Catalog No.
Product Name
Application
Product Information
Citations
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neurokinin-1 receptor antagonist
Aprepitant is classified as an NK1 antagonist. Aprepitant has been shown to inhibit both the acute and delayed emesis induced by cytotoxic chemotherapeutic drugs by blocking substance P landing on receptors in the brains neurons. It has also been shown to increase the activity of the 5-HT3 receptor antagonists ondansetron and the corticosteroid dexamethasone, which are also used to prevent nausea and vomiting caused by chemotherapy.
- Maya Tokumoto, .et al. , Connect Tissue Res, 2022, Jul 20;1-11 PMID: 35856812
- Kodji X, .et al. , FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499
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neurokinin-1 receptor antagonist
Fosaprepitant is a selective neurokinin-1 (NK-1) receptor 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
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. -
NK1 receptor antagonist
Rolapitant, also known as SCH-619734, is a selective, bioavailable, CNS penetrant neurokinin NK1 receptor antagonist that shows behavioral effects in animals models of emesis.- Bubak AN, .et al. , J Infect Dis, 2018, Sep 8;218(8):1324-1335 PMID: 29788447
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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). -
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. -
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. -
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. -
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. -
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. -
NK2R Agonist
EB1002 is a highly selective, long-acting agonist of the NK2 receptor (NK2R). This compound plays a crucial role in central appetite suppression, stimulates peripheral energy expenditure, and enhances insulin sensitivity, leading to effective reductions in body weight and improvements in glucose and lipid metabolism. EB1002 is a valuable tool for research focused on obesity and type 2 diabetes. -
Glutamate Derivative
H-Glu(OtBu)-OtBu hydrochloride is a glutamate derivative that serves as a critical intermediate in the synthesis of prostate-specific membrane antigen (PSMA) targeting probes. This compound enhances tumor/background contrast by utilizing negatively charged linkers to minimize nonspecific background binding. Its applications are primarily in prostate cancer PET and SPECT imaging studies, facilitating improved diagnostic imaging. -
NK-1/NK-3 Receptor Antagonist
Elinzanetant is an orally bioavailable and selective antagonist of the neurokinin-1 (NK-1) and neurokinin-3 (NK-3) receptors. It exhibits significant efficacy in alleviating menopause-associated vasomotor symptoms such as hot flashes and night sweats while also influencing levels of estradiol and progesterone. This compound is valuable for researching treatments for moderate to severe vasomotor and sleep disorders related to menopause. -
p75 Neurotrophin Receptor Ligand
LM11A-31 is a non-peptide ligand targeting the p75 neurotrophin receptor (p75NTR) and functions as a potent antagonist of proNGF (nerve growth factor). This orally active amino acid derivative demonstrates high permeability across the blood-brain barrier and effectively inhibits p75-mediated neurodegeneration. Research indicates that LM11A-31 can reverse cholinergic neurite dystrophy in mouse models of Alzheimer's disease, particularly during mid- to late-stage disease progression, making it valuable for studying neurodegenerative conditions and developing therapeutic strategies. -
NK1 Receptor Antagonist
L-733060 hydrochloride is a selective neurokinin-1 (NK-1) receptor antagonist that primarily targets pain transmission and neural plasticity. By inhibiting the binding of Substance P to the NK-1 receptor, L-733060 hydrochloride effectively blocks the enhancement of long-term potentiation (LTP) in the hippocampus. This compound has demonstrated the ability to reverse orofacial hyperalgesia induced by experimental occlusal interference in rat models. Additionally, L-733060 hydrochloride inhibits neurogenic plasma extravasation without adverse effects on cardiovascular function and may possess anti-tumor properties. It is suitable for exploring mechanisms of chronic orofacial pain. -
NK-1 Receptor Antagonist
L-732138 is a selective and potent antagonist of the neurokinin-1 (NK-1) receptor, exhibiting an IC50 of 2.3 nM. This compound demonstrates a 200-fold greater potency in cloned human NK-1 receptors compared to cloned rat NK-1 receptors, and is more than 1000-fold more selective than human NK-2 and NK-3 receptors. L-732138 is useful in research focused on pain modulation, particularly in the reduction of hyperalgesia, and has shown potential antitumor activity. -
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. -
Neurotransmitter
