Catalog No.
Product Name
Application
Product Information
Citations
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mGlu5 Negative Allosteric Modulator
VU0366248 is a negative allosteric modulator of the metabotropic glutamate receptor type 5 (mGlu5). This compound inhibits mGlu5 receptor signaling, offering potential therapeutic applications in disorders associated with glutamate dysregulation, such as anxiety, depression, and schizophrenia. Researchers can utilize VU0366248 to investigate the functional role of mGlu5 in synaptic plasticity and to explore its implications in neuropharmacology. -
mGluR Activator
VU0477886 is a positive allosteric modulator of metabotropic glutamate receptor subtype 4 (mGlu4), demonstrating potent activation with an EC50 value of 95 nM and achieving 89% of maximal glutamate response. This compound exhibits favorable pharmacokinetic properties, with a brain-to-plasma distribution ratio (Kp) of 1.3, making it a suitable candidate for neurological research. VU0477886 has shown significant therapeutic effects in preclinical models of Parkinson's disease, highlighting its potential for the treatment of movement disorders. -
mGluR Inhibitor
PF470 is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5). It has demonstrated significant efficacy in preclinical models of Parkinson's disease, making it a valuable tool for investigating the role of mGluR5 in neurological disorders. Despite its potential, further clinical development was halted due to concerns identified in toxicology assessments. -
mGluR Agonist
(1S,3R)-ACPD is a potent mGluR agonist that primarily targets metabotropic glutamate receptors. It is known to induce depolarization in pyramidal neurons, making it a valuable tool for studying synaptic transmission and neural signaling pathways. This compound has potential applications in research focusing on neurological disorders and the modulation of synaptic plasticity. -
mGluR5 Negative Allosteric Modulator
DMeOB (3,3'-Dimethoxybenzaldazine) is a negative allosteric modulator of the mGluR5 receptor, exhibiting an IC50 of 3 μM. This compound demonstrates reversible non-competitive inhibition of mGlu5-mediated signaling. DMeOB is instrumental for research into mGluR5-related pathways and may be utilized in studies focused on neurological disorders and psychiatric conditions. -
Group I mGluR Antagonist
HexylHIBO is a selective antagonist of group I metabotropic glutamate receptors, specifically mGlu1a and mGlu5a, with dissociation constants (Kbs) of 140 μM and 110 μM, respectively. This compound has shown efficacy in reducing spontaneous excitatory postsynaptic currents (sEPSCs) in rat models. It does not inhibit mGlu2 and mGlu4a receptors, making it a valuable tool for investigating the role of group I mGluRs in neurological research and the pathophysiology of neuropsychiatric disorders. -
mGluR6 Agonists
1-Benzyl-APDC functions as an agonist for metabotropic glutamate receptor 6 (mGluR6), exhibiting an EC50 of 20 μM in CHO cells. Additionally, it demonstrates weak antagonistic effects on mGluR2, with an IC50 of 200 μM. This compound is useful for studies investigating mGluR6 signaling pathways and the role of glutamate receptors in neurological research. -
mGluR4 Allosteric Agonist
VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). With EC50 values of 798 nM and 693 nM for human and rat mGluR4, respectively, this compound is instrumental in enhancing receptor activity. VU0155041 sodium shows promise in the study of Parkinson's disease, providing a valuable tool for understanding its pathophysiology and developing potential therapeutic strategies. -
mGluR2/3 Agonists
MGS 0210 is a potent mGluR2/3 agonist that demonstrates significant neuroprotective effects. This compound has been shown to enhance cognitive function and alleviate anxiety-related behaviors in animal models of Alzheimer's disease and post-traumatic stress disorder (PTSD). MGS 0210 serves as a valuable tool for investigating therapeutic strategies in various neurological disorders, including major depressive disorder and PTSD. -
mGluR Antagonist
MPPG is a selective antagonist of metabotropic glutamate receptors (mGluRs), specifically targeting L-AP4-sensitive receptors with a KD value of 9.2 μM. This reagent demonstrates significant inhibition of mGluR activity, making it valuable for studying excitatory neurotransmission and synaptic plasticity. Its applications include investigating the role of mGluRs in various neurological conditions using neonatal rat spinal cord models. -
mGlu2 Receptor Agonist
