Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
Neurokinin Receptor Agonist
GR-73632 is a novel neurokinin 1 (NK-1) receptor agonist that directly targets the peripheral terminals of primary sensory neurons. By activating the NK-1 receptor, GR-73632 effectively conveys itch signals, making it a valuable tool in studying mechanisms of pruritus and related sensory pathways. This compound is relevant for research applications focusing on itch-related disorders and sensory neuron functionality. -
Neurokinin Receptor Antagonist
Vapreotide is a neurokinin-1 (NK1) receptor antagonist, demonstrating an IC50 of 330 nM. It effectively inhibits the binding of substance P to the NK1 receptor, making it a valuable tool in research concerning pain modulation, anxiety, and the regulation of neurogenic inflammation. Vapreotide's applications extend to studies of gastrointestinal disorders and therapeutic strategies for conditions associated with elevated neurokinin levels. -
Neurokinin Receptor Modulator
Biotin-Substance P is a biotinylated form of the neuropeptide Substance P, which primarily targets the neurokinin 1 receptor (NK1R). This compound acts as both a neurotransmitter and neuromodulator within the central nervous system (CNS), playing a crucial role in pain perception, stress response, and neuroinflammation. Biotin-Substance P is particularly useful in research applications focused on neurokinin receptor signaling pathways and neuropeptide interactions in various physiological and pathological conditions. -
Neurokinin Receptor Activator
Eledoisin Related Peptide is a neurokinin receptor activator that functions as an analog of Substance P. This peptide is known to stimulate neurons, resulting in various behavioral responses. It serves as a valuable tool for research applications focused on neurokinin signaling pathways and tachykinin receptor interactions. -
Neurokinin Receptor Antagonist
Vapreotide acetate is a neurokinin-1 (NK1) receptor antagonist, exhibiting an IC50 of 330 nM. This compound has demonstrated significant biological activity, making it valuable in the research of neurokinin signaling pathways and their roles in various physiological and pathological processes. Vapreotide acetate is commonly utilized in studies involving pain management, cancer therapy, and gastrointestinal disorders. -
Neurokinin Receptor Agonist
Neurokinin B is a neurokinin receptor agonist that belongs to the tachykinin family of peptides. It selectively interacts with G protein-coupled receptors, including neurokinin receptor 1 (NK1R), NK2R, and NK3R, to elicit various physiological responses. This compound has been studied for its roles in pain modulation, neurogenic inflammation, and the regulation of reproductive functions, making it a valuable tool for research in neurobiology and pharmacology. -
Neurokinin Receptor Agonist
Hemokinin 1, human is a selective full agonist of the neurokinin 1 (NK1) receptor, demonstrating significant activity at both NK2 and NK3 receptors as well. This reagent is known for its capacity to induce opioid-independent analgesia, making it a valuable tool in pain research. Hemokinin 1, human can be utilized in studies exploring neurokinin signaling pathways and their implications in various physiological and pathological processes. -
Neurokinin Receptor
Substance P (1-9) is a neurokinin receptor peptide that plays a crucial role in modulating pain perception and inflammatory responses. This nonapeptide is known to inhibit the inactivation of substance P, enhancing its biological activity in both the guinea-pig ileum and urinary bladder. Substance P (1-9) is utilized in research applications aimed at understanding neurogenic inflammation and pain mechanisms. -
Neurokinin Receptor
Substance P(1-7) is a fragment of the neuropeptide substance P that primarily targets neurokinin receptors. This compound exhibits depressor and bradycardic effects when administered to the nucleus tractus solitarius, making it useful for studies on cardiovascular regulation and neuropeptide signaling pathways. Its applications extend to research involving neurokinin receptor modulation and their role in physiological responses. -
Neurokinin Receptor Antagonist
