Search Result
Results for "
mGluRs
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-100372
-
(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-101332
-
EGLU
1 Publications Verification
(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 Kd value of 66 μM. EGLU is an antidepressant agent .
|
-
-
- HY-103572
-
|
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-103562
-
3,3'-Dimethoxybenzaldazine
|
mGluR
|
Neurological Disease
|
DMeOB (3,3'-Dimethoxybenzaldazine) is a mGluR5 receptor negative allosteric modulator with an IC50 of 3 μM. DMeOB displays reversible non-competitive inhibition of mGlu5-mediated responses .
|
-
-
- HY-162232
-
|
mGluR
|
Neurological Disease
|
mGluR2 agonist 1 (Compound 5b) is a potent and selective metabotropic glutamate 2 receptor (mGluR) agonist with an EC50 of 82 nM. mGluR2 agonist 1 can be used for the research of central nervous system (CNS) diseases .
|
-
-
- HY-162232A
-
|
mGluR
|
Neurological Disease
|
mGluR2 agonist 1 hydrochloride is a potent selective agonist for metabotropic glutamate receptors mGluR 2 with EC50 of 82 nM .
|
-
-
- HY-123411
-
BCI 632
|
mGluR
|
Neurological Disease
|
MGS0039 is a type II group mGluR antagonist. MGS0039 has a high affinity for mGluR2 and mGluR3, with Ki values of 2.2 nM and 4.5 nM, respectively. MGS0039 can attenuate the inhibitory effect of glutamate-induced cyclic AMP formation triggered by Forskolin (HY-15371) in CHO cells expressing mGluR2/mGluR3. MGS0039 shows antidepressant-like activity in rats .
|
-
-
- HY-19434A
-
|
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-100838A
-
|
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-108546
-
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-103560
-
|
mGluR
|
Neurological Disease
|
(S)-HexylHIBO is the S-enantiomer of HexylHIBO. HexylHIBO is a group I mGluR antagonist. HexylHIBO elevates the hypothalamus-pituitary-adrenal axis response to restraint in rats. HexylHIBO is promising for research of central nervous system-related diseases .
|
-
-
- HY-103552
-
|
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-122255
-
|
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-107481
-
NS 105
|
mGluR
|
Neurological Disease
|
Fasoracetam (NS 105) is the activator of metabotropic glutamate receptor (mGluR). Fasoracetam (NS 105) has the potential for the research of attention-deficit hyperactivity disorder (ADHD) and Alzheimer's disease (AD) .
|
-
-
- HY-169808
-
|
mGluR
|
Neurological Disease
|
BOMA (Compound 7) is a potent and selective metabotropic glutamate receptor 5 (mGluR 5) antagonist with an IC50 value of 3 nM and an Ki value of 3 nM. BOMA is promising for research of various pain states, including acute, persistent and chronic pain, inflammatory pain and neuropathic pain .
|
-
-
- HY-15129
-
L-Serine O-phosphate; L-SOP
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
O-Phospho-L-serine is the immediate precursor to L-cystein 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
-
|
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
-
|
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-100840
-
(S)-4-Carboxy-3-hydroxyphenylglycine
|
mGluR
|
Neurological Disease
|
(S)-4C3HPG ((S)-4-Carboxy-3-hydroxyphenylglycine) is an antagonist of metabotropic glutamate receptor 1a (mGluR 1a) and an agonist of GluR2. (S)-4C3HPG has the anticonvulsant activity and protects against audiogenic seizures in DBA/2 mice .
|
-
-
- HY-158376
-
-
-
- HY-100804R
-
|
Reference Standards
mGluR
Endogenous Metabolite
|
Neurological Disease
|
L-Cysteinesulfinic acid (Standard) is the analytical standard of L-Cysteinesulfinic acid. This product is intended for research and analytical applications. 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-50906
-
|
mGluR
|
Neurological Disease
|
LY404039 is a potent, selective and orally active mGluR2 and mGluR3 agonist with Kis of 149 nM and 92 nM for recombinant human mGluR2 and mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects .
