|
T6457 |
CTEP
|
mGluR5 inhibitor,RO 4956371 |
GluR
|
|
CTEP (RO 4956371) (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors. |
|
T38659 |
mGluR5 modulator 1
|
|
|
|
mGluR5 modulator 1 is a compound that acts as a positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5). Its primary application lies in the field of schizophrenia and cognitive impairment... |
|
T81801 |
mGluR5 antagonist-1
|
|
|
|
mGluR5 antagonist-1 (compound 10) is a potent mGluR5 inhibitor exhibiting an IC50 of 11.5 nM and demonstrates antidepressant effects [1]. |
|
T22641 |
CDPPB
|
|
GluR
|
|
CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5). |
|
T23514 |
VU-1545
|
VU 1545 |
GluR
|
|
VU-1545 is mGlu5 positive allosteric modulator. |
|
T2053 |
ADX-47273
|
BA 94673139 |
GluR
|
|
ADX-47273 (BA 94673139) is a positive and selective allosteric modulator for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM). |
|
T11393 |
GET73
|
Gamma hydroxybutyric acid analogue,GET 73 |
GluR
|
|
GET73 (Gamma hydroxybutyric acid analogue) is an negative allosteric modulator of mGluR5. GET73 is a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties. |
|
T3479 |
(RS)-MCPG
|
alpha-MCPG,(±)-MCPG |
GluR
|
|
(RS)-MCPG ((±)-MCPG) is a non-selective group I/II metabotropic glutamate receptor antagonist. |
|
T14389 |
AZD 9272
|
|
GluR
|
|
AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux. |
|
T10573 |
BMT-145027
|
|
GluR
|
|
BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM). |
|
T8457 |
NPS2390
|
|
GluR
|
|
NPS2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 (IC50 of 5.2 and 82 nM, respectively) |
|
T26520 |
ABP688
|
ABP-688,ABP 688 |
GluR
|
|
ABP688 is a non-competitive and selective mGluR5 antagonist(Ki = 1.7 nM). ABP688 can be used as a PET tracer for clinical imaging. |
|
T22736 |
DMeOB
|
3,3'-Dimethoxybenzaldazine |
GluR
|
|
DMeOB (3,3'-Dimethoxybenzaldazine) is a negative regulator with mGluR5 agonist activity and can be used to study neurological diseases. |
|
T22976 |
MFZ 10-7
|
|
Others
,
GluR
|
|
MFZ 10-7 is anegative allosteric modulator of the mGluR5. |
|
T23353 |
(E/Z)-SIB-1893
|
SIB 1893 |
Others
,
GluR
|
|
(E/Z)-SIB-1893 (SIB 1893) is the racemate of (E)-SIB-1893 and (Z)-SIB-1893. (E)-SIB-1893 is a selective, noncompetitive mGluR5 antagonist with anticonvulsant activity . |
|
T23509 |
VU 0285683
|
|
GluR
|
|
VU 0285683 is a specific negative allosteric modulator of mGluR5 with a high affinity for the MPEP binding site. VU 0285683 shows anxiolytic-like activity. |
|
T15275 |
Fenobam
|
|
GluR
|
|
Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric mo... |
|
T22711 |
DCB
|
3,3'-dichlorobenzaldazine |
Others
,
GluR
|
|
DCB (3,3'-dichlorobenzaldazine) is an allosteric ligand for mGluR5 and shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB). DCB blocks the positive allosteric regulation of mGluRs with the help of ... |
|
T10809L |
CHPG hydrochloride
|
CHPG hydrochloride(170846-74-9 Free base) |
ERK
,
NF-κB
,
GluR
|
|
CHPG hydrochloride is a selective agonist of mGluR5. |
|
T23515 |
VU-29
|
VU 29 |
GluR
|
|
VU-29 is a positive allosteric mGlu5 receptor modulator with EC50=9 nM and Ki=244 nM for rmGluR5. It is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM). |
|
T10881 |
CPPHA
|
|
GluR
|
|
CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases. |
|
T26719 |
AZD6538
|
AZD 6538,AZD-6538 |
GluR
|
|
AZD6538 is an mGluR5 negative allosteric modulator used in the study of CNS-related diseases such as Alzheimer's disease. |
|
T13441 |
(R)-ADX-47273
|
|
GluR
|
|
(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator(EC50 of 168 nM for potentiation ). |
|
T3482 |
CFMTI
|
|
GluR
|
|
CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist (IC50: 2.6 nM). The selectivity of CFMTI to mGluR1 is higher 2000-fold than mGluR5. |
|
T41301 |
L-Cysteinesulfinic acid monohydrate
|
|
GluR
|
|
L-Cysteinesulfinic acid monohydrate is a potent agonist at 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, respectiv... |
|
T10808 |
CHPG sodium salt
|
|
NF-κB
,
GluR
|
|
CHPG sodium salt is a selective agonist of mGluR5 and activates the ERK and Akt signaling pathways. CHPG sodium salt can be used in studies about traumatic brain injury. |
|
T50112 |
5-(2-aminoethyl)-4-methyl-1,3-thiazol-2-amine dihydrochloride
|
|
Others
|
|
5-(2-aminoethyl)-4-methyl-1,3-thiazol-2-amine dihydrochloride is a potent and selective antagonist of metabotropic glutamate receptor 5 (mGluR5). It has been shown to be effective in several neurological disorders, inclu... |
|
