Catalog No.
Product Name
Application
Product Information
Citations
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mGluR Modulator
AZ12559322 is a positive allosteric modulator of the metabotropic glutamate receptor 2 (mGluR2), exhibiting a Ki value of 1.31 nM. This compound enhances receptor signaling and has applications in neurological research, particularly in studying conditions related to synaptic transmission and excitatory neurotransmission modulations. Its potent activity makes it a valuable tool for investigating mGluR2 functions and potential therapeutic outcomes in neuropsychiatric disorders. -
mGlu4 PAM
TC-N 22A is a selective positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGlu4), exhibiting an EC50 of 9 nM in human mGlu4-expressing BHK cells. This compound demonstrates minimal activity at other mGlu receptors (EC50 > 10 μM), including mGlu1, 2, 3, 5, and 7. TC-N 22A is suitable for in vivo research studies focused on central nervous system diseases, offering insights into mGlu4-mediated pathways. -
mGlu2 Antagonist
Ro 64-5229 is a selective, non-competitive antagonist of the metabotropic glutamate receptor 2 (mGlu2). This compound has been shown to reduce the presynaptic inhibitory effects mediated by Neuroligin 1, thereby modulating synaptic transmission. Ro 64-5229 is primarily utilized in research exploring neuropharmacology, synaptic plasticity, and potential therapeutic avenues for neuropsychiatric disorders. -
mGluR Antagonist
MTPG is a potent antagonist of metabotropic glutamate receptors 2 (mGluR2) and 3 (mGluR3). It effectively blocks the induction of brain ischemic tolerance facilitated by cerebral ischemic preconditioning. Additionally, MTPG significantly reduces the inhibitory effect of L-CCG-1 on potassium chloride (KCl)-induced dopamine release, making it a valuable tool for research in neuropharmacology and cerebrovascular studies. -
mGlu4R Agonist
Z-Cyclopentyl-AP4 is an orthosteric agonist of the metabotropic glutamate receptor 4 (mGlu4R). It demonstrates high selectivity for mGlu4 over mGlu8, making it a valuable tool for research in neurological studies. Its agonist activity is relevant for investigating the roles of mGlu4 in various physiological and pathological processes, including neuroprotection and modulation of synaptic transmission. -
mGluR Antagonist
BAY 36-7620 is a potent noncompetitive antagonist of the metabotropic glutamate receptor 1 (mGlu1), with an IC50 of 0.16 μM and exhibiting inverse agonist activity. This compound has demonstrated significant antitumor effects by inhibiting mGlu1 receptor activity, leading to reduced AKT phosphorylation in A549 tumor models and improved survival in mice with tumors. Additionally, BAY 36-7620 provides neuroprotective effects in acute subdural hematoma models. It serves as a valuable tool in research focused on non-small cell lung cancer and breast cancer. -
mGluR1a Antagonist
(±)-LY367385 is a potent and selective antagonist of the metabotropic glutamate receptor 1a (mGluR1a). It inhibits quisqualate-induced phosphoinositide hydrolysis with an IC50 value of 8.8 μM, demonstrating significant selectivity over mGluR5a, which has an IC50 greater than 100 μM. This compound is utilized in research applications focused on neuronal signaling and the modulation of excitatory neurotransmission in neurological studies. -
mGluR2 Agonist
GSK1331268 is a selective, orally active agonist of the metabotropic glutamate receptor 2 (mGluR2) with a pEC50 of 6.9. This compound demonstrates effective penetration of the blood-brain barrier, allowing for modulation of glutamate signaling within the central nervous system. GSK1331268 is suitable for research applications focused on neurodegenerative and neuropsychiatric disorders, providing valuable insight into potential therapeutic pathways. -
mGluR1 PAM
Ro 67-4853 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 1 (mGluR1), exhibiting an effective concentration (pEC50) of 7.16 for the rmGlu1a receptor. This compound interacts with the transmembrane domain of the receptor to enhance the potency of L-glutamate, thereby modulating group I mGlu receptors, including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 is useful in research applications focused on enhancing sensory synaptic responses, particularly in models involving repetitive vibrissa stimulation. -
mGluR Modulator
