Catalog No.
Product Name
Application
Product Information
Citations
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mGlu7 NAM
VU6012962 is a negative allosteric modulator of the metabotropic glutamate receptor 7 (mGlu7 NAM) with an IC50 of 347 nM. This compound demonstrates oral bioavailability and the ability to penetrate the central nervous system (CNS). VU6012962 is primarily utilized in research focused on neurological disorders and synaptic transmission modulation, providing insights into mGlu7 receptor functions and therapeutic potentials. -
mGlu1a antagonist
UPF-523 is a selective antagonist of the group I metabotropic glutamate receptor mGlu1a, exhibiting a potency with an IC50 of 214 µM. This compound does not influence group II (mGlu2), group III (mGlu4), or ionotropic glutamate receptors. UPF-523 serves as a valuable tool in research related to acute arthritis, facilitating the investigation of therapeutic strategies targeting mGlu1a receptor pathways. -
mGluR Agonist
VU0486321 is a positive allosteric modulator of the metabotropic glutamate receptor 1 (mGluR1), exhibiting significant potency and selectivity for this target. The compound demonstrates a favorable drug metabolism and pharmacokinetics (DMPK) profile along with central nervous system (CNS) permeability. VU0486321 is primarily applicable in research related to neurological disorders and the modulation of synaptic activity, making it a valuable tool for exploring mGluR1-related signaling pathways. -
mGluR5 NAM
Raseglurant hydrochloride is a negative allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). This compound is primarily utilized in research exploring its effects on neurological conditions, particularly migraines, by modulating glutamatergic signaling pathways. Its role in targeting mGluR5 offers potential insights into therapeutic strategies for related disorders. -
mGluR7 Antagonist
MMPIP is a selective allosteric antagonist of metabotropic glutamate receptor 7 (mGluR7) with a high affinity (KB values of 24-30 nM). This compound serves as a valuable tool for investigating the role of mGluR7 in central nervous system functions. Research demonstrates that MMPIP can alleviate pain and restore cognitive and affective behaviors in models of neuropathic pain, making it significant for studies in neuropharmacology and mental health. -
mGlu3 NAM
LY2389575 hydrochloride is a selective noncompetitive negative allosteric modulator (NAM) of the metabotropic glutamate receptor 3 (mGlu3), exhibiting an IC50 value of 190 nM. This compound enhances Mrc1 levels while independently intensifying Amyloid beta (Aβ) toxicity. It serves as a valuable tool for investigations related to Alzheimer's disease and the underlying mechanisms of neurodegeneration. -
mGluR5 Positive Allosteric Modulator
3,3'-Difluorobenzaldazine is a selective positive allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It enhances the efficacy of mGlu5 agonists, including glutamate, quisqualate, and 3,5-dihydroxyphenylglycine, increasing their action by 3- to 6-fold with effective concentrations (EC50) ranging from 2 to 5 μM. This compound is valuable for research applications focused on modulation of glutamatergic signaling and the investigation of neurological disorders associated with mGluR5 dysfunction. -
mGluR Modulator
MNI137 is a potent and selective negative allosteric modulator targeting group II metabotropic glutamate receptors (mGluRs). With IC50 values of 8.3 nM for human mGlu2 and 12.6 nM for rat mGlu2, MNI137 effectively inhibits glutamate-induced calcium mobilization. This compound is valuable for research applications in neuropharmacology and the exploration of mGluR-related disorders. -
mGluR Modulator
Ro 01-6128 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1). This compound enhances receptor activity, contributing to increased signaling through the mGluR pathway. Ro 01-6128 is valuable for investigating mGluR1-related functions in neurological and psychiatric research, as well as exploring its potential therapeutic implications in conditions such as anxiety and depression. -
mGluR Agonist
(RS)-PPG is a selective agonist for group III metabotropic glutamate receptors (mGluRs), exhibiting potent activity with EC50 values of 5.2 μM for hmGluR4a, 4.7 μM for hmGluR6, 185 μM for hmGluR7b, and 0.2 μM for hmGluR8a. This compound demonstrates significant anticonvulsive and neuroprotective effects, making it a valuable tool in neurological research. Its ability to modulate mGluR activity positions (RS)-PPG for potential applications in studying various neuropsychiatric disorders. -
mGluR1 Antagonist
