 2 Publications Verification 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 . Mavoglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-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-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) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-103575

MFZ 10-7	mGluR	Neurological Disease
MFZ 10-7 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 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-103562

DMeOB

3,3'-Dimethoxybenzaldazine
mGluR Neurological Disease

DMeOB is an agonist of mGluR5 receptor with an IC₅₀ of 3 μM. DMeOB has a negative modulatory effect .

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

DMeOB 3,3'-Dimethoxybenzaldazine	mGluR	Neurological Disease
DMeOB is an agonist of mGluR5 receptor with an IC₅₀ of 3 μM. DMeOB has a negative modulatory effect .

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-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-100728

BMT-145027

mGluR Neurological Disease

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

BMT-145027	mGluR	Neurological Disease
BMT-145027 is an *mGluR5* positive allosteric modulator without inherent agonist activity, exhibits an EC₅₀ of 47 nM.

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 . Dipraglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-16951

VU-1545

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 .

VU-1545
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-11095

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

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-103564

ACDPP	mGluR	Neurological Disease
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) .

HY-13206

MTEP hydrochloride 2 Publications Verification	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-100786

DL-AP3

DL-AP3 is a competitive mGluR1 and mGluR5 antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect .

DL-AP3
DL-AP3 is a competitive *mGluR1* and *mGluR5* antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect .

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-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-100804

L-Cysteinesulfinic acid
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-101364

CHPG	mGluR NF-κB ERK Akt	Cardiovascular Disease Inflammation/Immunology
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-101364A

CHPG sodium salt	mGluR NF-κB ERK Akt	Neurological Disease Inflammation/Immunology
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-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 . MTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-101478

Fenobam	mGluR Apoptosis	Neurological Disease Cancer
Fenobam is a selective and orally active *mGluR5* antagonist (IC₅₀=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the K_d values of 54 nM and 31 nM on rat and human recombinant *mGlu5* receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .

HY-101478A

Fenobam hydrate	mGluR Apoptosis	Neurological Disease Cancer
Fenobam hydrate is a selective and orally active *mGluR5* antagonist (IC₅₀=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the K_d values of 54 nM and 31 nM on rat and human recombinant *mGlu5* receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction .

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-12598A

DHPG 2 Publications Verification (RS)-3,5-DHPG
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-108034

GET73	Others	Neurological Disease
GET73 is a γ-hydroxybutyric acid (GHB) analog, a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties. GET73 significantly affects glutamate transmission in the hippocampus .

HY-100371

(RS)-MCPG 1 Publications Verification 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 .

L-Cysteinesulfinic acid monohydrate	Structural Classification Natural Products Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields	mGluR Endogenous Metabolite
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 .

Cat. No.	Compare	Product Name	Species	Source

HY-P701627

	GRM5 Protein, Human (His) GRM5; Metabotropic glutamate receptor 5; mGluR5	Human	Sf9 insect cells
	The GRM5 protein is a G protein-coupled glutamate receptor that undergoes ligand-induced conformational changes and activates signaling cascades through G proteins, affecting downstream effectors. This cascade includes the phosphatidylinositol-calcium second messenger system and induces calcium-activated chloride currents. GRM5 Protein, Human (His) is the recombinant human-derived GRM5 protein, expressed by Sf9 insect cells , with C-10*His labeled tag. ,

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mGluR5

Inhibitors & Agonists

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