Catalog No.
Product Name
Application
Product Information
Citations
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mGluR2/3 Antagonist
LY3020371 is a highly selective antagonist of the metabotropic glutamate receptors 2 and 3 (mGluR2/3), exhibiting inhibition constants (Kis) of 5.26 nM and 2.50 nM for human mGluR2 and mGluR3, respectively. This compound is primarily utilized in research focused on understanding the pathophysiology of depression and exploring potential therapeutic interventions. Its potent activity against these targets makes it a valuable tool for studying the glutamatergic system in neurological disorders. -
mGluR-2 Antagonist
EGLU ((2S)-α-Ethylglutamic acid; (2S)-α-EGLU) functions as a potent and competitive antagonist of the mGluR-2 receptor. It exhibits robust interaction with the (lS,3S)-ACPD-sensitive site, characterized by a dissociation constant (Kd) of 66 μM. Due to its interference with mGluR-2 signaling, EGLU has potential applications in research exploring its antidepressant properties. -
mGlu5R Modulator
VU-29 is a positive allosteric modulator of the metabotropic glutamate receptor 5 (mGlu5R), demonstrating an EC50 of 9 nM and a Ki of 244 nM for rat mGluR5. This compound exhibits remarkable selectivity for mGlu5R compared to other mGluR subtypes, with EC50 values of 557 nM and 1.5 μM for rat mGluR1 and rat mGluR2, respectively, and 154 nM for human mGluR4. VU-29 is valuable for research exploring mGlu5R modulation in neurological studies, potentially aiding in the understanding of mechanisms underlying various neuropsychiatric disorders. -
mGluR II Antagonist
(RS)-APICA is a selective antagonist of group II metabotropic glutamate receptors (mGluR II). This compound exhibits significant neuroprotective effects, making it a valuable tool for research in neurobiology and related therapeutic applications. It is useful for investigating the role of mGluR II in various neurological conditions. -
mGlu4 PAM
VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGlu4). It demonstrates effective modulation with EC50 values of 290 nM for rat mGlu4 and 1.1 μM for human mGlu4, while also exhibiting antagonist activity against mGlu5 and PAM activity at mGlu6. Additionally, VU0364770 hydrochloride shows inhibition of monoamine oxidase with Ki values of 8.5 μM for human MAO-A and 0.72 μM for human MAO-B, making it valuable for research in neuropharmacology and related fields. -
mGluR3 Modulator
mGluR3 modulator-1 is a selective modulator targeting the mGluR3 receptor, exhibiting an EC50 of 1-10 μM as determined by the HEK293T-mGluR-Gqi5 Calcium Mobilization Assay. This compound plays a crucial role in the modulation of glutamatergic signaling and is valuable for investigating neuropharmacological effects related to anxiety and depression. Its unique mechanism of action makes it a useful tool for research in neurotransmitter systems and related disorders. -
mGluR Antagonist
(RS)-4CPG ((RS)-4-Carboxyphenylglycine) is a type I metabotropic glutamate receptor antagonist that effectively inhibits the induction of long-term potentiation (LTP). In experimental models, notably in mice deficient in IP3R1, (RS)-4CPG at a concentration of 500 µM significantly blocked LTP induction. Research shows an LTP of 117.6±1.7% in IP3R1(-/-) and 116.9±1.8% in IP3R1(+/+) mice, underscoring its potential utility in studies of synaptic plasticity and neuropharmacology. -
mGluR5 Allosteric Modulator
DCB (3,3′-dichlorobenzaldazine) functions as a neutral allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5). It effectively inhibits the positive allosteric enhancement of mGluR5 activity. DCB serves as a valuable tool in research focused on modulating glutamatergic signaling pathways, with implications in understanding neurological disorders and related therapeutic interventions. -
mGlu5 Receptor NEM
Raseglurant (ADX-10059) is a negative allosteric modulator of the mGlu5 receptor, demonstrating potential therapeutic effects in migraine management. This compound has been shown to alleviate Haloperidol-induced catalepsy in murine models, indicating its utility in studying disorders related to dopaminergic signaling. Raseglurant can be employed in research focused on the modulation of mGlu5 receptor activity and its implications in neurological diseases. -
mGlu1 Modulator
VU0469650 is a potent and selective negative allosteric modulator of the mGlu1 receptor, exhibiting an IC50 of 99 nM. This compound demonstrates significant brain penetration, making it a valuable tool for investigating the role of mGlu1 in various neurological conditions. Its primary applications include studying glutamatergic signaling pathways and their implications in disorders such as anxiety and depression. -
