Catalog No.
Product Name
Application
Product Information
Citations
-
Group II/III mGluR Antagonist
CPPG ((RS)-CPPG) is a potent antagonist of group II and III metabotropic glutamate receptors (mGluRs). It demonstrates selective inhibition of group III mGluRs, with an IC50 of 2.2 nM, compared to an IC50 of 46.2 nM for group II mGluRs in rat cerebral cortex. Additionally, CPPG shows minimal activity at group I mGluRs. This compound is valuable for research into neuropharmacology and the modulation of glutamatergic signaling pathways. -
mGluR7 Agonist
AMN082 is a selective mGluR7 agonist that operates through allosteric activation of the receptor signaling pathway. It effectively inhibits cAMP accumulation and promotes GTPĪ³S binding in transfected mammalian cells, with EC50 values ranging from 64 to 290 nM. AMN082 demonstrates notable selectivity for mGluR7 over other mGluR subtypes and ionotropic glutamate receptors, making it a valuable tool for research into neuropharmacology and potential antidepressant effects. -
mGluR7 Allosteric Agonist
CVN636 is a selective allosteric agonist of the metabotropic glutamate receptor 7 (mGluR7) with an EC50 value of 7 nM for human mGluR7. This compound exhibits significant central nervous system (CNS) permeability, making it a valuable tool for exploring mGluR7 modulation. Its potent activity supports research applications in the investigation of neurological disorders and the pharmacological profiling of mGluR7-related pathways. -
mGlu3 Negative Allosteric Modulator
VU6010572 is a potent and selective negative allosteric modulator of the metabotropic glutamate receptor 3 (mGlu3), demonstrating an IC50 of 245 nM. Its high blood-brain barrier penetration makes it suitable for central nervous system studies. This compound is valuable in investigating the role of mGlu3 in neuropsychiatric disorders and evaluating potential therapeutic strategies in related research contexts. -
mGluR Agonist
L-Cysteinesulfinic acid monohydrate is a potent agonist that selectively targets rat metabotropic glutamate receptors (mGluRs), displaying pEC50 values of 3.92 for mGluR1, 4.6 for mGluR5, 3.9 for mGluR2, 2.7 for mGluR4, 4.0 for mGluR6, and 3.94 for mGluR8. This compound is valuable for studies investigating mGluR-mediated signaling pathways and provides insights into neuropharmacological responses. It can be utilized in research applications focused on neurological disorders and synaptic transmission mechanisms. -
mGlu1 Modulator
VU0483605 is a selective positive allosteric modulator of the metabotropic glutamate receptor 1 (mGlu1). It demonstrates strong PAM activity with EC50 values of 390 nM in human and 356 nM in rat, indicating effective modulation across species. This compound is valuable for investigating the role of mGlu1 in neurological disorders and in studying synaptic plasticity and cognitive functions. -
mGluR5 SAM
BMS-984923 is a potent silent allosteric modulator (SAM) of the metabotropic glutamate receptor 5 (mGluR5), characterized by a high binding affinity (Ki = 0.6 nM). This compound effectively inhibits the interaction between PrPC and mGluR5, thereby preventing pathological signaling associated with amyloid-beta oligomers while preserving normal glutamate signaling. BMS-984923 is suitable for research applications related to neurodegenerative diseases and offers favorable pharmacokinetic properties, including enhanced oral bioavailability and the ability to cross the blood-brain barrier. -
mGlu2 Negative Allosteric Modulator
VU6001966 is a potent negative allosteric modulator of the metabotropic glutamate receptor 2 (mGlu2), exhibiting an IC50 of 78 nM, while demonstrating selectivity for mGlu2 over mGlu3 with an IC50 of >30 ĀµM. This compound effectively crosses the blood-brain barrier, making it a valuable tool for neurological research. VU6001966 can also be utilized as a positron emission tomography (PET) tracer for studying mGlu2 dynamics, contributing to the understanding of glutamatergic signaling in various cognitive processes and neuropsychiatric disorders. -
mGlu5 NAM
HTL14242 is an advanced, orally active negative allosteric modulator (NAM) of the metabotropic glutamate receptor 5 (mGlu5). With a pKi of 9.3 and a pIC50 of 9.2, HTL14242 demonstrates significant binding affinity, making it a valuable tool for exploring the role of mGlu5 modulation in neurological disorders. This compound is particularly relevant for research investigating the therapeutic potential in Parkinson's disease. -
Group II mGluRs Agonist
DCG-IV is a potent agonist of group II metabotropic glutamate receptors (mGluRs), displaying EC50 values of 0.35 Ī¼M for mGlu2R and 0.09 Ī¼M for mGlu3R. Additionally, it acts as a competitive antagonist at group I and group III mGluRs, with respective IC50 values of 389 Ī¼M and 22.5-630 Ī¼M. DCG-IV has demonstrated anticonvulsive and neuroprotective properties, making it valuable for research in neurobiology and pharmacology. -