Substance P Receptor Antagonist 1 is a neurokinin receptor antagonist that effectively inhibits the activity of the substance P neuropeptide. This compound demonstrates significant biological activity in modulating pain perception and may be useful in research related to central nervous system disorders, respiratory conditions, inflammatory diseases, and gastrointestinal disorders. Its engagement with neurokinin receptors positions it as a valuable tool for studying therapeutic interventions in these areas. -
Neurokinin Receptor Antagonist
SB 235375 is a selective antagonist of the human neurokinin-3 (hNK-3) receptor, developed through structural optimization of 2-phenyl-4-quinolinecarboxylic acid amide. It exhibits high affinity specifically for the hNK-3 receptor, showing significantly lower binding to hNK-1 and hNK-2 receptors. In vitro, SB 235375 effectively inhibits NK-3 receptor-mediated contraction and calcium mobilization. Additionally, in vivo studies reveal its capability to attenuate NK-3 receptor-driven responses through both oral and intravenous administration in animal models. This makes SB 235375 a valuable tool for research in neurokinin signaling and related physiological processes. -
Neurokinin Receptor Antagonist
Orvepitant is a potent and selective neurokinin-1 (NK-1) receptor antagonist with a reported pKi of 10.2 for the human NK-1 receptor. This orally active compound is capable of crossing the blood-brain barrier, making it suitable for central nervous system applications. Orvepitant demonstrates potential therapeutic effects in the treatment of depressive disorders and chronic refractory cough (CRC), supporting its role in various neurological and respiratory research applications. -
Opioid Receptor Agonist
AWL 60 is an opioid receptor agonist that also exhibits properties as a substance P (SP) antagonist. This compound has been shown to antagonize SP agonists in vitro, as well as attenuate hypotension induced by SP agonists in vivo. AWL 60 is relevant for research applications focused on pain modulation, opioid receptor signaling, and neuroinflammatory responses. -
Neurokinin Receptor Inhibitor
NK3R-IN-1 is a potent inhibitor of the Neurokinin Receptor NK3R, characterized as an imidazolepiperazine derivative with oral bioavailability. This compound effectively lowers blood luteinizing hormone levels in ovariectomized models, demonstrating significant influence on neuroendocrine regulation. It serves as a valuable tool for research in reproductive biology and neurobiology, particularly in studies involving hormone modulation and neurological signaling pathways. -
Neurokinin Receptor Agonist
[Nle11]-Substance P is an agonist of neurokinin receptors, designed to circumvent the oxidation issues associated with methionine in natural Substance P. This analog exhibits enhanced stability and retains biological activity, making it suitable for research studies focused on pain modulation, neurogenic inflammation, and neuropsychiatric disorders. Its application in various in vitro and in vivo models supports investigations into neurokinin signaling pathways and their implications in therapeutic interventions. -
Neurokinin Receptor Agonist
Scyliorhinin II is a selective neurokinin-3 receptor agonist, exhibiting a Ki value of 2.5 nM for the neurokinin-3 receptor in rat cerebral cortex. This compound plays a significant role in modulating neurogenic inflammatory processes and has potential applications in the study of neurokinin signaling pathways. It is valuable for researching the physiological and pharmacological roles of neurokinin receptors in various biological systems. -
Neurokinin Receptor Antagonist
MEN 10208 is a neurokinin A antagonist that effectively targets neurokinin receptors, inhibiting their activity. This compound is primarily utilized in research focused on neurobiology and the regulation of pain, anxiety, and other neurological disorders. MEN 10208 can serve as a valuable tool for exploring the physiological roles of neurokinin signaling in various biological contexts. -
Neurokinin Receptor Agonist
C14TKL-1 is a tachykinin-like peptide that acts as an agonist for neurokinin receptor 1 (NK-1). This compound is utilized in research to study the physiological roles of NK-1 in neurogenic inflammation and pain pathways. Its activity may provide insights into the underlying mechanisms of various neurological disorders and potential therapeutic targets. -
Neurokinin Receptor