|
-
-
- HY-15129S
-
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 .
|
-
-
- HY-15129R
-
L-Serine O-phosphate (Standard); L-SOP (Standard)
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
O-Phospho-L-serine (Standard) (L-Serine O-phosphate (Standard)) is the analytical standard of O-Phospho-L-serine (HY-15129). This product is intended for research and analytical applications. O-Phospho-L-serine is the immediate precursor to L-cystein 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-141832
-
|
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-14612
-
|
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-155352
-
|
mGluR
|
Neurological Disease
|
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 .
|
-
-
- HY-110190
-
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-121623
-
|
Others
|
Others
|
VU0359516 is a compound that modulates mGluR4 activity, obtained through structure-activity relationship analysis of mGluR4 positive allosteric modulators, with improved potency and efficacy, as well as selectivity for mGluR4.
|
-
-
- HY-147530
-
|
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-153132
-
|
mGluR
|
Metabolic Disease
|
mGluR3 modulator-1 (compound 3) is a mGluR3 modulator, with an EC50 of 1-10 μM in HEK293T-mGluR-Gqi5 Calcium Mobilization Assay .
|
-
-
- HY-16766
-
RO4995819
|
mGluR
|
Neurological Disease
|
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant .
|
-
-
- HY-147528
-
|
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-131286A
-
LY-544344 hydrochloride
|
mGluR
|
Neurological Disease
|
Talaglumetad hydrochloride is a precursor of thetype II metabotropic glutamate receptor (mGluR2/3) agonist Eglumegad for the research of anxiety.
|
-
-
- HY-100405
-
|
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-130630
-
|
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-18654
-
|
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-147529
-
|
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-119282
-
|
mGluR
|
Neurological Disease
|
AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain .
|
-
-
- HY-11095
-
-
-
- HY-133555
-
|
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-117132
-
|
mGluR
|
Neurological Disease
|
YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
|
-
-
- HY-103556
-
|
mGluR
|
Neurological Disease
|
YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 fumarate has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
|
-
-
- HY-12598A
-
DHPG
4 Publications Verification
(RS)-3,5-DHPG
|
mGluR
|
Neurological Disease
|
DHPG is the agonist for mGluR 1/5 (EC50 for mGluR 1 is 60 nM) that activates the phospholipase C (PLC) pathway, and leads ultimately to the activation of protein kinase C (PKC) .
|
-
-
- HY-12598
-
|
mGluR
|
Neurological Disease
|
(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with Ki 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-162860
-
|
mGluR
CaMK
Tau Protein
|
Neurological Disease
|
FO-4-15 is an mGluR1/CaMKIIα activator. FO-4-15 has a protective effect against H2O2 in human neuroblastoma (SH-SY5Y) cells. FO-4-15 can improve cognitive impairment in Alzheimer’s disease mice by activating the mGluR1/CaMKIIα pathway, and can reduce Aβ accumulation, hyperphosphorylated Tau, and synaptic damage .
|
-
-
- HY-103561
-
|
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-168028
-
|
mGluR
|
Neurological Disease
|
mGluR2 modulator 5 (Compound 11) is an orally active, selective mGluR2 negative allosteric modulator with an IC50 of 8.9 nM. Pharmacokinetic studies in rats show that mGluR2 modulator 5 can effectively cross the blood-brain barrier. It can modulate cognitive and neurological functions in mood disorders and is suitable for research in the field of neurodegenerative diseases .
|
-
-
- HY-103564
-
|
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-110122
-
|
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-153615
-
|
mGluR
|
Neurological Disease
|
CVN636 is a potent, orally active and selective mGluR7 allosteric agonist with an EC50 value of 7 nM for hu mGluR7. CVN636 has central nervous system (CNS) permeability .
|
-
- HY-169835
-
|
mGluR
|
Neurological Disease
|
1-Benzyl-APDC acts as an agonist for mGluR6, with an EC50 of 20 μM in CHO cells. 1-Benzyl-APDC is a weak antagonist of mGluR2, with an IC50 of 200 μM .
