Catalog No.
Product Name
Application
Product Information
Citations
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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. -
NK1 receptor antagonist
GR 205171 is a selective neurokinin-1 receptor antagonist -
NK1 receptor antagonist
Casopitant mesylate is the mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. -
tachykinin NK2 receptor antagonist
Ibodutant is a tachykinin NK2 receptor antagonist for the treatment of Irritable Bowel Syndrome with diarrhoea (IBS-D) -
NK1R antagonist
Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist. -
neurokinin-1 receptor antagonist
Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist. -
NK1 receptor antagonist
Netupitant is a selective neurokinin 1 (NK1) receptor antagonist. It competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). -
NK1 receptor antagonist
Tradipitant, also known as VLY-686 and LY686017, is the 2nd generation neurokinin-1 receptor antagonist, which showed activity in preclinical anxiety models. -
NK1 receptor antagonist
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist. -
Neurokinin-1 (NK-1) receptor antagonist
Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist. -
triple tachykinin receptor antagonist
CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. -
NK3R antagonist
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes. -
neurokinin receptors antagonist
SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS). -
NK3R antagonist
Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist. -
NK2 antagonist
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide antagonist at tachykinin NK2 receptors, inhibits binding of [3H]GR100679 to hNK2-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction, with anxiolytic-like activity. -
NK-1 receptor antagonist
NK-1 Antagonist 1 (Rolapitant intermediate) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression. -
NK3 receptor antagonist
Talnetant Hcl is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.