VU0240382 is a modulator of metabotropic glutamate receptor subtype 5 (mGluR5), exhibiting dual mechanisms governed by its allosteric agonist activity. When functioning as an allosteric agonist, VU0240382 effectively activates mGluR5 receptors in cell line studies; however, it does not demonstrate agonist activity in natural biological systems. Its efficacy parallels that of mGluR5 modulators lacking allosteric agonist properties in animal models, making it a valuable tool for researching psychiatric disorders and neurological diseases where mGluR5 is implicated. -
mGlu4 PAM
VU0418506 is a selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4), displaying EC50 values of 68 nM and 46 nM for human and rat mGlu4, respectively. This compound demonstrates potential antiparkinsonian effects, making it a valuable tool for research into neurodegenerative disorders and related therapeutic avenues. Its specificity and efficacy make VU0418506 suitable for studies focused on modulation of glutamatergic signaling pathways in neurological contexts. -
mGluR7 Allosteric Antagonist
mGluR7 antagonist-2 is a potent and selective allosteric antagonist of the metabotropic glutamate receptor 7 (mGluR7), with an IC50 of 20 nM. This compound demonstrates significant selectivity for mGluR7 over other metabotropic glutamate receptors, including mGluR1, mGluR2, mGluR3, mGluR4, mGluR5, mGluR6, and mGluR8. mGluR7 antagonist-2 is valuable for research applications focusing on neuropharmacology and the investigation of glutamatergic signaling pathways. -
mGlu5 Receptor PAM
VU0360172 hydrochloride is a potent and selective positive allosteric modulator (PAM) of the mGlu5 receptor, exhibiting an EC50 value of 16 nM and a Ki of 195 nM. It enhances polyphosphoinositide (PI) hydrolysis in vivo, a process that is abolished in mice lacking the mGlu5 receptor gene. This compound serves as a valuable tool for investigating mGlu5 receptor functions and has potential applications in studying disorders related to synaptic transmission and neuropharmacology. -
mGlu2 Negative Allosteric Modulator
VU6001192 is a selective negative allosteric modulator of the metabotropic glutamate receptor 2 (mGlu2). Demonstrating potent inhibitory activity with an IC50 of 207 nM, VU6001192 does not affect the mGlu3 receptor or other mGlu receptor subtypes. This compound is valuable for research into neurological disorders, particularly in the context of depression. -
mGlu1 Negative Allosteric Modulator
VU0410425 is a negative allosteric modulator of the metabotropic glutamate receptor 1 (mGlu1). It demonstrates potent inhibitory activity in rat mGlu1 with an IC50 value of 140 nM. This compound is suitable for investigating the role of mGlu1 in various central nervous system disorders, providing valuable insights for therapeutic development. -
mGlu2/3 Agonist
MGS0008 is a potent and orally bioavailable agonist of the metabotropic glutamate receptors 2 and 3 (mGlu2/3), exhibiting EC50 values of 29.4 nM and 45.4 nM, respectively. This compound demonstrates significant biological activity in modulating glutamatergic neurotransmission and holds potential for advancing research in central nervous system disorders, including schizophrenia, anxiety, and neurodegenerative diseases. MGS0008 serves as a valuable tool for investigating therapeutic strategies targeting mGlu2 and mGlu3 receptors. -
mGluR Allosteric Modulator
VU 0360223 is a potent negative allosteric modulator of metabotropic glutamate receptors (mGluR) with an IC50 of 61 nM. This compound is useful for studying the modulation of glutamatergic signaling pathways and has potential applications in neuropharmacology and psychiatric research. Its ability to selectively inhibit mGluR may contribute to the understanding of various neurological disorders, making it a valuable tool in chemical biology. -
mGluR2 Modulator
mGluR2 modulator 6 is a selective modulator of the metabotropic glutamate receptor 2 (mGluR2), exhibiting significant anticonvulsant activity in the 6Hz epilepsy model. This compound has demonstrated enhanced efficacy when used in combination with Levetiracetam. It serves as a valuable tool for investigating the mechanisms underlying epilepsy and potential therapeutic strategies. -
mGlu1 Receptor Antagonist
R214127 is a selective antagonist of the mGlu1 receptor, exhibiting IC50 values of 6 nM for rat mGlu1a and 14 nM for human mGlu1a. This compound engages a site within the glutamate binding pocket, competing for the same transmembrane segment VII as other noncompetitive mGlu1 antagonists. R214127 is utilized in research applications focusing on neuromodulation and the elucidation of mGlu1 receptor functions in various physiological and pathological contexts. -
mGlu2 Receptor Modulator