|
-
- HY-107516
-
(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-100382
-
|
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
-
-
- HY-114863
-
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-167899
-
|
mGluR
|
Neurological Disease
|
PXT-012253 is a positron emission tomography (PET) ligand for mGluR4, as it binds to an allosteric site on mGluR4. PXT-012253 can be utilized in researches related to Parkinson's disease and levodopa-induced dyskinesia .
|
-
- HY-103570
-
|
mGluR
|
Neurological Disease
|
MCPG is a carboxylic phenyl glycine. MCPG can block metabotropic glutamate receptor (mGluR)(HY-15129) and has antagonistic activity of mGluR subtype. MCPG can be used to study the induction and maintenance of long-term potentiation (LTP) .
|
-
- HY-14417
-
|
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 mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD) .
|
-
- HY-125717
-
|
mGluR
|
Neurological Disease
|
VU0029251 is a mGluR5 partial antagonist (Ki: 1.07 μM). VU0029251 inhibits glutamate induced calcium mobilization in HEK293 cell membranes expressing rat mGluR5 (IC50: 1.7 μM) .
|
-
- HY-14417B
-
|
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 mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD) .
|
-
- HY-157998
-
|
mGluR
Src
|
Others
|
mG2N001 is a negative allosteric modulator (NAM) (IC50: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope [11C]mG2N001 can be used in PET imaging. [11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images .
|
-
- HY-129794
-
|
mGluR
|
Neurological Disease
|
YM-298198 is a potent mGlu1 receptor with an IC50 of 24 nM. YM-298198 can be used in the study of neurological disease .
|
-
- HY-12597
-
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 Ki of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis indica .
|
-
- HY-100406
-
(+)-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-100840A
-
4-Carboxy-3-hydroxyphenylglycine
|
mGluR
|
Neurological Disease
|
(RS)-4C3HPG (4-Carboxy-3-hydroxyphenylglycine) is an effective competitive antagonist at the metabotropic glutamate receptor 1 (mGluR1) in the central nervous system, and it is also an agonist at mGluR2/3. (RS)-4C3HPG exhibits neuroprotective effects in an acute global ischemia rat model .
|
-
- HY-107507
-
-
- HY-103565
-
AMN082
1 Publications Verification
|
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-107457
-
|
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-170499
-
BI02982816
|
mGluR
|
Neurological Disease
|
VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable .
|
-
- HY-101247
-
|
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-107457A
-
|
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
-
-
- HY-101164
-
-
- HY-103565A
-
|
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-103111
-
|
mGluR
|
Neurological Disease
|
MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB 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
-
|
mGluR
|
Neurological Disease
|
MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB 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-103574
-
ADX-10059 hydrochloride
|
mGluR
|
Neurological Disease
|
Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine .
|
-
- HY-121848
-
ML397
|
mGluR
|
Neurological Disease
|
VU0155094 is a positive allosteric modulator with differential activity at the various group III mGluRs .
|
-
- HY-103565R
-
|
mGluR
|
Neurological Disease
|
AMN082 (Standard) is the analytical standard of AMN082. This product is intended for research and analytical applications. 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-103575
-
|
mGluR
|
Neurological Disease
|
MFZ 10-7 is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki 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-103575A
-
|
mGluR
|
Neurological Disease
|
MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki 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-W714513
-
|
mGluR
|
Neurological Disease
|
VU0469650 hydrochloride is a brain-penetrant negative allosteric modulator of metabotropic glutamate receptor 1 (mGluR1). VU0469650 hydrochloride inhibits glutamate-induced calcium flux in cells expressing human mGluR1 (IC50= 99 nM). VU0469650 hydrochloride is promising for research of central nervous system diseases such as anxiety, addiction, and epilepsy .
|
-
- HY-103573
-
|
mGluR
|
Neurological Disease
|
VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC50 of 61 nM .