mGlu7 Antagonist
ADX71743 is a highly selective, noncompetitive antagonist of the metabotropic glutamate receptor 7 (mGlu7). This compound demonstrates significant brain penetration, facilitating its efficacy in neurological research. ADX71743 exhibits anxiolytic properties and is utilized in studies exploring treatments for anxiety disorders and related neuropsychiatric conditions. -
mGluR2 PAM
LY487379 is a selective positive allosteric modulator (PAM) of the human metabotropic glutamate receptor 2 (mGluR2). It enhances glutamate-stimulated [35S]GTPĪ³S binding with an EC50 of 1.7 Ī¼M for mGluR2 and >10 Ī¼M for mGluR3. LY487379 has been demonstrated to promote cognitive flexibility and facilitate behavioral inhibition in rat models, making it a valuable tool for schizophrenia research and the exploration of neuropsychological mechanisms. -
mGlu5 Receptor PAM
VU0360172 is a selective positive allosteric modulator of the mGlu5 receptor, exhibiting an EC50 of 16 nM and a Ki of 195 nM. It effectively stimulates polyphosphoinositide (PI) hydrolysis in vivo, an action that is absent in mice lacking the mGlu5 receptor gene. Additionally, VU0360172 features an alkyne group, facilitating its use as a click chemistry reagent that participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, making it valuable for various biochemical applications. -
mGlu2 PAM
JNJ-46281222 is a highly potent positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGlu2, exhibiting nanomolar affinity with a Kd value of 1.7 nM. This compound shows significant modulatory potency, with a pEC50 value of 7.71. It serves as a valuable tool for research applications focused on neuropharmacology, particularly in the context of disorders related to glutamatergic signaling. -
mGlu7 Antagonist
XAP044 is a highly selective antagonist of the metabotropic glutamate receptor subtype 7 (mGlu7), which serves as a key presynaptic modulator of neurotransmission in the central nervous system. It is characterized by significant brain permeability and has been shown to exhibit a broad range of anti-stress effects, as well as antidepressant and anxiolytic-like activity in rodent behavioral models. This compound is useful for research applications aimed at understanding mGlu7's role in neuropsychiatric disorders. -
mGluR2 Modulator
mGluR2 modulator 1 is a potent positive allosteric modulator of the metabotropic glutamate receptor-2 (mGluR2), exhibiting an EC50 of 0.03 Ī¼M and effective blood-brain barrier penetration. This compound is valuable for investigating the role of mGluR2 in neuropsychiatric disorders, particularly in psychosis research, where modulation of glutamatergic signaling may provide therapeutic insights. -
mGluR2/mGluR3 NAM
Decoglurant is a negative allosteric modulator of metabotropic glutamate receptors 2 and 3 (mGluR2/mGluR3). It exhibits potential antidepressant properties, making it a valuable compound for research into mood disorders and neuropharmacology. Decoglurant is of interest for studies focused on the modulation of glutamatergic signaling pathways and the development of new therapeutic strategies for anxiety and depression-related conditions. -
mGluR8 PAM
AZ 12216052 is a positive allosteric modulator of the metabotropic glutamate receptor 8 (mGluR8), enhancing its signaling in retinal ganglion cells. This compound demonstrates notable antianxiety effects and is useful in research focused on anxiety disorders and retinal signaling pathways. Its modulation of mGluR8 activity makes it a valuable tool for investigating therapeutic strategies in neuropsychiatric and ophthalmologic research. -
mGlu1 Positive Allosteric Modulator
VU6004909 is a positive allosteric modulator of the metabotropic glutamate receptor 1 (mGlu1), effectively crossing the blood-brain barrier. With EC50 values of 25.7 nM for human mGlu1 and 31 nM for rat mGlu1, it demonstrates significant modulation of receptor activity. VU6004909 has been shown to reduce dopamine release in the dorsolateral striatum in vivo, indicating potential applications in the treatment of psychotic disorders. -
mGluR5 Antagonist
mGluR5 antagonist-1 is a potent orally active antagonist of the metabotropic glutamate receptor 5 (mGluR5), exhibiting an IC50 value of 11.5 nM. This compound demonstrates notable antidepressant effects, making it a valuable tool for investigating the pathophysiology of depressive disorders. Researchers can utilize mGluR5 antagonist-1 to explore therapeutic strategies for depression and related neurological conditions. -
mGlu3 Negative Allosteric Modulator
ML289 is a selective negative allosteric modulator of the metabotropic glutamate receptor 3 (mGlu3), exhibiting an IC50 value of 0.66 Ī¼M. This compound demonstrates over 15-fold selectivity for mGlu3 when compared to mGlu2 and shows no activity against mGlu5. Additionally, ML289 features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool in click chemistry applications and research involving synaptic transmission and neurological disorders. -
