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Isoforms Recommended:	mGluR5

Results for "

mGlu5 receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) mGluR (25)
By Research Areas:	Cancer (2) Neurological Disease (25)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12510

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

HY-102095

SIB-1757	mGluR	Neurological Disease
SIB-1757 is a highly selective and noncompetitive antagonist of **mGlu5 receptor with an IC₅₀** of 0.4 μM .

HY-120589

VU0360172	mGluR	Neurological Disease
VU0360172 is a potent and selective **mGlu5 receptor positive allosteric modulator with an EC₅₀ value of 16 nM and a K_i** of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice . VU0360172 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-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-107504

VU0360172 hydrochloride	mGluR	Neurological Disease
VU0360172 hydrochloride is a potent and selective **mGlu5 receptor positive allosteric modulator (PAM) with an EC₅₀ value of 16 nM and a K_i** of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice .

HY-117697

Lu AF11205	Others	Others
Lu AF11205 is a mGlu5 receptor positive allosteric modulator with activity modulating mGlu5 receptor activity. Optimization of Lu AF11205 resulted in a series of potent fused thiazole analogs whose structures and activities were influenced by substituents and which could affect receptor function in cell lines expressing mGlu5 receptors.

HY-114589

VU0240382	Others	Others
VU0240382 is a metabotropic glutamate receptor subtype 5 modulator whose activity differs depending on whether it has allosteric agonist activity. VU0240382 with allosteric agonist activity can activate mGlu(5) receptors in cell lines, but has no agonist activity in natural systems and has similar efficacy to mGlu(5) modulators without allosteric agonist activity in animal models.

HY-119941

VU0652835	mGluR	Neurological Disease
VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC₅₀ of 81 nM .

HY-123667

NCFP	mGluR	Neurological Disease
NCFP is a metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM). NCFP can be used in the study of central nervous system diseases .

HY-14866

Raseglurant ADX-10059	mGluR	Neurological Disease
Raseglurant (ADX-10059) is a **mGlu5 receptor** negative allosteric modulator. Raseglurant is effective against migraine. Raseglurant reduces the Haloperidol (HY-14538)-induced catalepsy in mice .

HY-118238

Remeglurant MRZ-8456	mGluR	Neurological Disease
Remeglurant (MRZ-8456) acts as a selective, orally active and allosteric antagonist of the *mGlu5* receptor, with an IC₅₀ of 13 nM. Remeglurant (MRZ-8456) can be used in the research for dyskinesia in Parkinson’s disease (PD) .

HY-15257A

Mavoglurant racemate AFQ-056 racemate	mGluR	Neurological Disease
Mavoglurant racemate (AFQ-056 racemate) is the racemate of Mavoglurant. Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist . Mavoglurant (racemate) 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-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-103550

A-841720	mGluR	Neurological Disease
A-841720 is a potent, non-competitive and selective **mGlu1 receptor antagonist with an IC₅₀** of 10 nM for human mGlu1 receptor. A-841720 displays 34-fold selectivity over mGlu5 (IC₅₀ of 342 nM), and no significant activity at a range of other neurotransmitter receptors, ion channels, and transporters. A-841720 has the potential for chronic pain research .

HY-131019

JF-NP-26	mGluR	Neurological Disease
JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged **mGlu5 receptor** negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals .

HY-14609

MPEP Hydrochloride 3 Publications Verification	mGluR	Neurological Disease
MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active **mGlu5 receptor antagonist, with an IC₅₀** of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects . MPEP (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-14609A

MPEP 3 Publications Verification	mGluR	Neurological Disease
MPEP is a potent, selective, noncompetitive, orally active and systemically active **mGlu5 receptor antagonist, with an IC₅₀** of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects . MPEP 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-110152

LSN2463359	mGluR	Neurological Disease
LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu₅). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model . LSN2463359 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-100588

VU0364770	mGluR	Neurological Disease
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 K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .

HY-100588A

VU0364770 hydrochloride	mGluR	Neurological Disease
VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of *mGlu4. VU0346770 hydrochloride exhibits EC₅₀s of 290 nM and 1.1 μM at rat mGlu4* and human mGlu4 receptor, respectively. VU0364770 hydrochloride 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 hydrochloride also possesses activity at MAO with K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .

HY-19623

VU0092273	mGluR	Neurological Disease
VU0092273 is a potent mGlu5 positive allosteric modulator (PAM) that also binds to the MPEP site, with an EC₅₀ of 0.27 μM .

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-15393

VU 0357121	mGluR	Neurological Disease
VU 0357121 is a positive and highly selective *mGlu5R* allosteric modulator (PAM) with an EC₅₀ of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes .

HY-70059

LY341495 Maximum Cited Publications 9 Publications Verification	mGluR	Neurological Disease
LY341495 is a *metabotropic glutamate receptor* (mGluR) antagonist with IC₅₀*s 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-70059A

(Rac)-LY341495	Others	Neurological Disease
(Rac)-LY341495 is the isomer of LY341495 (HY-70059), and can be used as an experimental control. LY341495 is a *metabotropic glutamate receptor* (mGluR) antagonist with IC₅₀*s 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 .

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mGlu5 receptor

Inhibitors & Agonists