LY456066 is a selective non-competitive antagonist of metabotropic glutamate receptor 1 (mGluR1), exhibiting an IC50 of 52.0 nM. This compound demonstrates significant biological activity in rodent models, effectively reducing hyperalgesia and the pain-related behaviors of licking and flinching in response to formalin injection. LY456066 holds promise for investigating potential analgesic treatments in chronic pain research. -
mGluR5 Antagonist
MTEP is a potent non-competitive antagonist of the metabotropic glutamate receptor 5 (mGluR5), exhibiting an IC50 of 5 nM and a Ki of 16 nM. It demonstrates significant antidepressant and anxiolytic-like effects, making it valuable for research related to mood disorders and neurodegenerative diseases such as Parkinson's disease. Additionally, MTEP contains an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), thus serving as a versatile tool in click chemistry applications. -
mGluR5 NAM
AZD6538 is a selective negative allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It effectively inhibits DHPG-stimulated intracellular calcium release in HEK293 cells expressing either rat or human mGluR5, showing IC50 values of 3.2 nM and 13.4 nM, respectively. This compound is valuable for studying the role of mGluR5 in neuropathic pain and offers insights into potential therapeutic strategies for associated disorders. -
mGluR7 Agonist
AMN082 free base is a selective mGluR7 agonist that activates receptor signaling through an allosteric site within the transmembrane domain. This compound effectively inhibits cAMP accumulation and promotes GTPγS binding at transfected mammalian cells expressing mGluR7, with EC50 values ranging from 64 to 290 nM. AMN082 free base demonstrates selectivity for mGluR7 over other metabotropic glutamate receptor subtypes and certain ionotropic glutamate receptors, highlighting its potential for research in neuroscience and depression-related studies. -
human mGluR5 antagonist
ABP688 is a potent antagonist of the human metabotropic glutamate receptor 5 (mGluR5), with a binding affinity (Ki) of 1.7 nM. This compound serves as a valuable tool in elucidating the role of mGluR5 in various neurological disorders. Additionally, radioisotope-labeled ABP688 can be utilized as a PET tracer for in vivo imaging studies, aiding in the investigation of receptor dynamics and distribution in clinical settings. -
mGluRs Agonist
rel-ACPT-I is a selective agonist of group III metabotropic glutamate receptors (mGluRs) that exhibits neuroprotective, anticonvulsant, and anxiolytic-like properties. This compound plays a significant role in modulating glutamatergic signaling, making it valuable for research in neuropharmacology and mental health disorders. Its diverse biological activities support investigations into therapeutics for conditions such as epilepsy and anxiety disorders. -
mGlu4 Modulator
Valiglurax is a potent, orally active positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4), exhibiting EC50 values of 64.6 nM and 197 nM for human mGlu4/Gqi5 and rat mGlu4 GIRK, respectively. It effectively penetrates the central nervous system (CNS), making it a valuable tool for studying pharmacological pathways involved in neurological disorders. Valiglurax is particularly relevant for research focused on Parkinson's disease, enabling investigations into potential therapeutic interventions. -
mGlu2/3 Receptor Agonist
(rel)-Eglumegad is a highly potent and selective agonist for the group II metabotropic glutamate receptors, specifically mGlu2 and mGlu3. With EC50 values of 5 nM and 24 nM for the transfected human mGlu2 and mGlu3 receptors, respectively, it demonstrates strong receptor activation. This compound has applications in neuroscience research, particularly in studies related to neurological disorders and synaptic modulation. -
mGlu5 SAM Ligand
ML353 is a selective allosteric modulator targeting the metabotropic glutamate receptor 5 (mGlu5) with a Ki value of 18.2 nM. This compound enhances the affinity of common allosteric sites, demonstrating a 20-fold improvement over the previous mGlu5 SAM compound. ML353 is suitable for research applications aimed at elucidating the intrinsic activity of silent allosteric modulators in vivo or for use as an agent blocker. Additionally, as a click chemistry reagent featuring an alkyne group, ML353 can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules. -
mGlu3 Modulator
ML337 is a selective negative allosteric modulator of the metabotropic glutamate receptor 3 (mGlu3), exhibiting an IC50 value of 593 nM. This compound demonstrates effective brain penetration and possesses a favorable drug metabolism and pharmacokinetics (DMPK) profile. Furthermore, ML337 serves as a click chemistry reagent, containing an alkyne group capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. Its unique properties make it valuable for studying mGlu3 function and applications in neuropharmacology. -