|
-
- HY-13058B
-
|
mGluR
|
Neurological Disease
|
(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
|
-
- HY-15442
-
BINA
|
mGluR
|
Neurological Disease
|
Biphenylindanone A (BINA) is a selective human mGluR2 (hmGluR2) potentiator for the treatment of many neurological disorders .
|
-
- HY-122559
-
|
mGluR
|
Neurological Disease
|
BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 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-14418
-
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-100728
-
|
mGluR
|
Neurological Disease
|
BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
|
-
- HY-100823
-
-
- HY-103565AR
-
|
mGluR
|
Neurological Disease
|
AMN082 (free base) (Standard) is the analytical standard of AMN082 (free base). This product is intended for research and analytical applications. 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-129636
-
(E)-GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
|
-
- HY-163831
-
|
mGluR
|
Neurological Disease
|
AZ12559322 is a positive allosteric modulator of mGluR2, with the Ki value of 1.31 nM. AZ12559322 can be used in neurological research .
|
-
- HY-135441
-
|
mGluR
|
Inflammation/Immunology
|
PF-06422913 is an orally active, potent and selective metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator .
|
-
- HY-119078
-
|
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-16951
-
|
mGluR
|
Neurological Disease
|
VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a Ki of 156 nM and an EC50 of 9.6 nM .
|
-
- HY-101375
-
|
mGluR
|
Neurological Disease
|
(RS)-APICA is a selective group II metabotropic glutamate receptor (mGluR II) antagonist. (RS)-APICA shows potential neuroprotective effect .
|
-
- HY-101356
-
|
mGluR
|
Neurological Disease
|
CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of metabotropic glutamate receptor 1b (mGluR1b) .
|
-
- HY-130553
-
β-NAAG; β-N-Acetylaspartylglutamic acid
|
Aminopeptidase
mGluR
|
Neurological Disease
|
β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (Ki=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-107508
-
|
mGluR
|
Neurological Disease
|
VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=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-103571
-
|
mGluR
|
Neurological Disease
|
VU0285683 is a selective mGluR5 positive allosteric modulator (PAM). VU0285683 has anxiolytic-like activity in rodent models for anxiety .
|
-
- HY-101226
-
|
mGluR
|
Neurological Disease
|
MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
|
-
- HY-100409
-
|
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-116723
-
|
mGluR
|
Neurological Disease
|
CFMMC is a selective allosteric metabotropic glutamate receptor 1 (mGluR1) antagonist. CFMMC inhibits L-glutamate-induced intracellular Ca 2+ mobilization ([Ca 2+]i) in Chinese hamster ovary cells expressing recombinant human mGluR1a with an IC50 value of 50 nM. CFMMC is promising for research of various central nervous system disorders, such as schizophrenia, epilepsy, anxiety, pain, cognitive dysfunction and drug abuse .
|
-
- HY-110070
-
2-Amino-4-phosphonobutyric acid sodium
|
mGluR
|
Others
Neurological Disease
|
DL-AP4 sodium (2-Amino-4-phosphonobutyric acid sodium) is an agonist for metabotropic glutamate receptors (mGluR). DL-AP4 sodium binds to mGluR4, activates the signaling pathway that is negatively correlated with adenylate cyclase, and inhibits the Forskolin (HY-15371)-induced production of cAMP. DL-AP4 sodium is also an inhibitor for ON channel, that reduces the sensitivity of photoreceptors to brightness changes .
|
-
- HY-100403
-
Ro 67-7476
Maximum Cited Publications
12 Publications Verification
|
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-101387A
-
|
mGluR
|
Neurological Disease
|
ACPT-II is an antagonist of group III mGluRs with diverse biological activities including neuroprotective, anticonvulsant, and anxiolytic-like effects .
|
-
- HY-103491
-
|
iGluR
|
Neurological Disease
|
PF-06462894 is an alkyne-lacking metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator profiled in both rat and nonhuman primates .
