Catalog No.
Product Name
Application
Product Information
Citations
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Neurokinin-1 Receptor Antagonist
SLV-317 free base is a potent antagonist of the neurokinin-1 receptor, demonstrating oral bioactivity. It effectively inhibits substance P-induced effects, making it valuable for research into neurogenic inflammation and pain pathways. This compound is suitable for studies focused on the modulation of neurokinin signaling and its implications in various neurological disorders. -
NK2R Agonist
[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) is a selective agonist for the NK2 receptor (NK2R), exhibiting a potent EC50 of 3.7 nM for human NK2R. This compound has demonstrated significant biological activity by inhibiting weight loss in diet-induced obese mouse models and ameliorating Loperamide-induced voiding dysfunction in wild-type mice. It serves as a valuable tool for research into neurokinin receptor-mediated disorders, including obesity, insulin resistance, and type 2 diabetes. -
Active Compound
(R)-Casopitant, an NK(1)-receptor antagonist, serves as an active compound for research applications targeting chemotherapy-induced nausea and vomiting. As the isomer of Casopitant, (R)-GW679769 offers potential insights into the modulation of neurokinin signaling pathways. This compound is instrumental in evaluating therapeutic strategies for alleviating chemotherapy-related side effects. -
Substance P Analog
Substance P, Free Acid is a native analog of substance P that offers structural similarity without the associated biological activity. This compound can be utilized in research focused on neuropeptide signaling pathways and the role of substance P in various physiological processes. Its unique properties make it suitable for studies investigating receptor interactions and neurogenic inflammation. -
NK1 Inhibitor
SR140333B is a selective inhibitor of the neurokinin-1 (NK1) receptor, primarily involved in modulating pain and inflammatory responses. This compound demonstrates significant efficacy in reducing LPS-induced fever and attenuating LPS-induced alterations in brain tissue in rat models. SR140333B is valuable for research focusing on neuroinflammation, pain pathways, and the therapeutic potential of NK1 receptor modulation. -
Neurokinin Receptor Antagonist
Benzomalvin A is a potent antagonist of neurokinin receptors, derived from Penicillium sp. This compound demonstrates significant inhibitory activity against substance P, exhibiting Ki values of 12, 42, and 43 μM at guinea pig, rat, and human neurokinin NK1 receptors, respectively. Benzomalvin A is instrumental in research focused on neurokinin signaling pathways and its implications in various physiological and pathological processes. -
SP1-7 Ligand
Leucyl-phenylalanine amide is a dipeptide analog that serves as a specific ligand for the SP1-7 receptor, exhibiting a binding affinity characterized by a Ki value of 10.2 nM. This compound is valuable for research focused on neuropeptide signaling pathways and can be utilized in studies exploring the functional roles of SP1-7 in various physiological contexts. Notably, it does not show binding activity to human NK-1 or NK-3 receptors, making it a selective tool for targeted biological investigations. -
NK1 Receptor Antagonist
Maropitant citrate hydrate is an orally active antagonist of the neurokinin-1 (NK1) receptor. It exhibits significant antiemetic properties, making it effective in preventing vomiting. Additionally, Maropitant has been reported to inhibit ulcerative dermatitis, highlighting its utility in various research applications related to gastrointestinal and inflammatory conditions. -
Analog of Substance P
[MePhe8,Sar9] Substance P is an analog of the neuropeptide Substance P, functioning as a neurotransmitter and neuromodulator in the central nervous system (CNS). This compound exhibits biological activity relevant to pain modulation and neuroinflammation. It is utilized in research applications focused on the roles of neuropeptides in various physiological and pathological processes, including nociception and stress responses. -
NK1/NK2 Receptor Antagonist
S 16474 is a cyclic peptide that functions as an antagonist of NK1 and NK2 receptors. This compound demonstrates significant activity in modulating neurogenic inflammation. S 16474 is suitable for research applications focusing on pain pathways and inflammatory responses mediated by neurokinins. -
Substance P Fragment
Substance P (2-11) is a peptide fragment of Substance P that primarily targets neurokinin receptors. It exhibits contractile activity in guinea pig ileum, indicating its potential role in gastrointestinal motility. Additionally, Substance P (2-11) has been shown to inhibit the permeation of tritiated Substance P across blood-brain barrier endothelial cell monolayers, making it relevant for research in neurobiology and drug delivery. -
NK3 Receptor Antagonist
GSK256471 is a non-peptide antagonist targeting the tachykinin NK3 receptor, exhibiting a pKi of 8.9 for the human recombinant receptor and 8.4 for the guinea pig native receptor. This compound demonstrates over 100-fold selectivity against NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 irreversibly inhibits neurokinin B (NKB)-induced inositol phosphate accumulation, and has been shown to mitigate wet dog shaking behavior and suppress dopamine release. This compound serves as a valuable tool for studying the pathophysiology of schizophrenia. -
Analog of Substance P
Substance P-Gly-Lys-Arg is an analog of Substance P designed to interact with neurokinin receptors. This peptide exhibits key biological activity in modulating pain perception and inflammatory responses, making it a valuable tool for studying neuropeptide signaling pathways. Research applications include investigating the role of Substance P in pain management and exploring therapeutic avenues for neuroinflammatory conditions. -
NK1 Receptor Antagonist