JNJ-46356479 is a selective positive allosteric modulator of the mGlu2 receptor, exhibiting an EC50 value of 78 nM. It demonstrates significant in vivo activity, making it a valuable compound for research into neurological disorders. This reagent is suitable for studies focused on enhancing glutamate signaling and understanding its implications in various therapeutic contexts. -
mGluR1/CaMKIIα Activator
FO-4-15 is an mGluR1/CaMKIIα activator that demonstrates neuroprotective effects against oxidative stress, specifically H2O2, in human neuroblastoma SH-SY5Y cells. This compound enhances cognitive function in mouse models of Alzheimer’s disease by engaging the mGluR1/CaMKIIα signaling pathway, leading to a reduction in amyloid-beta accumulation, hyperphosphorylated Tau, and synaptic damage. It serves as a valuable tool for investigating mechanisms of neuroprotection and cognitive impairment in neurodegenerative diseases. -
mGluR2 Inhibitor
MK-8768 is a potent and selective negative allosteric modulator of the metabotropic glutamate receptor 2 (mGluR2), exhibiting an IC50 value of 9.6 nM. This compound demonstrates excellent bioavailability and brain permeability, making it suitable for investigations into neurological disorders associated with glutamate signaling. It serves as a valuable tool for research applications aimed at understanding the modulation of mGluR2 in various physiological and pathological contexts. -
mGlu5 Antagonist
Remeglurant is a selective, orally active allosteric antagonist of the metabotropic glutamate receptor 5 (mGlu5) with an IC50 of 13 nM. This compound demonstrates significant potential in advancing research related to dyskinesia in Parkinson's disease (PD). It is valuable for studies investigating the modulation of glutamatergic signaling and its impact on movement disorders. -
mGlu4 Agonist, mGlu8 Agonist
FP0429 is a potent full agonist of the metabotropic glutamate receptor 4 (mGlu4) and a partial agonist of metabotropic glutamate receptor 8 (mGlu8), exhibiting EC50 values of 48.3 μM and 56.2 μM, respectively. This compound is valuable for research involving glutamatergic signaling pathways, particularly in the context of neurodegenerative diseases, mood disorders, and other neurological conditions. Its unique pharmacological profile makes it a useful tool for studying the role of mGlu receptors in synaptic transmission and neuronal plasticity. -
mGluR5 Modulator
BMS-955829 is a selective positive allosteric modulator of the mGluR5 receptor, with an EC50 of 2.6 nM. It exhibits no intrinsic agonist activity and demonstrates a low glutamate fold shift of 2.4. Research indicates that BMS-955829 can effectively enhance cognitive and executive function deficits in rodent models. This compound is valuable for investigating cognitive impairment disorders, including schizophrenia. -
mGluR antagonist
MAP4 is a selective antagonist of group III metabotropic glutamate receptors (mGluRs). This compound is utilized in electrophysiological studies to investigate the role of mGluR signaling in various neurological processes. Its application aids in understanding potential therapeutic targets for disorders associated with dysregulated glutamate transmission. -
mGluR5 Positive Aallosteric Modulator
BMS-952048 is a positive allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5), exhibiting an EC50 of 10 nM. This compound enhances mGluR5 signaling, thereby influencing various neurological processes. It is primarily utilized in research focused on neurodegenerative diseases, anxiety, and related disorders, providing valuable insights into glutamatergic neurotransmission modulation. -
mGluR 5 Antagonist
BOMA, a selective antagonist of metabotropic glutamate receptor 5 (mGluR 5), exhibits potent activity with an IC50 and Ki of 3 nM. This compound is valuable in studying a range of pain states, including acute, persistent, chronic, inflammatory, and neuropathic pain. Its specificity and efficacy make it a significant tool for investigating the roles of mGluR 5 in pain modulation and therapeutic interventions. -
mGluR1 Antagonist
YM-202074 fumarate is a selective allosteric antagonist of the metabotropic glutamate receptor type 1 (mGluR1), demonstrating high affinity with a Ki of 4.8 nM. This compound effectively inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells, exhibiting an IC50 of 8.6 nM. Additionally, YM-202074 fumarate exhibits potent neuroprotective effects in models of transient middle cerebral artery occlusion, making it a valuable tool for research on neuroprotection and mGluR1-related pathways. -
mGluR2 PAM
