Catalog No.
Product Name
Application
Product Information
Citations
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NK1/NK2 Receptor Antagonist
DNK-333 is a potent dual antagonist of the NK1 and NK2 receptors, exhibiting IC50 values of 4.8 nM and 5.5 nM, respectively. This compound effectively inhibits Neurokinin A (NKA)-induced bronchoconstriction, making it a valuable tool for research on respiratory conditions such as asthma. Its balanced activity at both receptor sites allows for exploring therapeutic strategies targeting neurokinin signaling pathways. -
NK1 Receptor Antagonist
Vestipitant mesylate is a selective NK1 receptor antagonist that effectively crosses the blood-brain barrier. With a high affinity for the human NK1 receptor (pKi: 9.65), this compound is instrumental in studying various neuropsychiatric conditions, including depression and anxiety disorders, as well as in investigating its effects on nausea and vomiting. Its oral bioavailability further facilitates its use in in vivo research applications. -
NK2 Receptor Antagonist
GR 87389 is a potent antagonist of the NK2 receptor, effectively inhibiting its activity. This compound has been shown to competitively block GA 64349-induced contractions in smooth muscle strips derived from human detrusor, prostate, and prostatic urethra tissues. GR 87389 is valuable in research applications focused on the role of NK2 receptors in smooth muscle physiology and potential therapeutic strategies for related disorders. -
NK-1 Receptor Antagonist
R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist, demonstrating a Ki value of 0.45 nM against the human NK-1 receptor. This compound effectively inhibits Substance P-induced peripheral responses, such as skin reactions and plasma extravasation in guinea pig models, as well as central effects demonstrated in gerbils. Additionally, R116031, when labeled with 3H, shows significant accumulation in brain regions including the striatum, olfactory tubercle, olfactory bulb, and locus coeruleus, making it suitable for use as a PET ligand in imaging studies. -
NK2 Receptor Antagonist
Bz-Dab(NBD)-AwFpP-Nle-NH2 is a specific antagonist of the NK2 receptor, exhibiting potent activity with a pKi of 8.87 nM. This fluorescent compound, with excitation at 340 nm and emission at 505 nm, is valuable for studies investigating NK2 receptor-related signaling pathways and their roles in various biological processes. Its applications include receptor characterization and evaluation of receptor function in physiological and pathological contexts. -
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.