(±)-LY395756 is a potent agonist of the mGlu2 receptor and an antagonist of the mGlu3 receptor. This compound selectively engages the native mGlu2 and mGlu3 receptors, making it a valuable tool for studying glutamate receptor signaling pathways. Its unique pharmacological profile positions it for applications in neurological research and the exploration of potential therapeutic strategies targeting mGlu receptor subtypes. -
mGlu5 Antagonist
VU0431316 is a potent non-competitive antagonist of the metabotropic glutamate receptor 5 (mGlu5), exhibiting an IC50 value of 24 nM. This compound selectively inhibits mGlu5 signaling pathways, making it a valuable tool for research into glutamate-mediated neurological disorders. Its use in various preclinical studies may enhance the understanding of mGlu5 receptor functions and their role in neurobiology. -
mGluR Antagonist
MGS0039 is a type II group metabotropic glutamate receptor (mGluR) antagonist that exhibits high affinity for mGluR2 and mGluR3, with Ki values of 2.2 nM and 4.5 nM, respectively. This compound effectively inhibits glutamate-induced cyclic AMP formation in CHO cells expressing these receptors, suggesting its potential utility in modulating glutamatergic signaling. Additionally, MGS0039 demonstrates antidepressant-like effects in rat models, highlighting its relevance for research in neuropharmacology and mood disorders. -
mGluR2/3 Agonist
LY459477 is a selective and orally active agonist of metabotropic glutamate receptors 2 and 3 (mGluR2/3). It demonstrates significant effectiveness in suppressing locomotor activity induced by phencyclidine without impairing neuromuscular coordination. This compound serves as a valuable tool for investigating neurological diseases and the role of glutamate signaling in related therapeutic contexts. -
mGlu2/mGlu3 Receptor Agonist
LY2934747 is a selective dual agonist for the mGlu2 and mGlu3 receptors, demonstrating blood-brain barrier permeability. With Ki values of 260 nM and 177 nM and EC50 values of 8.4 nM and 62.4 nM for human receptors, it effectively mediates signaling pathways associated with these targets. LY2934747 displays antipsychotic and analgesic activities in vivo, making it a valuable tool for research into psychosis and pain management. -
mGluR1 Antagonist
CFMMC is a selective allosteric antagonist of the metabotropic glutamate receptor 1 (mGluR1). This compound effectively inhibits L-glutamate-induced intracellular calcium mobilization in Chinese hamster ovary cells expressing recombinant human mGluR1a, with an IC50 value of 50 nM. CFMMC is of particular interest for research into a range of central nervous system disorders, including schizophrenia, epilepsy, anxiety, pain, cognitive dysfunction, and substance abuse. -
mGlu1 Receptor Antagonist
YM-230888 is a selective allosteric antagonist of the metabotropic glutamate receptor 1 (mGlu1), exhibiting a binding affinity (Ki) of 13 nM. It effectively inhibits the production of inositol phosphates in rat cerebellar granule cells, with an IC50 of 13 nM. Research indicates that YM-230888 possesses significant antinociceptive effects in models of hyperalgesia induced by Streptozotocin, as well as in complete Freund's adjuvant-induced arthritis pain models, highlighting its potential utility in pain management studies. -
mGlu5 modulator
NCFP is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGlu5). This compound enhances the receptor's activity, making it valuable for investigating therapeutic avenues in central nervous system diseases. Its role in modulating mGlu5 function highlights its potential in understanding neurological disorders and developing novel treatments. -
mGluR2 Agonist
L-CCG-I is a selective mGluR2 agonist, characterized by its conformationally restricted glutamate analog structure. Demonstrating a potent activity with an EC50 value of 0.3 nM, L-CCG-I is instrumental for studies exploring the functions and mechanisms of the mGluR family. This compound is valuable for research applications involving neurotransmission and synaptic plasticity related to mGluR2 signaling pathways. -
mGluR Modulator
GRN-529 is a negative allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It has demonstrated the ability to modulate sleep-wake activity and exhibits anxiolytic effects in rodent models. This compound is of significant interest for research into sleep disorders and anxiety-related conditions, providing insights into mGluR5-targeted therapeutic strategies. -
mGlu2/3 Receptor Negative Allosteric Modulator