mGluR2 modulator 3 is a potent positive allosteric modulator (PAM) of the metabotropic glutamate receptor 2 (mGluR2), exhibiting an EC50 value of 0.87 μM. This compound demonstrates significant biological activity in preclinical models of psychotic disorders, including methamphetamine-induced hyperactivity and mescaline-induced scratching in mice. It is a valuable reagent for researching the modulation of mGluR2 in the context of neuropsychiatric diseases. -
mGluR2 PAM
mGluR2 modulator 4 is a potent positive allosteric modulator of the metabotropic glutamate receptor 2 (mGluR2), exhibiting an EC50 value of 0.8 μM. This compound enhances receptor function and signaling, making it valuable for investigating antipsychotic mechanisms. Its application in research may provide insights into therapeutic strategies for psychiatric disorders. -
mGlu5 Negative Allosteric Modulator
VU0366248 is a negative allosteric modulator of the metabotropic glutamate receptor type 5 (mGlu5). This compound inhibits mGlu5 receptor signaling, offering potential therapeutic applications in disorders associated with glutamate dysregulation, such as anxiety, depression, and schizophrenia. Researchers can utilize VU0366248 to investigate the functional role of mGlu5 in synaptic plasticity and to explore its implications in neuropharmacology. -
mGluR Activator
VU0477886 is a positive allosteric modulator of metabotropic glutamate receptor subtype 4 (mGlu4), demonstrating potent activation with an EC50 value of 95 nM and achieving 89% of maximal glutamate response. This compound exhibits favorable pharmacokinetic properties, with a brain-to-plasma distribution ratio (Kp) of 1.3, making it a suitable candidate for neurological research. VU0477886 has shown significant therapeutic effects in preclinical models of Parkinson's disease, highlighting its potential for the treatment of movement disorders. -
mGluR Inhibitor
PF470 is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5). It has demonstrated significant efficacy in preclinical models of Parkinson's disease, making it a valuable tool for investigating the role of mGluR5 in neurological disorders. Despite its potential, further clinical development was halted due to concerns identified in toxicology assessments. -
mGluR Agonist
(1S,3R)-ACPD is a potent mGluR agonist that primarily targets metabotropic glutamate receptors. It is known to induce depolarization in pyramidal neurons, making it a valuable tool for studying synaptic transmission and neural signaling pathways. This compound has potential applications in research focusing on neurological disorders and the modulation of synaptic plasticity. -
mGluR5 Negative Allosteric Modulator
DMeOB (3,3'-Dimethoxybenzaldazine) is a negative allosteric modulator of the mGluR5 receptor, exhibiting an IC50 of 3 μM. This compound demonstrates reversible non-competitive inhibition of mGlu5-mediated signaling. DMeOB is instrumental for research into mGluR5-related pathways and may be utilized in studies focused on neurological disorders and psychiatric conditions. -
Group I mGluR Antagonist
HexylHIBO is a selective antagonist of group I metabotropic glutamate receptors, specifically mGlu1a and mGlu5a, with dissociation constants (Kbs) of 140 μM and 110 μM, respectively. This compound has shown efficacy in reducing spontaneous excitatory postsynaptic currents (sEPSCs) in rat models. It does not inhibit mGlu2 and mGlu4a receptors, making it a valuable tool for investigating the role of group I mGluRs in neurological research and the pathophysiology of neuropsychiatric disorders. -
mGluR6 Agonists
1-Benzyl-APDC functions as an agonist for metabotropic glutamate receptor 6 (mGluR6), exhibiting an EC50 of 20 μM in CHO cells. Additionally, it demonstrates weak antagonistic effects on mGluR2, with an IC50 of 200 μM. This compound is useful for studies investigating mGluR6 signaling pathways and the role of glutamate receptors in neurological research. -
mGluR4 Allosteric Agonist
VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). With EC50 values of 798 nM and 693 nM for human and rat mGluR4, respectively, this compound is instrumental in enhancing receptor activity. VU0155041 sodium shows promise in the study of Parkinson's disease, providing a valuable tool for understanding its pathophysiology and developing potential therapeutic strategies. -
mGluR2/3 Agonists
MGS 0210 is a potent mGluR2/3 agonist that demonstrates significant neuroprotective effects. This compound has been shown to enhance cognitive function and alleviate anxiety-related behaviors in animal models of Alzheimer's disease and post-traumatic stress disorder (PTSD). MGS 0210 serves as a valuable tool for investigating therapeutic strategies in various neurological disorders, including major depressive disorder and PTSD. -
