Catalog No.
Product Name
Application
Product Information
Citations
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mGluR2 modulator
mGluR2 modulator 5 is a selective negative allosteric modulator of the mGluR2 receptor, exhibiting an IC50 of 8.9 nM. This compound is orally active and demonstrates the ability to cross the blood-brain barrier, as confirmed by pharmacokinetic studies in rats. Its modulation of cognitive and neurological functions makes it a valuable tool for investigating mood disorders and neurodegenerative diseases in preclinical research settings. -
mGlu1R Antagonist
A-794282 is a selective antagonist of the metabotropic glutamate receptor 1 (mGlu1R), primarily functioning to modulate pain signaling. This compound exhibits notable analgesic activity, effectively reducing pain behaviors in models of postoperative pain. Caution is advised, as higher doses may produce motor side effects, making it a critical focus for research in pain management and pharmacology. -
mGluR5 Positive Allosteric Modulator
mGluR5 modulator 1 is a positive allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). This compound enhances mGluR5 receptor activity and is relevant for research into schizophrenia and cognitive impairments. Its ability to modulate glutamatergic signaling may provide insights into therapeutic strategies for neuropsychiatric disorders. -
mGlu4 Agonist
LSP4-2022 is a selective orthosteric agonist of the metabotropic glutamate receptor subtype 4 (mGlu4) with an effective concentration (EC50) of 0.11 μM. This compound effectively inhibits neurotransmission in cerebellar slices derived from wild-type mice, demonstrating its functional specificity, as this effect is absent in mGlu4 receptor-knockout mice. Additionally, LSP4-2022 exhibits pro-depressant activity, making it a valuable tool for research in neuropharmacology and the study of mood disorders. -
mGluR2 PAM
LY487379 hydrochloride is a selective positive allosteric modulator (PAM) of the human mGluR2 receptor. It enhances glutamate-stimulated [35S]GTPγS binding, exhibiting an EC50 value of 1.7 μM for mGluR2, and shows significantly lower activity at mGlu3 receptors. This compound has demonstrated potential in promoting cognitive flexibility and facilitating behavioral inhibition in rat models, making it a valuable reagent for schizophrenia research and the study of related neuropsychiatric disorders. -
mGluR4 PAM
VU0361747 is a selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM). This compound exhibits neuroprotective effects and has been shown to significantly reverse amphetamine-induced hyperlocomotion in vivo. It is a valuable tool for research into neuropharmacology and the modulation of glutamatergic signaling pathways. -
mGluR Agonist
DL-AP4 sodium (2-Amino-4-phosphonobutyric acid sodium) is a potent agonist for metabotropic glutamate receptors (mGluR), specifically targeting mGluR4. This compound activates a signaling pathway that inhibits adenylate cyclase activity, consequently reducing Forskolin-induced cAMP production. Additionally, DL-AP4 sodium functions as an inhibitor of ON channels, leading to decreased sensitivity of photoreceptors to variations in brightness. These properties make it a valuable tool for research in neuropharmacology and synaptic plasticity. -
mGlu2/3 Antagonist
Ro-65-3479 is a selective antagonist of the metabotropic glutamate receptors mGlu2 and mGlu3. This compound effectively inhibits glutamate-induced signaling and modulates calcium channel activity. Ro-65-3479 is of particular interest in the research of disorders associated with glutamatergic dysregulation, including anxiety, schizophrenia, and neurodegenerative diseases. -
mGluR2 PAM
mGluR2 modulator 2 is a potent, selective positive allosteric modulator of the metabotropic glutamate receptor 2 (mGluR2), demonstrating an EC50 value of 0.13 μM. This compound enhances mGluR2 activity, making it a valuable tool for investigating its role in antipsychotic research. It is suitable for in vitro studies and can facilitate a deeper understanding of mGluR2-related pathways in various neuropsychiatric disorders. -
mGluR5 Negative Allosteric Modulator
Basimglurant sulfate is a selective negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5). With a Ki of 1.4 nM, it effectively inhibits mGlu5-mediated signaling and receptor constitutive activity, impacting dopamine regulation in the nucleus accumbens. This compound demonstrates anxiolytic, antidepressant-like, analgesic, and arousal-promoting effects, while also influencing δ-wave power during non-rapid eye movement sleep. Basimglurant sulfate is valuable for research applications in areas such as depression, anxiety disorders, and fragile X syndrome. -