|
-
- HY-155088
-
|
mGluR
|
Metabolic Disease
|
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
|
-
- HY-124393
-
|
mGluR
|
Neurological Disease
|
GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats .
|
-
- HY-101387
-
|
mGluR
|
Neurological Disease
|
rel-ACPT-I is an agonist of group III mGluRs with diverse biological activities including neuroprotective, anticonvulsant, and anxiolytic-like effects .
|
-
- HY-100841A
-
(S)-3HPG
|
mGluR
|
Neurological Disease
|
(S)-3-Hydroxyphenylglycine ((S)-3HPG) is a potent mGluR1 agonist without effect at mGlu2 or mGlu4 .
|
-
- HY-103559
-
|
mGluR
|
Neurological Disease
|
HexylHIBO is a potent group I mGluR antagonist with Kbs of 140 and 110 μM at mGlu1a and mGlu5a receptors, respectively. HexylHIBO decreased sEPSC in rat .
|
-
- HY-141848A
-
|
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-14417A
-
|
mGluR
|
Neurological Disease
|
(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
|
-
- HY-15257
-
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-118179
-
|
mGluR
|
Neurological Disease
|
VU0486321 is a compound in a class of mGlu1 positive allosteric modulators (PAMs). VU0486321 maintains acceptable mGlu1 PAM potency, DMPK profile, CNS permeability, and mGluR selectivity.
|
-
- HY-108703
-
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-176420
-
|
mGluR
|
Neurological Disease
|
VU6031545 is a potent mGlu 5 negative allosteric modulator with an IC50 of 15 nM. VU6031545 has excellent brain penetrant and oral bioavailability in rats .
|
-
- HY-100402
-
|
mGluR
|
Cancer
|
CFMTI inhibits L-glutamate-induced intracellular Ca 2+ mobilization in CHO cells expressing human and rat mGluR1a, with IC50s of 2.6 and 2.3 nM, respectively .
|
-
- HY-110141
-
|
mGluR
|
Others
|
ABP688 is a high affinity human mGluR5 antagonist with anKi of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor .
|
-
- HY-108703A
-
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-111332
-
|
mGluR
|
Others
|
(E)-PHCCC is a positive allosteric modulator (PAM) for mGluR4, that enhances the activity of the receptor's endogenous ligand (glutamate), and exhibits activity in the calcium mobilization assay in CHO cells with an EC50 of 3.2 μM .
|
-
- HY-103568
-
|
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-118285
-
|
mGluR
|
Neurological Disease
|
Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
|
-
- HY-118022
-
|
mGluR
|
Neurological Disease
|
VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .
|
-
- HY-13206
-
|
mGluR
|
Neurological Disease
|
MTEP hydrochloride is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP hydrochloride shows antidepressant and anxiolytic-like effects. MTEP hydrochloride can be used for Parkinson's disease research .
|
-
- HY-12629
-
PF-06297470
|
mGluR
|
Others
|
PF470 (PF-06297470) is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with significant efficacy in Parkinson's disease models, but clinical development was halted due to potential issues found in toxicology studies.
|
-
- HY-103567
-
|
mGluR
|
Neurological Disease
|
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 .
|
-
- HY-103567A
-
|
mGluR
|
Neurological Disease
|
Desmethyl-YM-298198 is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice .
|
-
- HY-111256
-
|
mGluR
|
Neurological Disease
|
A-850002 is a metabotropic glutamate receptor (mGluR) antagonist (IC50=27 nM) that significantly attenuates spontaneous pain behavior after skin incision in rats. A-850002 can be used for analgesia research .
|
-
- HY-13058
-
|
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-100841
-
3HPG
|
mGluR
|
Neurological Disease
|
(Rac)-3-Hydroxyphenylglycine (3HPG) is a racemic mixture of (S)-3-hydroxyphenylglycine and (R)-3-hydroxyphenylglycine. (S)-3-Hydroxyphenylglycine is a potent and selective mGluR1 agonist .