mGluR Antagonist
MPPG is a selective antagonist of metabotropic glutamate receptors (mGluRs), specifically targeting L-AP4-sensitive receptors with a KD value of 9.2 μM. This reagent demonstrates significant inhibition of mGluR activity, making it valuable for studying excitatory neurotransmission and synaptic plasticity. Its applications include investigating the role of mGluRs in various neurological conditions using neonatal rat spinal cord models. -
mGlu2 Receptor Agonist
(±)-LY395756 is a potent agonist of the mGlu2 receptor and an antagonist of the mGlu3 receptor. This compound selectively engages the native mGlu2 and mGlu3 receptors, making it a valuable tool for studying glutamate receptor signaling pathways. Its unique pharmacological profile positions it for applications in neurological research and the exploration of potential therapeutic strategies targeting mGlu receptor subtypes. -
mGlu5 Antagonist
VU0431316 is a potent non-competitive antagonist of the metabotropic glutamate receptor 5 (mGlu5), exhibiting an IC50 value of 24 nM. This compound selectively inhibits mGlu5 signaling pathways, making it a valuable tool for research into glutamate-mediated neurological disorders. Its use in various preclinical studies may enhance the understanding of mGlu5 receptor functions and their role in neurobiology. -
mGluR Antagonist
MGS0039 is a type II group metabotropic glutamate receptor (mGluR) antagonist that exhibits high affinity for mGluR2 and mGluR3, with Ki values of 2.2 nM and 4.5 nM, respectively. This compound effectively inhibits glutamate-induced cyclic AMP formation in CHO cells expressing these receptors, suggesting its potential utility in modulating glutamatergic signaling. Additionally, MGS0039 demonstrates antidepressant-like effects in rat models, highlighting its relevance for research in neuropharmacology and mood disorders. -
mGluR2/3 Agonist
LY459477 is a selective and orally active agonist of metabotropic glutamate receptors 2 and 3 (mGluR2/3). It demonstrates significant effectiveness in suppressing locomotor activity induced by phencyclidine without impairing neuromuscular coordination. This compound serves as a valuable tool for investigating neurological diseases and the role of glutamate signaling in related therapeutic contexts. -
mGlu2/mGlu3 Receptor Agonist
LY2934747 is a selective dual agonist for the mGlu2 and mGlu3 receptors, demonstrating blood-brain barrier permeability. With Ki values of 260 nM and 177 nM and EC50 values of 8.4 nM and 62.4 nM for human receptors, it effectively mediates signaling pathways associated with these targets. LY2934747 displays antipsychotic and analgesic activities in vivo, making it a valuable tool for research into psychosis and pain management. -
mGluR1 Antagonist
CFMMC is a selective allosteric antagonist of the metabotropic glutamate receptor 1 (mGluR1). This compound effectively inhibits L-glutamate-induced intracellular calcium mobilization in Chinese hamster ovary cells expressing recombinant human mGluR1a, with an IC50 value of 50 nM. CFMMC is of particular interest for research into a range of central nervous system disorders, including schizophrenia, epilepsy, anxiety, pain, cognitive dysfunction, and substance abuse. -
mGlu1 Receptor Antagonist
YM-230888 is a selective allosteric antagonist of the metabotropic glutamate receptor 1 (mGlu1), exhibiting a binding affinity (Ki) of 13 nM. It effectively inhibits the production of inositol phosphates in rat cerebellar granule cells, with an IC50 of 13 nM. Research indicates that YM-230888 possesses significant antinociceptive effects in models of hyperalgesia induced by Streptozotocin, as well as in complete Freund's adjuvant-induced arthritis pain models, highlighting its potential utility in pain management studies. -
mGlu5 modulator
NCFP is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGlu5). This compound enhances the receptor's activity, making it valuable for investigating therapeutic avenues in central nervous system diseases. Its role in modulating mGlu5 function highlights its potential in understanding neurological disorders and developing novel treatments. -
mGluR2 Agonist
L-CCG-I is a selective mGluR2 agonist, characterized by its conformationally restricted glutamate analog structure. Demonstrating a potent activity with an EC50 value of 0.3 nM, L-CCG-I is instrumental for studies exploring the functions and mechanisms of the mGluR family. This compound is valuable for research applications involving neurotransmission and synaptic plasticity related to mGluR2 signaling pathways.
