Catalog No.
Product Name
Application
Product Information
Citations
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NK2 Receptor Antagonist
L-659837 is a selective antagonist of the neurokinin-2 (NK2) receptor, effectively inhibiting GR 64349-induced contraction. This compound serves as a valuable tool in the investigation of urinary bladder disorders, allowing researchers to explore its therapeutic potential in conditions like overactive bladder and related urinary dysfunctions. -
Substance P Release Inhibitor
Dilopetine citrate is a potent inhibitor of substance P release, demonstrating significant activity in attenuating the vocalizations of isolated guinea pig pups in a dose-dependent manner. Its mechanisms suggest potential applications in the field of psychiatry, particularly as an antidepressant agent. This compound may facilitate research on the modulation of neuropeptide systems involved in mood regulation and pain perception. -
SP1-7 Ligand
Phenylalanylphenylalanylamide (H-Phe-Phe-NH₂) functions as a potent ligand for the substance P 1–7 (SP1-7) binding site, exhibiting a Ki value of 1.5 nM. This compound demonstrates significant anti-allodynic and anti-hyperalgesic properties in animal models of neuropathic pain when administered centrally. However, it shows no distinct effects when delivered peripherally via intraperitoneal injection. Phenylalanylphenylalanylamide is valuable for investigations into pain-related disorders and therapeutic interventions. -
NK1R Antagonist
Telmapitant is an orally active antagonist of the neurokinin-1 receptor (NK1R). This compound exhibits antiemetic properties, making it valuable for studying delayed onset emesis. It is utilized in research to investigate the mechanisms and treatment options related to nausea and vomiting. -
Tachykinin ReceptoR Antagonist
YM-44778 is a selective antagonist of tachykinin receptors, specifically blocking NK1, NK2, and NK3 receptors with pKi values of 8.08, 8.55, and 8.24, respectively. This compound demonstrates significant inhibition of bladder pressure elevation induced by the neuropeptide substance [Sar9,Met(O2)11]-P in anesthetized rat models. Its pharmacological profile makes YM-44778 valuable for research in bladder function and disorders related to tachykinin signaling. -
Substance P Antagonist
(D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P is a potent antagonist of the neuropeptide Substance P. This compound specifically inhibits the neurokinin-1 receptor (NK1R), playing a significant role in modulating pain perception and inflammatory responses. It is commonly utilized in research focused on pain management, neurobiology, and the exploration of neuropeptide signaling pathways. -
Substance P Antagonist
[D-Pro2,D-Trp7,9] Substance P is a selective antagonist of the neuropeptide Substance P, targeting the neurokinin-1 (NK1) receptor. This compound exhibits weak agonistic properties while demonstrating potent competitive antagonism, making it useful in research applications aimed at studying pain modulation, neuroinflammatory responses, and anxiety pathways. Its unique structural modifications facilitate investigations into neurokinin signaling and potential therapeutic interventions. -
Racemate
(Rac)-LM11A-31 is a racemate that serves as a non-peptide modulator of the p75 neurotrophin receptor (p75NTR). This compound functions as an antagonist to proNGF, significant in studies related to neurodegenerative diseases and neuronal survival. Its oral efficacy provides a valuable tool for research applications aimed at understanding neurotrophic signaling pathways and developing therapeutic strategies. -
Tachykinin NK-2 Receptor Antagonist
TAC 363 is a selective antagonist of the tachykinin NK-2 receptor, demonstrating considerable potency with a pA2 value of 9.82, reflecting a rightward shift in the contractile response curve induced by Neurokinin A. While TAC 363 exhibits a weak antagonistic effect on NK-1 receptors, it effectively inhibits Neurokinin A-induced bronchoconstriction in guinea pigs, with an ED50 of 0.3 mg/kg. This compound is valuable for research into bronchial asthma and related respiratory conditions. -
NK3 Receptor Antagonist
GSK172981 is a potent antagonist of the tachykinin NK3 receptor, demonstrating pKi values of 7.7 and 7.8 for human and native guinea pig NK3 receptors, respectively. This compound exhibits brain penetrance and is primarily utilized in research focused on schizophrenia, providing valuable insights into neurokinin signaling pathways and their implications in psychiatric disorders. -
NK-2 Receptor Agonist
