Catalog No.
Product Name
Application
Product Information
Citations
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Melatonin Receptor Antagonist
S-20928 is a selective antagonist of melatonin receptors, inhibiting melatonin’s binding to these receptors. This compound has been demonstrated to enhance the 2-Deoxy-D-glucose (2DG)-induced elevation of blood glucose and glucagon levels in rat brain studies. S-20928 is relevant for research on metabolic regulation and the physiological effects of melatonin modulation. -
MT2 Antagonist
N-Pentanoyl 2-benzyltryptamine is a selective antagonist of the MT2 melatonin receptor, exhibiting a pKi of 8.03 for human MT2. This compound demonstrates significant selectivity, with 89-fold and 229-fold preference for human MT2 over human MT1 and Xenopus mel1c receptor subtypes, respectively. N-Pentanoyl 2-benzyltryptamine effectively inhibits melatonin-induced enhancement of electrically-evoked responses, making it a valuable tool for research in circadian rhythms and melatonin signaling pathways. -
Melatonin Receptor Agonist
Melatonin Receptor Agonist 1 is a selective agonist for the melatonin receptors, specifically showing Ki values of 108 nM for MT2 and 1140 nM for MT1. This compound is useful for studying melatonin signaling pathways and their roles in various physiological processes, including sleep regulation and circadian rhythm modulation. Its potential applications in research extend to areas such as neurobiology, sleep disorders, and the effects of melatonin on metabolic processes. -
MT2 Inverse Agonist/MT1 Antagonist
UCM 549 is an inverse agonist of the melatonin MT2 receptor and an antagonist of the MT1 receptor. This compound modulates melatonin signaling pathways, making it a valuable tool for investigating sleep disorders and circadian rhythm regulation. Its application extends to studies focused on the role of melatonin receptors in neuroprotection and mood regulation. -
MT3 Receptor Agonist
5-MCA-NAT is an agonist of the melatonin MT3 receptor. It has been shown to induce contraction of the colonic band in a concentration-dependent manner and effectively reduce intraocular pressure (IOP) in glaucomatous primate models. This compound is valuable for research applications related to gastrointestinal motility and ocular health, particularly in studies addressing conditions such as glaucoma and colonic issues. -
MT2 Antagonist
DH97-7 is a potent antagonist of the melatonin receptor 2 (MT2), demonstrating a Ki value of 252 nM for MT2 and 1100 nM for MT1. It effectively blocks MT2 receptor activity, making it a valuable tool for research in circadian rhythm regulation and sleep disorders. This compound is suitable for studies aiming to elucidate the biological pathways influenced by melatonin signaling and its therapeutic implications. -
Melatonin Receptor Agonist
6-Chloromelatonin is a highly effective melatonin receptor agonist that exhibits enhanced metabolic stability compared to melatonin. It demonstrates strong binding affinity to the MT1 receptor, competing with both [3H]-melatonin and 2-[125I]-iodomelatonin (pKi = 8.9 and 9.1, respectively). Additionally, 6-Chloromelatonin shows significant competition for [3H]-melatonin binding at MT2 receptors with a pKi value of 9.77. This compound is valuable for research in sleep regulation, circadian rhythms, and neuropharmacology. -
Melatonin Receptor Agonist
GR 196429 is a melatonin receptor agonist primarily targeting the MT1 subtype. This compound has been shown to promote sleep and modify circadian rhythms, in addition to stimulating melatonin release in murine models. It serves as a valuable tool for investigating sleep disorders and the biological mechanisms underlying circadian regulation. -
Inactive Isomer of Melatonin Receptor
(R)-Ramelteon is an orally active compound that serves as an inactive isomer of melatonin receptors 1 and 2. It has been studied for its potential role in modulating sleep patterns and may provide insight into the mechanisms underlying sleep regulation. This compound is of particular interest in research applications related to sleep disorders and circadian rhythm studies. -
Melatonin Receptor Antagonist
GR 128107 is a competitive antagonist of melatonin receptors, exhibiting a high binding affinity with a pKi of 9.6. This compound is utilized in research to investigate the physiological roles of melatonin signaling pathways and its involvement in circadian rhythm regulation. GR 128107 can aid in the exploration of sleep disorders, neurodegenerative diseases, and the modulation of various neurochemical processes. -
Melatonin Receptor Agonist