mGlu5 PAM
VU0092273 is a potent positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5), exhibiting an EC50 value of 0.27 μM. This compound enhances mGlu5 receptor activity by binding to the MPEP site, thereby increasing the responsiveness of the receptor to glutamate. VU0092273 is utilized in research applications investigating synaptic plasticity, neuroprotection, and potential therapeutic strategies for neuropsychiatric disorders. -
mGluR Agonist
THIIC (LY2607540) is a positive allosteric modulator of metabotropic glutamate receptors (mGluRs). This compound exhibits significant anxiolytic and antidepressant-like activities in various animal models, making it a valuable tool for studying anxiety and depression mechanisms. Additionally, THIIC impacts sleep patterns and induces neurochemical alterations, providing further insights into its pharmacological profile and potential therapeutic applications in neuropsychiatric disorders. -
mGlu4 Receptor Agonist
mGlu4 receptor agonist 1 is a potent positive allosteric modulator targeting the mGlu4 receptor, exhibiting an EC50 value of 308 nM. This compound has demonstrated significant anxiolytic and antipsychotic-like activity, making it a valuable tool for research into neuropharmacology and the modulation of glutamatergic processes. Its unique mechanism of action offers potential insights into the treatment of anxiety and psychotic disorders. -
mGlu 5 Negative Allosteric Modulator
VU6031545 is a potent negative allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGlu 5), exhibiting an IC50 of 15 nM. This compound demonstrates significant brain penetrance and oral bioavailability in rat models, making it valuable for exploring the role of mGlu 5 in neurological disorders. Research applications include the investigation of anxiety, depression, and other neuropsychiatric conditions. -
mGluR Agonist
Lu AF11205 is a positive allosteric modulator of the mGlu5 receptor, enhancing its activity through a unique mechanism. This compound has demonstrated potent biological activity and is useful in studying mGlu5 receptor involvement in various neurological processes. Research applications include examining its effects in cellular models that express mGlu5 receptors, providing insights into potential therapeutic pathways for neurological disorders. -
mGluR Receptor Agonist
LY2979165 free base is a selective and potent orthosteric agonist of the mGluR2 receptor. This compound exhibits significant biological activity in modulating glutamatergic signaling, making it valuable for research into neuropharmacology and the potential treatment of various neurological disorders. Its ability to enhance mGluR2 receptor activity provides a promising avenue for understanding synaptic function and the development of therapeutic agents targeting glutamatergic pathways. -
mGlu Positive Allosteric Modulator
VU0404251 is a potent positive allosteric modulator of the metabotropic glutamate receptor (mGlu). This compound enhances receptor activity and is invaluable for research into neuropsychiatric disorders, including psychosis. Its ability to modulate glutamatergic signaling makes it a promising tool for studies aimed at unraveling the underlying mechanisms of related pathologies. -
mGlu2/3 Receptor Agonist
MGS0028 is a selective agonist for the metabotropic glutamate 2/3 (mGlu2/3) receptors. This compound has been shown to exhibit robust biological activity, making it a valuable tool in the study of psychiatric disorders. It is particularly relevant for research focused on mGlu2/3 receptor modulation and its implications in neuropharmacology. -
mGluR5 NAM
MFZ 10-7 hydrochloride is a potent and selective negative allosteric modulator (NAM) of the metabotropic glutamate receptor 5 (mGluR5), exhibiting a Ki of 0.67 nM for rat mGluR5. This compound serves as a valuable tool in neurological research, particularly for studies related to synaptic transmission and potential therapeutic approaches for neurodegenerative diseases. Furthermore, MFZ 10-7 hydrochloride features an alkyne group, enabling its use in click chemistry applications, including copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-bearing molecules. -
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.