|
-
- HY-102094
-
|
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
-
|
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-120662
-
|
mGluR
|
Neurological Disease
|
GSK1331268 is a selective, orally active agonist for mGluR2 with a pEC50 of 6.9. GSK1331268 exhibits good blood-brain barrier penetration. GSK1331268 regulates glutamate signaling, and can be used in research of neurodegenerative and neuropsychiatric diseases .
|
-
- HY-103344
-
|
Aminopeptidase
mGluR
|
Neurological Disease
Inflammation/Immunology
|
ZJ43 is a potent NAAG peptidase inhibitor, with an IC50 of 2.4 nM and a Ki 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
-
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-110254
-
|
mGluR
|
Neurological Disease
|
AZD 9272 is a selective, orally active and brain penetrant mGluR5 antagonist with IC50s of 2.6 nM and 7.6 nM for rat and human receptors, respectively. AZD 9272 shows >3900-fold selectivity over other mGlu receptors 2].
|
-
- HY-100781B
-
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
-
|
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
1 Publications Verification
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
-
|
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-107517
-
|
mGluR
|
Neurological Disease
|
UBP 1112 is a selective group III mGluR antagonist, with a Kd of 5.1 μM.UBP 1112 shows 96-fold affinity for group III over group II mGlu receptor (Kd, 488 μM), and shows no significant activity at group I mGlu receptor or iGlu receptor .
|
-
- HY-107514
-
|
mGluR
|
Neurological Disease
|
(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 .
|
-
- HY-110255B
-
|
mGluR
Calcium Channel
Trk Receptor
|
Neurological Disease
|
AZD-2066 hydrochloride is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydrochloride activates the BDNF/trkB signaling pathway. AZD 2066 hydrochloride can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease .
|
-
- HY-110255
-
|
mGluR
Calcium Channel
Trk Receptor
|
Neurological Disease
|
AZD-2066 is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 activates the BDNF/trkB signaling pathway. AZD 2066 can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease .
|
-
- HY-110255A
-
|
mGluR
Calcium Channel
Trk Receptor
|
Neurological Disease
|
AZD-2066 hydrate is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydrate activates the BDNF/trkB signaling pathway. AZD 2066 hydrate can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease .
|
-
- HY-14611
-
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 mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range .
|
-
- HY-70059
-
LY341495
Maximum Cited Publications
12 Publications Verification
|
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-119097
-
|
mGluR
|
Neurological Disease
|
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 .
|
-
- HY-100617
-
(S)-4-Carboxyphenylglycine
|
mGluR
|
Neurological Disease
|
(S)-4CPG ((S)-4-Carboxyphenylglycine) is a potent mGluR2 agonist. (S)-4CPG reduces hyperalgesia and allodynia associated with sciatic nerve contraction injury in rats. (S)-4CPG can be used in research on neurological diseases .
|
-
- HY-101364A
-
|
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. .
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-
- HY-101364
-
|
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 .
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-
- HY-14569
-
CDPPB
1 Publications Verification
|
mGluR
Akt
ERK
Caspase
Mitochondrial Metabolism
|
Neurological Disease
|
CDPPB is a selective, orally active mGluR5 allosteric modulator. CDPPB increases AKT and ERK1/2 activation and augments the BDNF mRNA. CDPPB inhibits caspase-3 activation and mitochondrial dysfunction. CDPPB improves cognitive impairment, depression, and Huntington's disease .
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-
- HY-W015546
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BMAA hydrochloride
|
Bacterial
mGluR
PKC
|
Neurological Disease
Inflammation/Immunology
|
β-N-methylamino-L-alanine hydrochloride (BMAA hydrochloride) is a neurotoxin produced by cyanobacteria. β-N-methylamino-L-alanine hydrochloride activates mGluR3 and inhibits PKC. β-N-methylamino-L-alanine hydrochloride can be used in the research of neurodegenerative diseases and immune diseases .