RO4988546 is a negative allosteric modulator (NAM) of metabotropic glutamate receptors 2 and 3 (mGlu2 and mGlu3). This compound decreases the binding affinity of [3H]-LY354740 at the receptor's positive allosteric site, which impacts G protein coupling and intracellular signaling pathways. RO4988546 is valuable for research in developing antidepressants and cognitive enhancers, offering insights into therapeutic mechanisms targeting glutamatergic signaling. -
mGluR Agonist
LSP1-2111 is a phosphinic glutamate derivative that functions as an agonist of metabotropic glutamate (mGlu) receptors. This compound demonstrates significant biological activity in modulating neuronal signaling pathways associated with glutamate transmission. It is primarily used in research applications focusing on neurological disorders, synaptic plasticity, and the exploration of mGlu receptor functions. -
mGluR 1a Antagonist/GluR2 Agonist
(S)-4C3HPG, a selective antagonist of metabotropic glutamate receptor 1a (mGluR 1a) and agonist of GluR2, exhibits significant anticonvulsant properties. This compound demonstrates protective effects against audiogenic seizures in DBA/2 mice, making it a valuable tool for research in epilepsy and related neurological disorders. Its dual action on glutamate receptors positions (S)-4C3HPG as a promising candidate for studies aimed at understanding the modulation of excitatory neurotransmission. -
mGluRs III Antagonist
ACPT-II is a selective antagonist of group III metabotropic glutamate receptors (mGluRs), notably influencing neurotransmitter release and signaling pathways. This compound exhibits neuroprotective, anticonvulsant, and anxiolytic-like properties, making it valuable for research in neurological disorders. Its unique profile allows for the exploration of glutamatergic modulation in various models of disease. -
mGluR5 Partial Antagonist
VU0029251 is a partial antagonist of the metabotropic glutamate receptor subtype 5 (mGluR5), exhibiting a binding affinity with a Ki value of 1.07 μM. It effectively inhibits glutamate-induced calcium mobilization in HEK293 cells expressing rat mGluR5, with an IC50 of 1.7 μM. This compound is valuable for research into mGluR5-related signaling pathways and potential therapeutic applications in neurological disorders. -
mGluR5 Negative Allosteric Modulator
PF-06422913 is a potent and selective negative allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). This compound exhibits significant biological activity in modulating glutamatergic signaling, making it valuable in the study of neuropsychiatric disorders. Its applications include investigating therapeutic strategies for conditions such as anxiety and schizophrenia, where mGluR5 activity is implicated. -
mGluR1 Antagonist
Desmethyl-YM-298198 is a high-affinity, selective noncompetitive antagonist of the metabotropic glutamate receptor 1 (mGluR1), exhibiting an IC50 value of 16 nM. This compound demonstrates significant analgesic properties in models of neuropathic pain, specifically in Streptozotocin-induced hyperalgesia. It serves as a valuable tool in research aimed at understanding the role of mGluR1 in pain modulation and the development of therapeutic strategies for pain disorders. -
mGluR Antagonist
A-850002 is a selective antagonist of metabotropic glutamate receptors (mGluRs) with an IC50 of 27 nM. This compound has been shown to significantly reduce spontaneous pain behavior following skin incision in rodent models. A-850002 is suitable for research applications focused on analgesia and the investigation of pain pathways. -
mGluR1 Agonist
(S)-3-Hydroxyphenylglycine is a selective agonist of the metabotropic glutamate receptor 1 (mGluR1). This compound demonstrates significant biological activity in modulating mGluR1 signaling pathways, making it valuable for research focused on neuropharmacology and neural signaling. Its lack of effect on mGlu2 and mGlu4 further underscores its specificity, facilitating studies on mGluR1-related physiological and pathological processes. -
mGluR Inhibitor
Ro4491533 is a selective negative allosteric modulator of the mGluR2 and mGluR3 receptors. It effectively inhibits glutamate-induced calcium mobilization and decreases [35S]GTPγS binding, demonstrating its capacity to modulate glutamatergic signaling. This compound exhibits favorable pharmacokinetic properties, including high oral bioavailability and the ability to penetrate the blood-brain barrier. Additionally, Ro4491533 has shown potential in reversing motor inhibition caused by LY379268 and displays antidepressant effects in various behavioral tests such as the forced swim test and tail suspension test. -