Dapitant is a non-peptide antagonist targeting the neurokinin-1 (NK1) receptor, demonstrating high affinity for the human receptor. By inhibiting the binding of Substance P to NK1 receptors, Dapitant effectively blocks neurokinin-mediated biological effects. This compound serves as a potential therapeutic candidate for various conditions associated with Substance P, including neurogenic inflammation and pain modulation, making it valuable for research in pain management and inflammatory disorders. -
Neurokinin Receptor Antagonist
Benzomalvin A is a potent antagonist of neurokinin receptors, derived from Penicillium sp. This compound demonstrates significant inhibitory activity against substance P, exhibiting Ki values of 12, 42, and 43 μM at guinea pig, rat, and human neurokinin NK1 receptors, respectively. Benzomalvin A is instrumental in research focused on neurokinin signaling pathways and its implications in various physiological and pathological processes. -
Neurokinin Receptor Antagonist
L-659877 is a neurokinin receptor antagonist that serves as a valuable tool for investigating peptide fragmentation and structural properties. This compound facilitates the study of collision-induced dissociation mechanisms, allowing researchers to analyze the structural changes of beta-fragment ions across varying lengths. Its application is essential for advancing understanding in neuropharmacology and peptide-based therapeutics. -
Neurokinin Receptor Inhibitor
SCH 60057 is a potent neurokinin receptor inhibitor, selectively targeting NK1 and NK2 receptors with IC50 values of 6 μM and 12 μM, respectively. This compound is derived from Acremonium sp. and is useful in research applications related to pain modulation, inflammation, and neurogenic disorders. Its ability to inhibit neurokinin signaling pathways makes it a valuable tool for investigating the roles of these receptors in various biological processes. -
Neurokinin Receptor
Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor, demonstrating a 46% inhibition of substance P binding at a concentration of 100 μg/mL in vitro. Additionally, it exhibits weak inhibitory activity against indoleamine 2,3-dioxygenase (IDO), with an IC50 value of 130 μM for recombinant IDO. Isolated from Penicillium, Benzomalvin C features a distinct epoxide group at C-19 and C-20, which differentiates it from other benzomalvins such as A, B, and E. This compound may prove valuable in neurobiology and cancer research applications due to its modulation of neurokinin signaling and IDO activity. -
Neurokinin Receptor Antagonist
YM-49598 iodide is a tachykinin NK-1 receptor antagonist that effectively inhibits neurokinin signaling. This compound has demonstrated the ability to reduce drug-induced bladder contractions in rat models, exhibiting an IC50 value of 11 μg/kg. Its application extends to research focused on pain modulation, inflammation, and bladder dysfunction, making it a valuable tool in pharmacological studies related to neurokinin pathways. -
Neurokinin Receptor Antagonist
WS9326A is a neurokinin receptor antagonist derived from Streptomyces violaceus. This compound demonstrates significant activity in inhibiting tachykinin signaling pathways, making it a valuable tool for investigating neurokinin receptor-related processes. Its application spans various fields, including neuropharmacology and studies of pain modulation, providing insights into the physiological roles of neurokinins. -
Neurokinin Receptor Antagonist
Vapreotide diacetate is a neurokinin-1 (NK1) receptor antagonist with an IC50 of 330 nM. It exerts its biological activity by inhibiting NK1 receptor signaling, which plays a critical role in pain modulation, anxiety, and other neuropsychiatric conditions. This compound is employed in research applications targeting neurokinin signaling pathways, contributing to the exploration of therapeutic interventions for related disorders. -
Neurokinin Receptor Agonist
Monohydroxy Netupitant is the active metabolite of Netupitant, functioning as a neurokinin receptor agonist. It exhibits significant biological activity in modulating neurokinin signaling pathways and is primarily utilized in researching mechanisms of nausea and vomiting associated with chemotherapy and other treatments. Its role in neurokinin Receptor modulation makes it a valuable tool for investigating related physiological and pharmacological processes. -
Neurokinin Receptor Agonist
Neurokinin A (4-10) is a selective agonist of the neurokinin receptor NK2. This peptide exhibits significant biological activity by mediating various physiological responses, including smooth muscle contraction and modulation of pain perception. It is instrumental in research applications related to neuropeptide signaling, gastrointestinal functions, and respiratory physiology. -