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-
- HY-B0340
-
DM9384; DZL-221
|
nAChR
iGluR
mGluR
PKC
GABA Receptor
Calcium Channel
|
Neurological Disease
|
Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca 2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research .
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-
- HY-14859
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ADX48621
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mGluR
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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.
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-
- HY-100371R
-
alpha-MCPG (Standard)
|
Reference Standards
mGluR
|
Neurological Disease
|
(RS)-MCPG (Standard) is the analytical standard of (RS)-MCPG. This product is intended for research and analytical applications. (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 .
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-
- HY-13206A
-
|
mGluR
|
Neurological Disease
|
MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki 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.
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-
- HY-B0340R
-
DM9384 (Standard); DZL-221 (Standard)
|
nAChR
iGluR
mGluR
PKC
GABA Receptor
Calcium Channel
|
Neurological Disease
|
Nefiracetam (Standard) is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca 2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research .
|
-
- HY-101364AR
-
|
Reference Standards
mGluR
NF-κB
ERK
Akt
|
Neurological Disease
Inflammation/Immunology
|
CHPG (sodium salt) (Standard) is the analytical standard of CHPG (sodium salt). This product is intended for research and analytical applications. 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. .
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-
- HY-101478
-
|
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 Kd 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
-
|
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 Kd 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-70059A
-
|
mGluR
|
Neurological Disease
|
(Rac)-LY341495 is the isomers of LY341495 (HY-70059) can be used as control compounds in experiments. 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-101478R
-
|
Reference Standards
mGluR
Apoptosis
|
Neurological Disease
Cancer
|
Fenobam (Standard) is the analytical standard of Fenobam. This product is intended for research and analytical applications. Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd 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-107506
-
|
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-102091
-
(2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic acid
|
mGluR
|
Neurological Disease
|
(2R,4R)-APDC is a group II metabotropic glutamate receptor (mGluR) agonist. (2R,4R)-APDC affects cell proliferation by inhibiting glutamate release, enhancing motor responses produced by D1 receptor activation, or reducing brain-derived neurotrophic factor (BDNF) levels. (2R,4R)-APDC can be used in the study of epilepsy and other neurological diseases .
|
-
- HY-115860
-
|
iGluR
|
Neurological Disease
|
TAS-4 is a potent and selective mGluR4 positive allosteric modulator with significant anti-Parkinson's disease activity. TAS-4 is able to show efficacy when used alone or in combination with l-DOPA. TAS-4 is able to reverse haloperidol-induced spasticity when administered alone. TAS-4 enhances the contralateral rotation behavior induced by l-DOPA in a dose-dependent manner. TAS-4 combined with low-dose l-DOPA shows anti-Parkinson's effects similar to full-dose l-DOPA without exacerbating abnormal motor side effects .
|
-
- HY-102091A
-
(2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic acid hydrate
|
mGluR
|
Neurological Disease
|
(2R,4R)-APDC hydrate ((2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic acid hydrate) is a group II metabotropic glutamate receptor (mGluR) agonist. (2R,4R)-APDC hydrate affects cell proliferation by inhibiting glutamate release, enhancing motor responses produced by D1 receptor activation, or reducing brain-derived neurotrophic factor (BDNF) levels. (2R,4R)-APDC hydrate can be used in the study of epilepsy and other neurological diseases .
|
-
- HY-101335
-
|
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 .
|
-
-
-
HY-L006
-
|
2,895 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 2,895 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-15129
-
-
-
- HY-100804
-
|
Structural Classification
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
mGluR
Endogenous Metabolite
|
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
-
|
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 .
|
-
-
- HY-100786
-
-
-
- HY-12597
-
-
-
- HY-W015546
-
-
-
- HY-100804R
-
|
Structural Classification
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Reference Standards
mGluR
Endogenous Metabolite
|
L-Cysteinesulfinic acid (Standard) is the analytical standard of L-Cysteinesulfinic acid. This product is intended for research and analytical applications. 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 .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-15129S
-
|
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 .
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-118022
-
|
|
Alkynes
|
VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .
|
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