Nedemelteon is a melatonin receptor agonist that selectively binds to MT1 and MT2 receptors, playing a crucial role in regulating circadian rhythms and sleep-wake cycles. Its primary biological activity includes promoting sleep onset and improving sleep quality, making it valuable for research on sleep disorders and related conditions. This compound is utilized in studies investigating the therapeutic potential of melatonin modulation in various neurological and psychological contexts. -
Melatonin Receptor
Pareptide monohydrochloride is a stable analogue of melanotropin-inhibiting factor (MIF) that primarily targets melatonin receptors. This compound exhibits significant biological activity in modulating melatonin signaling pathways, making it a valuable tool for research in circadian rhythms and sleep disorders. Its application spans various studies focused on neurobiology, pharmacology, and the mechanisms of sleep regulation. -
mGluR5 Negative Allosteric Modulator
VU0477573, a partial negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5), demonstrates brain penetrance and engages in neuroprotective and anxiolytic activities. This compound is of significant interest in the research of neurological disorders, including Parkinson's disease, providing insights into potential therapeutic strategies targeting mGluR5. -
mGlu7 Modulator
VU6010608 is a negative allosteric modulator of the metabotropic glutamate receptor 7 (mGlu7), with an IC50 value of 0.76 μM, and effectively crosses the blood-brain barrier. This compound has been shown to inhibit long-term potentiation (LTP) of Schaffer-collateral CA1 synapses in mouse brain slices induced by high-frequency stimulation. VU6010608 is suitable for research applications investigating neurological disorders and the modulation of synaptic plasticity. -
mGluR1/5 Agonist
DHPG is a potent agonist for metabotropic glutamate receptors mGluR1 and mGluR5, with an EC50 of 60 nM for mGluR1. Its activation triggers the phospholipase C (PLC) signaling pathway, subsequently activating protein kinase C (PKC). DHPG is widely utilized in research to explore synaptic transmission, neuroplasticity, and the therapeutic potential of targeting mGluR signaling in neurological disorders. -
mGluRs Positive Allosteric Modulator
VU0422288 is a positive allosteric modulator of group III metabotropic glutamate receptors (mGluRs). It demonstrates inhibitory activity with EC50 values of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively, as established in calcium mobilization assays. This compound has potential applications in addressing deficits in contextual fear memory, social recognition, and apneas in models of Rett syndrome. -
mGluR1a Antagonist
LY367385 hydrochloride is a selective antagonist of the metabotropic glutamate receptor 1a (mGluR1a). It exhibits a potent inhibitory effect on quisqualate-induced phosphoinositide hydrolysis, with an IC50 value of 8.8 μM. This compound has demonstrated neuroprotective properties and exhibits anticonvulsant and antiepileptic effects, making it valuable for research in neurological disorders and related pharmacological studies. -
mGluR7 Antagonist
MMPIP hydrochloride is a selective allosteric antagonist of the metabotropic glutamate receptor 7 (mGluR7) with KB values ranging from 24 to 30 nM. It serves as a valuable pharmacological tool for investigating the role of mGluR7 in central nervous system functions. Research indicates that MMPIP hydrochloride can alleviate pain and restore normative affective and cognitive behaviors in models of neuropathic pain. -
mGluR Activator
Quisqualic acid is a potent mGluR (metabotropic glutamate receptor) activator derived from the natural source Quisqualis indica. As an excitatory amino acid agonist, it exhibits significant potency with an EC50 of 45 nM and a Ki of 10 nM for mGluR1R. This compound is valuable for research applications involving neurological studies, receptor signaling pathways, and the exploration of excitatory neurotransmission mechanisms. -
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 GTPγS 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 µM. 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 μM for mGlu2R and 0.09 μM for mGlu3R. Additionally, it acts as a competitive antagonist at group I and group III mGluRs, with respective IC50 values of 389 μM and 22.5-630 μM. 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]GTPγS binding with an EC50 of 1.7 μM for mGluR2 and >10 μM 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 μM 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 μM. 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 μM. 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 µM 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 Alzheimer’s disease (AD). Its modulatory effects on synaptic plasticity make it a valuable tool for studying neurological disorders and cognitive enhancement pathways.