Neurokinin Receptor Antagonist
MEN11467 is a selective neurokinin (NK1) receptor antagonist that exhibits peptidomimetic properties. It functions by blocking NK1 receptor activation, thereby modulating neurokinin signaling pathways. MEN11467 has potential applications in the treatment of conditions such as anxiety, depression, and pain, making it a valuable tool for researchers studying neurokinin-related disorders. -
Neurokinin Receptor Antagonist
Tachykinin Antagonist 1 is a potent antagonist of neurokinin receptors, specifically designed to inhibit the actions of tachykinins such as substance P. This compound has demonstrated the ability to modulate pain signaling and inflammation processes, making it valuable for research in neurobiology and pharmacology. Applications may include studies on pain management, neuroinflammation, and the broader implications of neurokinin signaling in various physiological and pathological conditions. -
Neurokinin Receptor Antagonist
Neurokinin Antagonist 1 is a selective antagonist of the neurokinin receptor, primarily targeting the neurokinin-1 (NK1) receptor. This compound exhibits potent inhibitory effects on neurokinin-mediated signaling pathways, making it a valuable tool for investigating the roles of substance P and neurokinin receptors in various physiological and pathological processes. Research applications include studies on pain modulation, anxiety, depression, and potential therapeutic interventions in neuroinflammatory conditions. -
NPY Y1 Receptor Antagonist
BIBO3304 is a selective antagonist of the neuropeptide Y (NPY) Y1 receptor, exhibiting subnanomolar affinity with IC50 values of 0.38 nM for the human receptor and 0.72 nM for the rat receptor. This compound serves as a valuable tool for investigating the role of NPY signaling in various biological processes, including appetite regulation and anxiety-related behaviors. Its oral bioavailability makes it suitable for in vivo studies in pharmacological research and neurobiology. -
NPY Y1/NPFF Receptor Antagonist
BIBP3226 TFA is a potent and selective antagonist of the neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptors. It exhibits inhibition constants (Kis) of 1.1 nM, 79 nM, and 108 nM for the rat NPY Y1, human NPFF2, and rat NPFF receptors, respectively. BIBP3226 TFA is utilized in research focused on anxiety and neuropeptide signaling pathways, providing valuable insights into the role of these receptors in various biological processes. -
NPY Y1 Receptor Agonist
[Leu31,Pro34]-Neuropeptide Y (porcine) is a selective agonist of the neuropeptide Y Y1 receptor. This analog exhibits significant anxiolytic effects, making it a valuable tool for studying anxiety-related disorders. It is predominantly utilized in neuropharmacological research to explore the role of NPY in stress and anxiety modulation. -
NPY Receptor Y2 Agonist
Neuropeptide Y (3-36) (human, rat) is an agonist of the Neuropeptide Y receptor Y2 (NPY Y2). This neuropeptide Y metabolite, generated by the action of dipeptidyl peptidase-4 (DPP4), has been shown to reduce the release of norepinephrine through its interaction with the Y2 receptor. It is primarily utilized in research related to neurophysiology and metabolic disorders, providing insights into pathways associated with appetite regulation and anxiety. -
NPY Y5 Receptor Antagonist
NTNCB hydrochloride is a selective antagonist of the neuropeptide Y Y5 receptor, exhibiting a Ki of 8 nM for human Y5. This compound is valuable for investigating the role of NPY signaling in various physiological processes and disorders. Its ability to specifically inhibit Y5 receptor activity makes it a useful tool in both pharmacological studies and drug discovery related to metabolic and neuropsychiatric diseases. -
NPYY2 Receptor Antagonist
CYM 9484 is a selective neuropeptide Y (NPY) Y2 receptor antagonist, demonstrating high potency with an IC50 value of 19 nM. This compound effectively inhibits Y2 receptor activity, making it a valuable tool for studying neuropeptide signaling pathways and the role of NPY in various physiological processes. CYM 9484 is relevant for research in neurobiology and metabolic disorders where modulation of the Y2 receptor may provide therapeutic insights.