(β-Ala8)-Neurokinin A (4-10) is a selective agonist of the NK-2 tachykinin receptor, a key player in neuropeptide signaling. This compound demonstrates significant biological activity in modulating neurogenic inflammation and smooth muscle contraction. It is valuable for research applications focused on pain, gastrointestinal motility, and respiratory physiology. -
NK Inhibitor
Dazodeunetant is a selective inhibitor of neurokinin receptors (NK), exhibiting an IC50 of 75.99 nM against NK3R in HEK293-NK3 cells. This nitrogen-containing fused ring derivative demonstrates potential in the study of menopausal hot flashes and related therapeutic strategies. Its ability to modulate neurokinin signaling positions it as a valuable tool in neurobiology and women's health research. -
NK-1 Receptor Antagonist
(1R,2S,3R)-Aprepitant is a competitive antagonist of the human neurokinin-1 (NK-1) receptor. This compound exhibits significant potential in the study of conditions such as cancer and postoperative nausea and vomiting. Its ability to modulate NK-1 receptor activity makes it a valuable tool for research exploring therapeutic interventions in these areas. -
NK1 Receptor Antagonist
Maropitant citrate is an orally active antagonist of the neurokinin-1 (NK1) receptor. It exhibits significant antiemetic properties, effectively preventing vomiting, and demonstrates potential in mitigating ulcerative dermatitis. This compound is valuable in research focused on gastric disorders and skin conditions related to inflammation and neurogenic factors. -
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. -
NK3 Receptor Antagonist
Osanetant monohydrochloride is a selective antagonist of the NK3 receptor, known for its modulatory effects on neuropeptide signaling. It exhibits anxiolytic and antidepressant-like properties, making it a valuable tool for research into anxiety and mood disorders. This compound can facilitate studies aimed at understanding the role of NK3 receptors in various neurological conditions. -
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. -
NK3 Receptor Antagonist
SSR 146977 hydrochloride is a selective antagonist of the tachykinin NK3 receptor. This compound exhibits significant inhibitory activity, making it a valuable tool for studying the pathophysiology of psychiatric disorders and airway inflammation. Research involving SSR 146977 hydrochloride can enhance the understanding of NK3 receptor signaling pathways and their implications in various therapeutic areas. -
NK1 Receptor Antagonist
(R)-Nolpitantium is a potent and selective antagonist targeting the NK1 receptor. By competitively inhibiting tachykinin activity, (R)-Nolpitantium effectively blocks neuronal activation in the rat thalamus following nociceptive stimulation. This compound is valuable for research applications studying pain pathways and the role of tachykinin signaling in neurobiology. -
NK1 Antagonist
Vestipitant is a selective neurokinin-1 (NK1) receptor antagonist with a high binding affinity (pKi: 9.4, hNK1). This compound demonstrates significant hypnotic properties, effectively alleviating primary insomnia and other anxiety-related disorders. Its action includes the inhibition of substance P-mediated extracellular regulated kinase phosphorylation, showing potential applications in addressing conditions such as functional dyspnea, irritable bowel disease, gastroesophageal reflux disease, and tinnitus. Researchers may find vestipitant useful in studies related to anxiety, depression, and sleep disturbances. -
NK-2R Antagonist
ZM 253270 is a non-peptide antagonist targeting the neurokinin-2 receptor (NK-2R). It competitively inhibits the binding of [3H]NKA to native or cloned hamster NK-2R, demonstrating high potency with a Ki value of 2 nM. In contrast, ZM 253270 exhibits reduced efficacy on cloned human NK-2R, with a 48-fold weaker inhibitory effect. This compound is valuable for research investigating the role of NK-2R in various physiological and pathological processes. -
Neurokinin 1 Receptor Antagonist
ZD6021 is a potent antagonist of the Neurokinin 1 (NK1) receptor, exhibiting a Ki value of 0.12 nM for NK1 and 0.62 nM for NK2. This compound has demonstrated significant biological activity by reducing plasma protein extravasation in guinea pigs induced by ASMSP, with an effective dose (ED50) of 0.5 mg/kg. Additionally, ZD6021 effectively mitigates NK2-mediated bronchoconstriction, showcasing an ED50 of 13 mg/kg. Its selective antagonism supports research applications in understanding neurogenic inflammation and respiratory conditions. -
Tachykinin (NK) Receptor Antagonist