mGluR1 antagonist
(RS)-4C3HPG, or 4-Carboxy-3-hydroxyphenylglycine, serves as a competitive antagonist of the metabotropic glutamate receptor 1 (mGluR1) in the central nervous system and acts as an agonist at mGluR2/3. This compound demonstrates neuroprotective properties in models of acute global ischemia, making it a valuable tool for investigating glutamate receptor signaling and associated neuroprotective mechanisms. Its dual activity presents opportunities for research in neurodegenerative diseases and synaptic modulation. -
Motilin Receptor Antagonist
MA-2029 is a selective, orally active antagonist of the motilin receptor, exhibiting an IC50 of 4.9 nM. It demonstrates high selectivity for the motilin receptor compared to a variety of other receptors and ion channels. This compound is particularly relevant for research into gastrointestinal disorders linked to impaired gastrointestinal motility, providing a valuable tool for studying motility-related pathophysiology and potential therapeutic interventions. -
Motilin Receptor Agonist
Motilin (26-47), human, porcine is a potent agonist of the motilin receptor, exhibiting a Ki value of 2.3 nM and an EC50 of 0.3 nM in a Chinese hamster ovary cell line. This peptide plays a critical role in gastrointestinal motility and is instrumental in research focused on digestive system disorders and hormone signaling pathways. Its application extends to various studies involving gut motility regulation and the therapeutic potential of motilin-related compounds. -
Smooth Muscle Contraction Agonist
Motilin, canine is a 22-amino acid peptide that acts as a potent agonist of gastrointestinal smooth muscle contraction. This bioactive peptide plays a crucial role in stimulating intestinal motility and has potential applications in gastrointestinal research. It is primarily used to study motility disorders and the regulation of digestive processes in canine models. -
Motilin Agonist
KC-11458 is a motilin agonist that enhances gastric motility by stimulating motilin receptors in the gastrointestinal tract. This compound is primarily used for research into gastrointestinal motility disorders and can be valuable in studies investigating the regulation of gastric emptying processes. Its ability to accelerate gastric emptying makes it a potential tool for exploring therapeutic targets in digestive disorders. -
Motilin Agonist
EM-523 is a motilin agonist and an erythromycin derivative that selectively targets motilin receptors. It has demonstrated biological activity with pED50 values of 8.19 and 6.08 for inducing contractions in rabbit small intestinal tissue and human duodenal tissue, respectively. This compound is valuable for investigating gastrointestinal diseases and advancing research related to motility disorders. -
Motilin Analogue
[Leu13]-Motilin is a motilin analogue that primarily targets motilin receptors. This compound promotes gastrointestinal motility by inducing concentration-dependent contractions in various segments of the gastrointestinal tract, including the gastric antrum, duodenum, jejunum, ileum, and descending colon. [Leu13]-Motilin is utilized in research to explore the mechanisms of gut motility and to investigate potential therapeutic applications in gastrointestinal disorders. -
Motilin Antagonist
ANQ-11125 is a potent and selective antagonist of motilin, exhibiting a pKd of 8.24. This compound effectively inhibits motilide-induced contractions in vitro in rabbit models, making it a valuable tool for studying gastrointestinal motility and related disorders. ANQ-11125 has potential applications in research focused on gastrointestinal physiology and pharmacology. -
Gastrointestinal Hormone
Motilin, human, porcine, is a gastrointestinal hormone that plays a critical role in regulating gastrointestinal motility. Released during fasting, eating, and water intake, Motilin enhances enteric cholinergic activity in the human stomach with an EC50 of 33 nM. This biological activity makes it a valuable tool for research into gastrointestinal function and motility disorders. -
Motilin Receptor Agonist
Mitemcinal fumarate is a selective agonist of the motilin receptor. It demonstrates significant biological activity in promoting defecation and increasing stool bulk without causing excessive diarrhea, as evidenced in preclinical studies in rabbits and dogs. Its rapid onset and short duration of action suggest potential applications in the treatment of constipation, making it a valuable compound for gastrointestinal research. -
Motilin receptor agonist