Group II mGluRs Agonist
(2R,4R)-APDC is an agonist of the group II metabotropic glutamate receptors (mGluRs). It modulates cell proliferation by inhibiting glutamate release, enhancing motor responses linked to D1 receptor activation, and lowering levels of brain-derived neurotrophic factor (BDNF). This compound is valuable for investigating epilepsy and other neurological disorders, providing insights into glutamatergic signaling and its impact on neurobiology. -
mGluR Antagonist
L-AP3 is a selective antagonist of metabotropic glutamate receptors (mGluRs). It demonstrates inhibitory activity against D-phosphoserine and L-phosphoserine, with IC50 values of 368 μM and 2087 μM, respectively. This compound is valuable for research applications focusing on the modulation of glutamatergic signaling and its implications in various neurological conditions. -
mGlu2/mGlu3 Receptor Agonist
MGS0274 is an ester-based lipophilic prodrug targeting metabotropic glutamate (mGlu) receptors 2 and 3. It exhibits enhanced oral bioavailability compared to its parent compound, MGS0008. MGS0274 is valuable for investigating the role of mGlu2 and mGlu3 receptor modulation in schizophrenia research. -
mGlu5 NAM
VU0463841 is a selective negative allosteric modulator (NAM) of the metabotropic glutamate receptor 5 (mGlu5), demonstrating a potent IC50 of 13 nM. This compound exhibits specificity, showing no significant activity against mGlu1-4 and mGlu7-8. VU0463841 is valuable for research into the mechanisms underlying cocaine addiction and other neuropsychiatric disorders. -
mGluR1 Antagonist
YM-202074 is a selective allosteric antagonist of metabotropic glutamate receptor type 1 (mGluR1) with significant affinity, exhibiting a Ki value of 4.8 nM for rat mGluR1. This compound effectively inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells, with an IC50 of 8.6 nM. Additionally, YM-202074 demonstrates potent neuroprotective effects in transient middle cerebral artery occlusion rat models, making it a valuable tool for research in neuroprotection and glutamatergic signaling pathways. -
mGlu5R Negative Allosteric Modulator
JF-NP-26 is a photocaged derivative of raseglurant that acts as a negative allosteric modulator of the metabotropic glutamate receptor 5 (mGlu5R). When activated by light pulses at 405 nm, JF-NP-26 demonstrates light-dependent analgesic effects in models of inflammatory and neuropathic pain in vivo. This unique capability provides valuable insights into the modulation of mGlu5 receptors and their role in pain pathways, facilitating research in neuropharmacology and pain management. -
mGluR1 Antagonist
Desmethyl-YM-298198 hydrochloride is a selective and noncompetitive antagonist of the metabotropic glutamate receptor 1 (mGluR1), with an IC50 value of 16 nM. This compound exhibits notable analgesic effects in mouse models of hyperalgesia induced by Streptozotocin. Its unique mechanism of action makes it a valuable tool for research into pain modulation and the role of mGluR1 in neurological disorders. -
Group III mGluR Antagonist
UBP 1112 is a selective antagonist of group III metabotropic glutamate receptors (mGluRs), demonstrating a dissociation constant (Kd) of 5.1 μM. This compound exhibits a 96-fold preference for group III mGluRs over group II receptors, with a Kd value of 488 μM for the latter. UBP 1112 does not display significant activity at group I mGluRs or ionotropic glutamate receptors (iGluRs). This specificity positions UBP 1112 as a valuable tool for studying the physiological and pathological roles of group III mGluRs in various neurological research applications. -
mGlu5 Modulator
LSN2814617 is a selective positive allosteric modulator of the metabotropic glutamate receptor 5 (mGlu5), exhibiting potent oral bioactivity with EC50 values of 52 nM in human and 42 nM in rat models. This compound has demonstrated a wake-promoting effect, making it a valuable tool in the investigation of neurological disorders. LSN2814617 is particularly relevant for research focused on schizophrenia and related conditions, where modulation of glutamatergic signaling may provide therapeutic insights. -
mGlu2 Receptor Modulator
JNJ-40068782 is a potent positive allosteric modulator of the metabotropic glutamate receptor 2 (mGlu2). With an IC50 value of 38 nM, this compound enhances mGlu2 receptor activity, influencing various neurobiological processes. It is primarily utilized in research investigating neurological disorders and psychiatric conditions, providing insight into mGlu2 signaling pathways and potential therapeutic applications. -
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.