mGluR5 Antagonist
ACDPP is a selective antagonist of the metabotropic glutamate receptor 5 (mGluR5). It effectively inhibits the elevation of fragile X mental retardation protein (FMRP) induced by DHPG, a group I mGluR agonist. ACDPP is utilized in research to investigate the role of mGluR5 signaling in neurodevelopmental disorders, particularly in the context of fragile X syndrome. -
mGlu2 PAM
TASP0433864 is a selective positive allosteric modulator (PAM) of the metabotropic glutamate 2 (mGlu2) receptor, exhibiting EC50 values of 199 nM and 206 nM for human and rat mGlu2 receptors, respectively. This compound demonstrates significant antipsychotic activity, making it a valuable tool for research into neuropsychiatric disorders. Its ability to modulate mGlu2 receptor activity highlights its potential in studying glutamatergic signaling and developing new therapeutics for related conditions. -
mGluR5 PAM
VU0285683 is a selective positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGluR5). It demonstrates anxiolytic-like effects in rodent models of anxiety, providing valuable insights into the modulation of glutamatergic signaling. This compound is primarily utilized in biological research focused on anxiety disorders and the pharmacological mechanisms underlying mGluR5 modulation. -
mGluR III Agonist
L-AP4 monohydrate is a selective agonist of group III metabotropic glutamate receptors (mGluR), demonstrating EC50 values of 0.13 μM for mGlu4, 0.29 μM for mGlu8, 1.0 μM for mGlu6, and 249 μM for mGlu7. Its potent activity makes L-AP4 a valuable tool for investigating the physiological roles of mGluR III in various neurological processes. This compound is widely used in research focused on synaptic modulation and potential therapeutic applications for neuropsychiatric disorders. -
mGluR1a Antagonist
LY367385 is a highly selective antagonist of the metabotropic glutamate receptor 1a (mGluR1a). This compound demonstrates an IC50 of 8.8 μM in inhibiting quisqualate-induced phosphoinositide hydrolysis, showcasing its potency in modulating mGluR1a activity. LY367385 has been investigated for its neuroprotective, anticonvulsant, and antiepileptic effects, making it a valuable reagent for research in neuropharmacology and epilepsy studies. -
mGluR4 PAM
VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), exhibiting an EC50 of 4.6 μM. This compound enhances mGluR4 receptor activity, making it a valuable tool for studying glutamatergic signaling. VU0080241 holds potential applications in neurological research and may contribute to the development of therapies for conditions involving glutamate dysregulation. -
mGluR5 Antagonist
MFZ 10-7 is a highly potent and selective negative allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5), exhibiting a Ki of 0.67 nM for rat mGluR5. This compound serves as an essential tool for investigating the pharmacological modulation of mGluR5 activity, particularly in studies of psychiatric and neurodegenerative disorders. Additionally, MFZ 10-7 contains an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it suitable for applications in click chemistry. -
mGluR5 PAM
VU-1545 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with a Ki of 156 nM and an EC50 of 9.6 nM. This compound enhances mGluR5 activity, offering potential insights into synaptic transmission and plasticity. VU-1545 is valuable in research focused on neurological disorders, cognition, and mood regulation, making it a useful tool for studying the role of mGluR5 in various pathological conditions. -
mGlu5 NAM
VU0409106 is a potent and selective negative allosteric modulator (NAM) of the metabotropic glutamate receptor 5 (mGlu5), exhibiting an IC50 of 24 nM. This compound demonstrates anxiolytic effects in rat models, influenced by concentration-dependent mechanisms. Additionally, VU0409106 effectively crosses the blood-brain barrier, making it a valuable tool for investigating mGlu5-related neurological conditions and potential therapeutic strategies in anxiety disorders. -
mGluR2 NAM/mGluR3 PAM
PHCCC(4Me) is a dual-action modulator targeting mGluR2 and mGluR3, functioning as a negative allosteric modulator (NAM) and a positive allosteric modulator (PAM), respectively. This compound exhibits a half maximal inhibitory concentration (IC50) of 1.5 μM for mGluR2 and an effective concentration (EC50) of 8.9 μM for mGluR3. Its unique pharmacological profile makes PHCCC(4Me) valuable for research applications in neuropharmacology, particularly in the study of glutamate receptor functions and potential therapeutic strategies for neurological disorders. -
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.