Mitemcinal is an oral motilin receptor agonist, specifically targeting motilin pathways to enhance gastrointestinal motility. Research demonstrates its capability to promote defecation in animal models, such as rabbits and dogs, without inducing severe diarrhea. Additionally, Mitemcinal increases stool weight while maintaining water content and reduces the latency to first defecation in dogs. This makes Mitemcinal a promising candidate for studies on constipation management and gastrointestinal disorders. -
Motilin Receptor Agonist
EM574 is a potent agonist of the motilin receptor, demonstrating significant activity in the human gastric antrum and rabbit gastrointestinal tract in vitro. As an erythromycin derivative, EM574 is utilized in research applications exploring gastrointestinal motility and related disorders. Its ability to selectively modulate motilin receptor signaling makes it a valuable tool for advancing studies in gastrointestinal physiology and pharmacology. -
Motilin Receptor Agonist
[Nle13]-Motilin is a synthetic analog of motilin that functions as a motilin receptor agonist. It effectively stimulates gastrointestinal motility by activating the motilin receptor, making it a valuable tool in studies related to gastrointestinal physiology and potential therapeutics for gut motility disorders. Research applications include investigations into the modulation of gastric emptying and the treatment of gastrointestinal dysmotility. -
Motilin Receptor Agonist
Atilmotin is a selective motilin receptor agonist with a pKd value of 8.94. It enhances gastrointestinal motility by increasing lower esophageal sphincter (LES) and gastric pressures, making it a valuable tool for studying esophageal and gastric motility. This compound is particularly relevant for research applications focused on gastrointestinal disorders and the development of prokinetic agents. -
Motilin Receptor Antagonist
RWJ-68022 is a cyclopentene derivative that acts as a motilin receptor antagonist. It effectively competes with motilin and erythromycin for binding to the motilin receptor site. This compound is valuable in research related to gastrointestinal disorders, providing insights into motilin's role in digestive physiology and its potential therapeutic applications. -
NPR3 Antagonist
AP 811 is a selective antagonist of the natriuretic peptide clearance receptor (NPR3) with a binding affinity (Ki) of 0.48 nM. It demonstrates over 20,000-fold selectivity for NPR3 compared to NPR1. AP 811 effectively inhibits atrial natriuretic peptide (ANP)-induced stimulation of transport pumps, making it a valuable tool for research into cardiovascular and kidney function regulation. -
ANP antagonist
A 71915 is a potent and competitive antagonist of the natriuretic peptide receptor A (NPRA), exhibiting a pKi value of 9.18. It effectively displaces [125I]ANP in a dose-dependent manner, with a dissociation constant (Ki) of 0.65 nM. In cellular assays, A 71915 demonstrates a significant inhibition of rat ANP-induced cGMP production in NB-OK-1 cells, making it a valuable tool for research into cardiovascular signaling pathways and related therapeutic applications. -
Npr1 Inhibitor
JS11 is a selective inhibitor of natriuretic polypeptide receptor 1 (Npr1), exhibiting an IC50 of 1.9 μM for human Npr1. This compound has demonstrated the ability to alleviate pruritus in mouse models, making it a valuable tool for investigating the role of Npr1 in pruritic conditions. Its pharmacological activity positions JS11 as a significant reagent for research in dermatology and other fields related to itch sensation and regulation. -
NPR-C Ligand
ANP [Des18-22] 4-23 amide (rat) is a polypeptide fragment derived from rat atrial natriuretic peptide (ANP) that selectively interacts with the natriuretic peptide receptor C (NPR-C). This compound is instrumental in studying NPR-C signaling pathways and evaluating the physiological effects of natriuretic peptides in cardiovascular research and related fields. Its specificity for NPR-C makes it a valuable tool for in vitro experiments aimed at elucidating receptor-mediated responses. -
Neuropeptide
BNP(1-32), porcine is an atrial natriuretic peptide that primarily targets neuropeptide pathways. This cardiac hormone exhibits significant natriuretic, diuretic, and vasorelaxant effects, making it valuable for cardiovascular research. Furthermore, BNP(1-32) has been shown to influence passive avoidance learning in rodent models, highlighting its potential role in neurobiology studies involving dopaminergic and cholinergic systems, as well as adrenergic receptor interactions.
