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T3483 |
FTIDC
|
|
GluR
|
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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... |
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T6598 |
MPEP
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|
GluR
|
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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. |
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T3482 |
CFMTI
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|
GluR
|
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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. |
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T2497 |
MPEP hydrochloride
|
|
GluR
|
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MPEP hydrochloride is an effective and highly specific non-competitive antagonist at the mGlu5 receptor subtype (IC50: 36 nM). |
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T3477 |
E4CPG
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|
GluR
|
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E4CPG is a novel group I/II metabotropic glutamate receptor antagonist, more potent than (RS)-MCPG. |
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T15275 |
Fenobam
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|
GluR
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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... |
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T3464 |
PHCCC
|
(-) PHCCC |
GluR
|
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PHCCC ((-) PHCCC) is a Group I metabotropic glutamate receptor antagonist and a positive allosteric modulator of mGluR4. It also is a potent to antagonism for mGluR2 and mGluR8. |
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T10573 |
BMT-145027
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|
GluR
|
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BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM). |
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T13441 |
(R)-ADX-47273
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|
GluR
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(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator(EC50 of 168 nM for potentiation ). |
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T13321 |
VU6005649
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|
GluR
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|
|
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T3451 |
JNJ-42153605
|
|
GluR
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JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM). |
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T6725 |
VU 0357121
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|
GluR
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VU0357121, a positive allosteric modulator of mGlu5 (EC50: 33 nM), is inactive or very weakly antagonizing at other mGlu receptor subtypes. |
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T4500 |
ADX88178
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|
GluR
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ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4. |
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T22641 |
CDPPB
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|
GluR
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CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5). |
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T6160 |
VU 0364439
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|
GluR
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VU 0364439 is a mGlu4 positive allosteric modulator (C50: 19.8 nM). |
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T13323 |
VU6012962
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GluR
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|
|
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T8862 |
ML 254
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|
GluR
|
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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... |
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T6727 |
VU0364770
|
VU 0364770 |
GluR
|
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VU0364770 (VU 0364770)(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes. |
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T7494 |
TCN238
|
TCN 238 |
GluR
|
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TCN238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4with an EC50 of 1 μM). |
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T8457 |
NPS2390
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|
GluR
|
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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) |
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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 ... |
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T23514 |
VU-1545
|
VU 1545 |
GluR
|
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VU-1545 is mGlu5 positive allosteric modulator. |
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T9353 |
OXOMEMAZINE
|
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AChR
,
Histamine Receptor
|
|
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic activity. Oxomemazine is a selective antagonist of mycotoxins M1 receptors, showing high (Ki=84 nM, M1 receptors) and low ... |
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T13318 |
VU0650786
|
|
GluR
|
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VU0650786 is a selective and potent CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM) (IC50: 392 nM), with antidepressant and anxiolytic activity in rodents. |
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T12717 |
Basimglurant
|
CTEP Derivative,RG7090 |
GluR
|
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Basimglurant (CTEP Derivative) is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM). |
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T22976 |
MFZ 10-7
|
|
Others
,
GluR
|
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MFZ 10-7 is anegative allosteric modulator of the mGluR5. |
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T21747 |
VU0483605
|
|
GluR
|
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VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively. |
|
T3539 |
Lu AF21934
|
|
GluR
|
|
Lu AF21934 is a brain-penetrant and selective mGlu4 receptor positive allosteric modulator (IC50: 500 nM, human). |
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T23515 |
VU-29
|
VU 29 |
GluR
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|
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). |
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T41301 |
L-Cysteinesulfinic acid monohydrate
|
|
GluR
|
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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... |
|
T15090 |
Decoglurant
|
RO4995819 |
GluR
|
|
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3 and it also is developed as an antidepressant. |
|
T9021 |
Ro0711401
|
Ro-0711401,Ro 0711401 |
GluR
|
|
Ro0711401 is an agonist of mGlu1 receptor. |
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T5512 |
JNJ16259685
|
.TN.T 16259685 |
GluR
|
|
JNJ16259685 (TN.T 16259685) is a selective mGluR1 antagonist, and inhibits the synaptic activation of mGluR1 in a concentration-dependent manner with IC50 of 19 nM. |
|
T29126 |
VU0360172
|
VU-0360172,VU 0360172 |
GluR
|
|
VU0360172 is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM). |
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T6022 |
LY404039
|
pomaglumetad |
Glucocorticoid Receptor
,
GluR
|
|
LY404039 (pomaglumetad) is an effective agonist of recombinant human mGlu2(Ki =149 nM)/mGlu3(Ki =92 nM). |
|
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. |
|
T11032 |
DHPG
|
(RS)-3,5-DHPG |
GluR
|
|
DHPG ((RS)-3,5-DHPG) ((RS)-3,5-DHPG) is an effective antagonist of mGluR linked to phospholipase D. It is an amino acid that can be used as a selective and potent agonist for Group I mGluR (mGluR 1 and mGluR 5) and has n... |
|
T3478 |
Ro 67-7476
|
|
GluR
|
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Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors. No activity at human mGlu1 receptors. Potentiates glutamate-induced calcium release with EC 50 of 60.1 nM. |
|
T3565 |
VU0155041
|
UV0155041,VU-0155041 |
GluR
|
|
VU0155041 is an effective and positive allosteric modulator/allosteric agonist at mGlu4 receptors (EC50: 798/693 nM, at human/rat). |
|
T21995 |
XAP044
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|
GluR
|
|
XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm[1]. |
|
TQ0094 |
JNJ-40411813
|
ADX-71149 |
GluR
|
|
JNJ-40411813 (ADX-71149) (ADX-71149) is a new positive allosteric modulator of the metabotropic glutamate 2 receptor (mGlu2R, EC50: 147 nM). |
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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). |
|
T10432L |
AZD-8529 mesylate
|
|
GluR
|
|
AZD-8529 mesylate is a highly selective, and orally bioavailable positive allosteric modulator of mGluR2 (EC50: 285 nM). It shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 ... |
|
T9011 |
VU0155094
|
ML 397,ML-397,VU 0155094,VU-0155094 |
GluR
|
|
VU0155094 (ML 397) is a positive allosteric modulator with differential activity at the various group III mGluRs. |
|
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... |
|
T6726 |
VU0361737
|
ML-128,VU 0361737 |
GluR
|
|
VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of mGlu4 receptor.The EC50 of VU 0361737 is 240 nM for the human receptors. The EC50 of VU 0361737 is110 nM for rat receptors.It exhibits weak activity... |
|
T7292 |
FITM
|
|
GluR
|
|
FITM is a potent negative allosteric modulator of mGlu1 receptor(Ki : 2.5 nM). |
|
T8434 |
SIB-1757
|
6-methyl-2-[(E)-phenyldiazenyl]pyridin-3 |
GluR
|
|
SIB-1757 (6-methyl-2-[(E)-phenyldiazenyl]pyridin-3) is a selective antagonist of mGlu5 metabotropic glutamate receptor subtype (hmGlu5, IC50 : 0.4 μM) |
|
T21935L |
AMN082 free base
|
AMN082 |
GluR
|
|
AMN082 free base is a metabotropic glutamate receptor 7 allosteric agonist. |
|
T3479 |
(RS)-MCPG
|
alpha-MCPG,(±)-MCPG |
GluR
|
|
(RS)-MCPG ((±)-MCPG) is a non-selective group I/II metabotropic glutamate receptor antagonist. |