(D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P is a selective antagonist of the neurokinin-1 (NK1) receptor. It exhibits significant biological activity by inhibiting NK1 receptor-mediated signaling pathways, which play a crucial role in pain perception, inflammation, and neurogenic responses. This compound is valuable for research in neurobiology, cancer therapy, and the development of analgesics targeting the NK1 receptor. -
NK-3 Antagonist
PD-161182 is a non-peptide antagonist targeting the neurokinin-3 (NK-3) receptor. It exhibits potential activity in modulating NK-3 receptor-related pathways, making it a valuable tool for studying various central nervous system disturbances, as well as pain, inflammation, and diseases affecting the pulmonary and skin systems. This compound is essential for researchers exploring the therapeutic implications of NK-3 antagonism in these contexts. -
NK1 Receptor Antagonist
ASN-1377642 is an NK1 receptor antagonist with a Ki value of 251 nM. This compound demonstrates antitumor activity, particularly in breast cancer cells that exhibit high expression of the NK1 receptor. ASN-1377642 may facilitate research into targeted cancer therapies and the role of neurokinin signaling in tumor progression. -
Neurokinin Receptor Antagonist
L-659877 is a neurokinin receptor antagonist that serves as a valuable tool for investigating peptide fragmentation and structural properties. This compound facilitates the study of collision-induced dissociation mechanisms, allowing researchers to analyze the structural changes of beta-fragment ions across varying lengths. Its application is essential for advancing understanding in neuropharmacology and peptide-based therapeutics. -
Neurokinin Receptor Inhibitor
SCH 60057 is a potent neurokinin receptor inhibitor, selectively targeting NK1 and NK2 receptors with IC50 values of 6 μM and 12 μM, respectively. This compound is derived from Acremonium sp. and is useful in research applications related to pain modulation, inflammation, and neurogenic disorders. Its ability to inhibit neurokinin signaling pathways makes it a valuable tool for investigating the roles of these receptors in various biological processes. -
Substance P Antagonist
FR 113680 is a tripeptide antagonist that selectively targets the NK1 neurokinin receptor, inhibiting the action of substance P. This compound displays significant biological activity in modulating pain and inflammatory responses. It is widely utilized in research exploring the role of neurokinin pathways in various neurological and psychiatric disorders. -
Neurokinin B Antagonist
(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B is a competitive antagonist of Neurokinin B, primarily targeting the Neurokinin Receptor, with a pA2 value of 5.5. This compound selectively inhibits Neurokinin B activity without affecting Substance P or Neurokinin A, making it valuable for studies of neuromodulation and neuropeptide signaling. Its ability to modulate neurokinin pathways is relevant for research in neurobiology and potential therapeutic applications related to pain and inflammatory responses. -
Substance P Fragment
Substance P (3-11) is a truncated form of the neuropeptide Substance P that effectively crosses the blood-brain barrier. This fragment exhibits potent contracting activity on guinea pig ileum and stimulates chemotaxis in human monocytes. It is utilized in research focused on neuroinflammation, pain pathways, and immune response modulation. -
NK-1 Agonist
[Pro9]-Substance P is a highly selective and reversible agonist of the NK-1 tachykinin receptors, demonstrating an EC50 of 0.93 nM. This compound plays a significant role in modulating neurokinin signaling pathways and is instrumental in research focused on pain management, neuroinflammation, and various neurological disorders. Its precise activity profile makes it an invaluable tool for studying the therapeutic potential of NK-1 receptor modulation. -
Substance P (6-11) Analogue
[Glp6] Substance P (6-11) is a potent analogue of substance P (6-11) that primarily targets tachykinin receptors. This compound is known to stimulate the formation of [3H]-inositol monophosphate ([3H]-IP1) in rat urinary bladder tissues. It serves as a valuable tool in research focused on neuropeptide signaling, pain pathways, and bladder function. -
NK1 Receptor Antagonist
Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist that effectively inhibits the action of substance P at the NK1 receptor. This compound demonstrates key biological activity in modulating neurogenic inflammation and pain pathways. It is predominantly used in research applications involving pain management, gastrointestinal disorders, and anxiety models, making it a valuable tool for studying the neurokinin system and its therapeutic potential. -
NTSR1 Anagonist
Zalsenertant tetraxetan is a DOTA-conjugated antagonist of the neurohypophyseal hormone receptor subtype 1 (NTSR1). Labeled with the radioactive isotope Lu-177 (177Lu), it serves as a valuable tool for molecular imaging to identify potential responders. This compound is particularly relevant in radiotherapy research for solid tumors, facilitating the exploration of targeted therapeutic strategies. -
Neurokinin Receptor
Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor, demonstrating a 46% inhibition of substance P binding at a concentration of 100 μg/mL in vitro. Additionally, it exhibits weak inhibitory activity against indoleamine 2,3-dioxygenase (IDO), with an IC50 value of 130 μM for recombinant IDO. Isolated from Penicillium, Benzomalvin C features a distinct epoxide group at C-19 and C-20, which differentiates it from other benzomalvins such as A, B, and E. This compound may prove valuable in neurobiology and cancer research applications due to its modulation of neurokinin signaling and IDO activity. -
NK1 Receptor Antagoinst
CGP-49823 is a selective antagonist of the neurokinin 1 receptor (NK1 receptor) with oral bioavailability. It exhibits potent anti-anxiety effects, demonstrated in social interaction assays in rats, and shows a slow development of tolerance without eliciting anxiety-like withdrawal symptoms upon cessation. This compound is applicable in research focused on anxiety and depression. -
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.
