Catalog No.
Product Name
Application
Product Information
Citations
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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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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. -
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. -
NK1 Antagonist
Fosnetupitant chloride monohydrochloride is an NK1 receptor antagonist designed to inhibit neurokinin-1 signaling. It demonstrates high affinity for the human NK1 receptor with a pKi value of 9.5 and exhibits moderate activity at the NK3 receptor with a pKi value of 6.1. This compound serves as a methylene phosphate prodrug of Netupitant, making it a valuable tool for research in the fields of oncology and pain management, particularly for evaluating antiemetic properties and exploring neurokinin-related pathways. -
NK1 Receptors Antagonist, Substance P Antagonist
RP 67580 is a non-peptide antagonist targeting neurokinin receptor 1 (NK1) with a competitive inhibition mechanism for the binding of [3H]substance P (SP) in rat brain membranes, exhibiting a Ki value of 4.16 nM. This compound selectively inhibits NK1 receptors and serves as an essential tool in the study of pain mechanisms and neurogenic inflammation, facilitating research into potential therapeutic approaches for related conditions. -
Substance P Analogue
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) is a Substance P analogue that selectively activates the neurokinin 1 receptor (NK1R) in the rat brain, exhibiting effects similar to those of Substance P with an extended duration of action. This compound plays a significant role in modulating dopamine metabolism within the mesencephalon and midbrain cortex. Additionally, [Glp5,(Me)Phe8,Sar9] Substance P (5-11) has been shown to enhance motor activity and facilitate recovery from addictive behavior in rodent models, making it a valuable tool in neuropharmacological research. -
NK3R Agonist
[MePhe7]-Neurokinin B is a potent agonist of the neurokinin-3 receptor (NK3R) with an IC50 value of 3 nM. This compound plays a pivotal role in the modulation of pulsatile gonadotropin-releasing hormone (GnRH) secretion through NK3R activation. It is particularly valuable in research focused on reproductive physiology and neuroendocrine signaling pathways. -
Tachykinin/Substance P Receptor Inhibitor
CP-96,345 is a potent, non-peptide inhibitor targeting tachykinin and substance P receptors. This compound effectively inhibits the hypotensive effects induced by substance P and neurokinin A, making it a valuable tool for studying neurogenic inflammation. Its oral bioactivity allows for convenient application in research settings focused on pain modulation and inflammatory responses. -
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. -
Prodrug Of Netupitant
Fosnetupitant is a prodrug of Netupitant, functioning primarily as a selective antagonist of the human neurokinin-1 (NK1) receptor. With a pKi of 9.5, it offers significant inhibitory activity, making it a valuable tool in research focused on neurokinin signaling pathways. Fosnetupitant is utilized in studies related to pain management, nausea, and the effects of substance P in various biological systems. -
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. -
Tachykinin NK1 Receptor Agonist
[Sar9,Met(O2)11]-Substance P TFA is a selective agonist for the tachykinin NK1 receptor, a key player in neurokinin signaling pathways. This compound has demonstrated potent biological activity, making it useful in research applications related to pain modulation, stress response, and anxiety disorders. It serves as a valuable tool for investigating NK1 receptor functions and the development of therapeutic strategies targeting this receptor. -
NK1 Receptor Antagonist
Nolpitantium is a potent and selective competitive antagonist of the tachykinin NK1 receptor. By inhibiting NK1 receptor activation, Nolpitantium effectively blocks the excitability of rat thalamic neurons in response to nociceptive stimulation. This compound is valuable for research into pain mechanisms and the role of neurokinin signaling in various neurophysiological processes. -
NK1 Receptor Agonist
Septide, a potent NK1 receptor agonist, exhibits a Kd value of 0.55 nM, indicating strong binding affinity. It is primarily utilized in research investigating neurokinin signaling pathways and their roles in pain modulation, stress responses, and other neurobiological processes. This compound serves as a valuable tool for exploring therapeutic targets in conditions associated with NK1 receptor activity. -