SCH 206272 is a selective antagonist of tachykinin (NK) receptors, effectively inhibiting binding at human NK(1), NK(2), and NK(3) receptors with Ki values of 1.3, 0.4, and 0.3 nM, respectively. This compound demonstrates significant biological activity in modulating neurokinin signaling pathways, making it valuable in research applications related to pain, anxiety, and other tachykinin-related disorders. Additionally, SCH 206272 is orally active, facilitating its use in in vivo studies. -
Neurokinin1 Receptor Antagonist
L-703606 is a potent and selective antagonist of the Neurokinin-1 (NK1) receptor. This compound effectively inhibits NK1 receptor activity, making it a valuable tool for investigating the role of neurokinin signaling in various physiological processes, including gastric acid secretion. Its application extends to studies focusing on pain modulation, inflammation, and other neuropsychiatric conditions, providing insights into the therapeutic potential of targeting NK1 receptors. -
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 1 Receptor Antagonist
Fosrolapitant is a selective neurokinin 1 (NK1) receptor antagonist, primarily utilized in the study of pain and anxiety pathways. By inhibiting NK1 receptor activity, it effectively alleviates symptoms related to various neurogenic processes. This compound is valuable for research applications involving the modulation of neurokinin signaling in both preclinical and clinical settings. -
Tachykinin
Physalaemin is a non-mammalian tachykinin that acts as a selective agonist for the neurokinin-1 (NK1) receptor. It demonstrates high affinity for this receptor, making it valuable in studying neurokinin signaling pathways and their physiological effects. This compound is useful in research applications related to neurobiology, pain modulation, and inflammatory responses. -
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. -
NMUR2 Antagonist
R-PSOP is a potent and selective nonpeptidic antagonist of the neuropeptide receptor NMUR2. With binding affinities (Kis) of 52 nM for human and 32 nM for rat NMUR2, R-PSOP demonstrates effective receptor inhibition. Its moderate central nervous system penetration makes it a valuable tool for investigating eating disorders, obesity, pain mechanisms, and stress-related disorders in research settings. -
NMUR2 Agonist
CPN-219 is a next-generation hexapeptidic agonist specifically targeting NMUR2. It demonstrates a selective and dose-dependent activation of NMUR2, with an EC50 value of 2.2 nM. This compound is invaluable for research applications aimed at understanding the physiological roles of NMUR2 in various biological processes. -
NMUR2 Agonist
CPN-116 is a selective agonist of the neuromedin U receptor 2 (NMUR2), which plays a critical role in the regulation of appetite and energy homeostasis. This compound has demonstrated potential biological activity in modulating metabolic processes, making it a valuable tool for research into obesity and related metabolic disorders. Its ability to activate NMUR2 may provide insights into developing therapeutic strategies for weight management and obesity treatment. -
NMU2R Agonist
3'-Methoxyflavonol is a selective agonist of the neuromedin U 2 receptor (NMU2R). It plays a significant role in various physiological processes, including modulation of appetite and anxiety behavior. This compound is useful in research applications focused on neuropeptide signaling pathways and their implications in metabolic and behavioral disorders. -
NMUR2 Agonist
Neuromedin U (rat) is a 23-amino acid neuropeptide that acts as an agonist for the NMUR2 receptor. This receptor-mediated action is crucial for the modulation of various physiological processes, including energy homeostasis, stress response, and pain perception. Neuromedin U is valuable for research investigating neuropeptide signaling pathways and their implications in metabolic disorders and stress-related conditions. -
NMUR1 Antagonist
CPN-351 is a selective antagonist of the human neuropeptide FF receptor 1 (NMUR1), exhibiting a pA2 of 7.35. Its antagonistic potency towards NMUR1 is significantly greater than its effect on NMUR2, being approximately ten times more effective. CPN-351 is a valuable tool for investigating inflammatory processes and the role of neuropeptide signaling in various biological systems. -
NMUR2 Agonist
NY0116 is an agonist of the neuromedin U receptor 2 (NMUR2), exhibiting an EC50 of 13.61 μM for hNMUR2 and 27.76 μM for hNMUR1. This compound effectively reduces cAMP levels while enhancing calcium signaling in HEK293 cells stably expressing NMUR2. NY0116 is suitable for research applications involving neuropeptide signaling pathways and their physiological implications. -
NPFF1/NPFF2 Receptor Agonist