T50094 |
DL-Willardiine
|
2-amino-3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)propanoic acid |
Others
|
|
DL-Willardiine (2-amino-3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)propanoic acid) is an unnatural amino acid, a derivative of glutamate. It is an agonist of mGluR5, which regulates the activity of enzymes involved in... |
|
T3483 |
FTIDC
|
|
GluR
|
|
FTIDC is a highly potent and selective allosteric antagonist of mGluR1 receptors and shows very weak potency against human and rat mGluR5 receptors. The inhibition of FTIDC for mGluR1 receptors is shown to be in noncompe... |
|
T6598 |
MPEP
|
|
GluR
|
|
MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors. |
|
T8862 |
ML 254
|
|
GluR
|
|
ML254 competitively interacts with the MPEP allosteric binding site. ML254 is highly selective for mGlu5 versus other mGlu receptors, has a clean ancillary Ricerca profile, and suitable dystrophia myotonica protein kinas... |
|
T6725 |
VU 0357121
|
|
GluR
|
|
VU0357121, a positive allosteric modulator of mGlu5 (EC50: 33 nM), is inactive or very weakly antagonizing at other mGlu receptor subtypes. |
|
T15134 |
Dipraglurant
|
ADX48621 |
Others
|
|
Dipraglurant is a negative allosteric regulator (NAM) of blood-brain barrier transmissible mGluR5 with effective, selective and oral activity, with an IC50 value of 21 nM. Dipraglurant can treat levodopa-induced dyskines... |
|
T12025 |
MFZ 10-7 hydrochloride
|
|
GluR
|
|
|
|
T10430 |
AZD 2066
|
|
Others
|
|
AZD 2066 is a selective, orally active, and brain-penetrant mGluR5 antagonist with analgesic activity. |
|
T24500 |
MRZ-8676
|
MRZ8676,MRZ 8676 |
|
|
MRZ-8676 is an orally bioavailable and negative allosteric modulator of subtype 5 metabotropic glutamate receptors (mGluR5). |
|
T27457 |
GSK2210875
|
GSK-2210875,GSK 2210875 |
|
|
GSK2210875 is a mGluR5 antagonist with oral activity. |
|
T61708 |
AZD 2066 hydrate
|
|
|
|
AZD 2066 hydrate is a selective, orally active, and brain-penetrant antagonist of mGluR5. It exhibits antinociceptive effects [1]. |
|
T27434 |
GRN-529
|
GRN 529,GRN529 |
|
|
GRN-529 is a selective negative allosteric modulator of the mGluR5 receptor. |
|
T10809 |
CHPG
|
|
Others
|
|
CHPG is a selective agonist of mGluR5. In BV2 microglial cells, it attenuates SO2-induced oxidative stress and inflammation through the TSG-6/NF-κB pathway. |
|
T74185 |
(S,S)-BMS-984923
|
|
|
|
(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC 50 >1μM for mGluR5 receptor [1] . BMS-984923 is a potent mGluR5 silent allosteric modulator [2] . |
|
T38789 |
BMS-984923
|
|
|
|
BMS-984923, a highly potent silent allosteric modulator (SAM) of mGluR5, demonstrates exceptional binding affinity (K i = 0.6 nM). Additionally, this compound possesses favorable oral bioavailability and blood-brain barr... |
|
T73568 |
MTEP
|
|
|
|
MTEP, a potent, non-competitive, and highly selective antagonist of mGluR5, exhibits an IC50 value of 5 nM and a K_i value of 16 nM. Demonstrating antidepressant and anxiolytic-like effects, MTEP is utilized in Parkinson... |
|
T78600 |
VU0029251
|
|
|
|
VU0029251 serves as a partial antagonist of mGluR5, exhibiting a binding affinity with a K i of 1.07 μM. It also attenuates glutamate-induced calcium mobilization in HEK293 cell membranes that express rat mGluR5, demonst... |
|
T68959 |
Fenobam hydrate
|
|
|
|
Fenobam hydrate is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5). It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate and inhibits ba... |
|
T3484 |
Trans-ACPD
|
Trans-(±)-ACP,1-amino-1,3-dicarboxycyclopentane,(±)-trans-ACPD |
GluR
|
|
trans-ACPD ((±)-trans-ACPD) is an equimolecular mixture of (1S, 3R)- and (1R, 3S)-ACPD. trans-ACPD is a selective agonist of the mGluR (metabotropic glutamate receptor); active at the group I/II mGlu receptors (EC50: 2/1... |
|
T3486 |
3-MATIDA
|
|
GluR
,
NMDAR
|
|
3-MATIDA is an effective mGluR-1 antagonist (IC50: 6.3 μM, rat mGluR-1a). Displays ≥ 40-fold selectivity over other receptors: mGluR-5, mGluR-2, mGluR-4 (mGluR-4a) (IC50 > 300 μM), NMDA and GluR (AMPA) (IC50 = 250 μM). 3... |
|
T17241 |
Auglurant
|
VU0424238 |
Others
|
|
Auglurant is a novel and selective mGlu5 antagonist (IC50: 11 nM (rat) and an IC50: 14 nM (human)). Auglurant has an acceptable CNS penetration. |
|
T10978 |
DCG-IV
|
|
Others
|
|
DCG-IV is an effective agonist of class II mGluR. DCG-IV has anticonvulsant and neuroprotective effects. The EC50 of mGlu2R and mGlu3R are 0.35 and 0.09 μM, respectively. DCG-IV is also a competitive antagonist of Group ... |