Substance P TFA, a CNS-penetrant neuropeptide, primarily targets the neurokinin 1 receptor (NK1R). This compound functions as both a neurotransmitter and neuromodulator within the central nervous system, playing a crucial role in mediating pain perception, anxiety, and stress responses. Its application in research includes studying neuronal signaling pathways and exploring therapeutic approaches for pain management and psychiatric disorders. -
Neurokinin-1 Receptor Antagonist
Orvepitant maleate is a potent and selective antagonist of the neurokinin-1 (NK-1) receptor, exhibiting a pKi of 10.2 for the human receptor. This orally active compound effectively crosses the blood-brain barrier, making it a valuable tool in neurological research. Orvepitant maleate shows promise for therapeutic applications in depressive disorders and chronic refractory cough (CRC), providing insights into the modulation of neurokinin pathways. -
NK3 Receptor Antagonist
Osanetant is a selective antagonist of the neurokinin-3 (NK3) receptor. This compound exhibits anxiolytic and antidepressant-like effects, making it a valuable tool for research in the fields of anxiety, depression, and schizophrenia. Its mechanism of action involves modulation of neurokinin signaling pathways, providing insights into potential therapeutic applications for mood disorders. -
NK-1R Antagonist
Spantide II is a potent neurokinin-1 receptor (NK-1R) antagonist, functioning as an undecapeptide analog of substance P. By binding to NK-1R, Spantide II effectively inhibits the proinflammatory activities associated with substance P. This reagent is valuable for research into inflammatory skin disorders, including psoriasis and contact dermatitis, contributing to the understanding of neurogenic inflammation. -
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. -
Active Compound
Substance P (7-11) is a C-terminal fragment of the neuropeptide Substance P, primarily known for its role in modulating pain perception and inflammatory responses. This compound increases intracellular calcium concentrations, leading to diverse biological activities. It is widely utilized in research related to neurobiology, pain signaling pathways, and inflammation response mechanisms. -
Tachykinin NK1 Receptor Agonist
[Sar9,Met(O2)11]-Substance P is a selective agonist for the tachykinin NK1 receptor. It exhibits significant biological activity, promoting receptor activation which is implicated in pain modulation, stress response, and neurogenic inflammation. This compound is valuable for research applications in neurobiology, pain syndromes, and the study of substance P-related pathways. -
NK1 Receptor Antagonist
Spantide I is a selective antagonist of the neurokinin-1 (NK1) receptor, demonstrating Ki values of 230 nM for NK1 and 8150 nM for NK2 receptors. This compound effectively modulates cytokine profiles by reducing type 1 and enhancing type 2 cytokine IL-10 in the infected cornea, thereby significantly decreasing corneal perforation. Spantide I serves as a valuable tool in research focused on inflammatory responses and therapeutic interventions in corneal diseases. -
Neurokinin 1 Receptor Agonist
Hemokinin 1 (mouse) is a selective agonist of the neurokinin-1 receptor (NK1R), exhibiting a Ki value of 0.175 nM for mouse NK1R. This compound demonstrates a much lower affinity for the human NK2 receptor, with a Ki of 560 nM. Hemokinin 1 is primarily utilized in research applications aimed at studying pain modulation, inflammatory processes, and neurogenic signaling pathways involving the NK1 receptor. -
NK2R Agonist
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) is a selective agonist of the NK2 receptor (NK2R) that demonstrates potent biological activity. This peptide analog of Neurokinin A exhibits prokinetic effects, making it valuable for research into gastrointestinal motility and related pathways. Its application can elucidate the role of NK2R in smooth muscle contraction across various tissues, providing insights into receptor functionality and potential therapeutic targets. -
NK1 Receptor Antagonist
Rolapitant hydrochloride hydrate is a potent and selective neurokinin 1 (NK1) receptor antagonist, exhibiting a Ki value of 0.66 nM. This compound is known for its long-acting and orally bioactive properties, making it suitable for therapeutic applications. Notably, Rolapitant hydrochloride hydrate demonstrates significant anti-emetic activity, as evidenced in ferret emesis models, supporting its potential use in managing nausea and vomiting. Additionally, it does not interact with CYP3A4, allowing for broader applicability in combination therapies. -
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. -
NK-2 Antagonist
MEN 10207 is a selective antagonist of the NK-2 tachykinin receptor, demonstrating significant activity with pA2 values of 5.2, 7.9, and 4.9 across in vitro assays for NK-1, NK-2, and NK-3 receptors, respectively. This compound is primarily utilized in research to elucidate the physiological roles of tachykinins and their associated receptors. MEN 10207 can be instrumental in studies focused on neurogenic inflammation, pain modulation, and various neuropsychiatric disorders.