Neuropeptide FF (NPFF) functions as an agonist for the NPFF1 and NPFF2 receptors, exhibiting Ki values of 2.82 nM and 0.21 nM, respectively. This octapeptide plays a crucial role in mediating various physiological processes, including the modulation of pain, opioids, autonomic function, and neuroendocrine responses. It is involved in the regulation of memory and the control of food and water intake, while also demonstrating significant antiopioid and analgesic properties. Neuropeptide FF is particularly relevant for research into opioid tolerance, morphine-induced analgesia, abstinence syndrome, and pain-related conditions, including inflammatory and neuropathic pain. -
NPFFR2 Activator
AC-263093 free base is an activator of the neuropeptide FF receptor 2 (NPFFR2), exerting functional activation while inhibiting NPFF receptor 1 (NPFFR1), with pKi values of 6.9 and 7.0, respectively. This compound holds potential in the investigation of mechanisms to reverse opioid tolerance, making it valuable for research related to pain management and neuropharmacology. -
NPFF1-R Antagonist
NPFF1-R antagonist 1 is a potent antagonist of the neuropeptide FF (NPFF) receptor, specifically targeting the NPFF1-R subtype. This compound, a piperidine analogue, demonstrates a selective blockade with a Ki of 211 nM for NPFF1-R and 3270 nM for NPFF2-R, indicating a remarkable 15-fold selectivity. It is suitable for research applications exploring neuropeptide signaling pathways and potential neurological disorders linked to NPFF receptor activity. -
NPFF2R/1R Agonist
AC-099 hydrochloride is a selective full agonist of the neuropeptide FF receptor 2 (NPFF2R) with an EC50 of 1189 nM, and a partial agonist of NPFF1R with an EC50 of 2370 nM. This compound has demonstrated the ability to attenuate hypersensitivity induced by spinal nerve ligation in rat models. AC-099 hydrochloride is valuable for research focusing on pain modulation and the neuropeptide signaling pathways associated with nociception. -
NPFF-Related Peptides
Neuropeptide FF (5-8) is a derivative of Neuropeptide FF that acts as a potent antagonist of NPFF-related receptors. This peptide, with the sequence Q-P-Q-R-F-NH2, exhibits a Ki value of 20.9 nM, indicating its strong binding affinity. It is primarily used in research to study pain modulation, stress responses, and neuroendocrine functions in various biological models. -
NPFFR Antagonist
DP32 is a bifunctional compound that serves as an antagonist of the neuropeptide FF receptor (NPFFR) while simultaneously acting as an agonist at the mu-opioid receptor (MOP). This unique dual activity makes DP32 a valuable tool in analgesia-related research, offering insights into pain modulation pathways and potential therapeutic applications in pain management. Researchers can utilize DP32 to explore the interplay between opioid signaling and neuropeptide regulation in various biological contexts. -
NPFFR2 modulator
NPFFR2 modulator-1 is a selective modulator of the neuropeptide FF receptor 2 (NPFFR2). This compound influences various signaling pathways associated with pain modulation and may provide insights into neuroinflammatory responses. It is valuable for researchers investigating neuropeptide interactions and their roles in pain perception and related disorders. -
NPFF2R/1R Agonist
AC-099 is a selective agonist for the neuropeptide FF receptor 2 (NPFF2R) with an EC50 of 1189 nM and a partial agonist for NPFF1R, exhibiting an EC50 of 2370 nM. This compound demonstrates significant potential in modulating pain responses, as evidenced by its ability to attenuate spinal nerve ligation-induced hypersensitivity in rat models. AC-099 serves as a valuable tool in pain research and for exploring the roles of NPFF receptors in the central nervous system. -
NPSR Antagonist
ML154 is a selective non-peptide antagonist of the neuropeptide S receptor (NPSR), demonstrating efficient brain penetration. This compound effectively inhibits NPS-induced cellular responses, including calcium influx, cAMP accumulation, and ERK phosphorylation, with IC50 values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively. ML154 is a valuable tool for investigating the role of NPSR in various physiological and pathological processes. -
NPSR Agonist
R06039-691 is an agonist of the neuropeptide S receptor (NPSR), exhibiting an EC50 of 93 nM. This compound is involved in the modulation of several biological functions, including arousal, stress and anxiety responses, memory processes, and food intake, through the activation of NPSR. Its ability to influence these physiological pathways makes R06039-691 a valuable tool for research in neurobiology and potential therapeutic applications in anxiety and related disorders.