NK1 receptor antagonist
L-760735 is a selective NK1 receptor antagonist that demonstrates high affinity with an IC50 of 0.19 nM for human NK1 receptors. This compound exhibits notable anxiolytic and antidepressant-like effects, making it a valuable tool for research in anxiety and mood disorders. Its oral bioavailability further enhances its utility in preclinical studies. -
NK2 Antagonist
GR 94800 is a potent and selective antagonist of the NK2 receptor, exhibiting a pKB value of 9.6, along with lower values of 6.4 and 6.0 for NK1 and NK3 receptors, respectively. This compound is valuable for investigating the role of NK2 receptors in various biological processes and can be employed in studies related to pain, inflammation, and neurogenic responses. Research applications include exploring neurokinin signaling pathways and potential therapeutic targets for related diseases. -
NK3 Receptor Antagonist
SB 218795 is a selective non-peptide antagonist of the neurokinin-3 (NK3) receptor, exhibiting a Ki of 13 nM for human NK3 (hNK3). This compound demonstrates significant selectivity, being approximately 90-fold and 7000-fold more potent against hNK3 compared to human NK2 and NK1 receptors, respectively. Research applications include studying the role of NK3 receptors in neurobiology and investigating potential therapeutic targets for managing related disorders. Additionally, SB 218795 has been shown to inhibit NK3 receptor-mediated pupillary constriction in rabbits, presenting further opportunities for exploration in translational research. -
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. -
NK-1 Receptor Antagonist
WIN 51708 is a nonpeptide antagonist of the neurokinin-1 (NK-1) receptor, predominantly exhibiting higher affinity for the rat NK-1 receptor than the human variant. This compound serves as a valuable tool in research aimed at understanding pain modulation and neurogenic inflammation. Its application can extend to studies investigating pain pathways and the potential therapeutic roles of NK-1 receptor antagonism in various neurological disorders. -
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. -
NK-R Antagonist
Substance P(1-4) is a selective antagonist of neurokinin receptors (NK-R). This compound demonstrates regulatory effects on normal hematopoiesis and effectively inhibits the formation of endogenous erythroid colonies (EEC). It is valuable for research applications related to cell signaling and hematopoietic processes. -
NK1 Receptor Antagonist
SDZ NKT 343 is a selective NK1 receptor antagonist, exhibiting an IC50 of 0.62 nM against the human NK1 receptor. This compound demonstrates significant analgesic activity, making it valuable for research focused on pain management and neuropharmacology. SDZ NKT 343 can be utilized in studies investigating the role of NK1 receptors in various physiological and pathological processes. -
NK1R Agonist
Ranakinin is a potent NK1R agonist that selectively activates neurokinin-1 receptors. It inhibits the binding of selective NK1 radioligands, leading to the activation of phospholipase C and subsequent enhancement of polyphosphoinositide hydrolysis. This compound stimulates inositol phosphate production while decreasing membrane polyphosphoinositide levels, and it also promotes the secretion of corticosterone and aldosterone. Ranakinin is valuable for research applications related to neurobiology and endocrine signaling. -
NK3 Antagonist
(Trp7,β-Ala8)-Neurokinin A (4-10) is a selective antagonist of the neurokinin-3 (NK3) receptor. This compound exhibits significant inhibitory activity on NK3-mediated signaling pathways, making it a valuable tool for studying neurokinin signaling dynamics. It is applicable in research focusing on neuropsychiatric disorders and the modulation of stress and anxiety responses. -
Tachykinin Receptor Agonist
Scyliorhinin I is a potent agonist of the tachykinin receptors NK-1 and NK-2, exhibiting Ki values of 0.9 nM and 2 nM, respectively, for rat submandibular gland NK-1 and hamster bladder NK-2 receptors. This compound is known to induce contraction of the longitudinal muscles in the guinea pig ileum, making it a valuable tool for studying gastrointestinal motility and tachykinin receptor signaling. It is relevant in research focusing on neurogenic inflammation and enteric neuron activity.