mGluR Modulator
VU0155094 is a positive allosteric modulator that selectively interacts with group III metabotropic glutamate receptors (mGluRs). This compound demonstrates differential activity among various mGluR subtypes, making it an important tool for researching the modulation of synaptic transmission and neuroplasticity. VU0155094 is used to elucidate the roles of mGluRs in neurological disorders and for drug discovery efforts targeting neuropsychiatric conditions. -
Group I mGluR Antagonist
PHCCC is a Group I metabotropic glutamate receptor (mGluR) antagonist with an IC50 of 3 Ī¼M. This compound selectively modulates the mGlu4 receptor, demonstrating potential antiparkinsonian effects. PHCCC is useful for research into neurological disorders and provides insights into the role of mGluRs in synaptic transmission and neuroprotection. -
mGluR2 PAM
AZD-8529 mesylate is a potent and highly selective positive allosteric modulator (PAM) of the metabotropic glutamate receptor 2 (mGluR2), exhibiting an EC50 of 285 nM. It demonstrates no significant allosteric modulation at concentrations up to 25 ĀµM for mGluR subtypes 1, 3, 4, 5, 6, 7, and 8. This compound is instrumental for research on neurological disorders and mGluR2-related signaling pathways. -
mGluR2 Antagonist
mGluR2 antagonist 1 is a selective negative allosteric modulator of the metabotropic glutamate receptor 2 (mGluR2) with an IC50 of 9 nM. This compound demonstrates high potency and oral bioavailability, coupled with excellent brain permeability. It is primarily utilized in research focused on neurological disorders, providing insights into glutamatergic signaling and potential therapeutic interventions. -
mGlu5 Negative Allosteric Modulator
VU6043653 is a potent negative allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGlu5), exhibiting an IC50 value of 325 nM for human mGlu5. This compound selectively influences mGlu5 signaling pathways, making it a valuable tool for studying neuropharmacology and neurodegenerative diseases. Its ability to cross the blood-brain barrier enhances its utility in in vivo research applications focused on central nervous system disorders. -
mGluR Agonist
(S)-3,4-DCPG is a selective agonist of metabotropic glutamate receptor 8a (mGluR8a), exhibiting an EC50 of 31 nM in AV12-664 cells expressing human mGluR8. This compound is valuable for studying mGluR8a-mediated signaling pathways and its role in neurological research. Its selective activation provides a useful tool for investigating potential therapeutic applications in psychiatric and neurological disorders. -
mGlu2 Receptor PAM
CBiPES is a potent positive allosteric modulator of the mGlu2 receptor, exhibiting an EC50 of 92.8 nM. This compound effectively attenuates stress-induced hyperthermia and phencyclidine-induced hyperlocomotor activity, making it a valuable tool in the study of neurological disorders. CBiPES is particularly relevant for research related to Parkinson's disease and other neuropsychiatric conditions. -
mGluR2/3 agonist
Talaglumetad hydrochloride is a potent agonist of the type II metabotropic glutamate receptors, mGluR2 and mGluR3. It plays a crucial role in modulating synaptic transmission and is primarily utilized in research related to anxiety and neuropsychiatric disorders. Talaglumetad serves as a precursor to the more active compound, Eglumegad, facilitating studies aimed at understanding the therapeutic potential of mGluR2/3 modulation. -
mGluR1 Antagonist
YM-298198 hydrochloride is a selective, high-affinity, and orally active non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). This compound is utilized in research studies investigating various neurological disorders, providing insights into mGluR1 signaling pathways and potential therapeutic interventions. -
mGluR Activator
Fasoracetam is an activator of metabotropic glutamate receptors (mGluR), playing a significant role in modulating glutamatergic transmission in the central nervous system. This compound demonstrates potential therapeutic applications in the research of attention-deficit hyperactivity disorder (ADHD) and Alzheimerās disease (AD). Its modulatory effects on synaptic plasticity make it a valuable tool for studying neurological disorders and cognitive enhancement pathways. -
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 ĀµM. 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 (AĪ²) 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 Ī¼M. 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 Ī¼M for hmGluR4a, 4.7 Ī¼M for hmGluR6, 185 Ī¼M for hmGluR7b, and 0.2 Ī¼M 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 GTPĪ³S 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.
