Catalog No.
Product Name
Application
Product Information
Citations
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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. -
NK-1/NK-2 Antagonist
MDL 105212A is a potent, orally active nonpeptide antagonist targeting neurokinin receptors NK-1 and NK-2. This compound exhibits significant potential in studies related to inflammation, immunology, and neurological disorders, including asthma. Its efficacy in modulating tachykinin signaling pathways makes it a valuable tool for researchers investigating these conditions. -
Tachykinin Antagonist
[D-Trp2,7,9] Substance P is a tachykinin antagonist primarily targeting neurokinin receptors. It exhibits Ki values of 1 μM, 1.3 μM, and approximately 9 μM for NK-1, NK-2, and NK-3 receptors, respectively. This compound is utilized in research applications focused on modulating pain, inflammation, and neurogenic responses. Its ability to selectively block neurokinin receptor activity makes it a valuable tool for exploring tachykinin-related biological processes. -
NK1R Agonist
[S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10) is a selective agonist for the neurokinin-1 receptor (NK1R). This peptide fragment serves as a valuable tool in studying the biological activities associated with neuropeptide signaling, particularly in mouse and human models. It is instrumental in investigating neurogenic inflammation, pain modulation, and a variety of physiological responses linked to NK1R activation. This compound can facilitate research in neurobiology and the therapeutic exploration of receptor-targeted treatments. -
Antibronchitis Agent
Eprazinone is an antibrinchitis agent that enhances lung function and arterial oxygen levels. It is particularly useful in investigating chronic bronchitis, showing a dose-dependent ability to alter bronchoalveolar lavage fluid composition by increasing phospholipid levels while decreasing neutral lipid content. Additionally, eprazinone reduces short-circuit current primarily through the modulation of chloride secretion and influences both sodium and chloride transport at elevated doses. Its anti-inflammatory properties may be linked to its regulation of airway ion transport and lipid composition in the bronchoalveolar lavage fluid. -
NK2 Tachykinin Receptor Antagonist
MDL 29913 is a cyclic pseudopeptide that acts as a competitive antagonist for the NK2 tachykinin receptor, exhibiting a pA2 value of 8.66. This compound is instrumental in studies investigating the role of tachykinins in various physiological and pathological processes. Its selective blockade of the NK2 receptor provides valuable insights into neurokinin signaling and associated therapeutic targets. -
Tachykinin NK1 Receptor Antagonist
[Tyr6,D-Phe7,D-His9]-Substance P (6-11) is a potent antagonist of the tachykinin NK1 receptor. This compound effectively inhibits hyperalgesia induced by histamine, making it valuable for research into pain pathways and the mechanisms of nociception. Its application extends to studies investigating the role of tachykinins in various biological processes and pain modulation. -
Analog of Substance P
[DAla4] Substance P (4-11) is an analog of Substance P that primarily targets neurokinin-1 receptors. It exhibits inhibitory activity against the binding of 125I-Bolton Hunter-conjugated Eledoisin and 125I-Bolton Hunter-conjugated Substance P to rat brain cortex membranes, with IC50 values of 0.5 μM and 0.15 μM, respectively. This compound is valuable for research into neuropeptide signaling, pain modulation, and related neurological pathways. -
NK-2R Antagonist
SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist, exhibiting a Ki of 193 nM for human NK-2R and a much higher Ki of 1 nM for human NK-3R. This compound demonstrates a lack of binding affinity for the human μ-opioid receptor (hMOR). SB 414240 is particularly valuable for research focused on neurological diseases, enabling studies on the modulation of neurokinin pathways in various neurological contexts. -
Tachykinin NK-2 Receptor Antagonist
Men 10376 is a selective tachykinin NK-2 receptor antagonist that exhibits a Ki value of 4.4 μM for the rat small intestine NK-2 receptor. This compound demonstrates significant inhibition of NK-2 receptor-mediated biological activities, making it a valuable tool for research into neurokinin signaling pathways. It is applicable in studies focused on gastrointestinal motility, pain modulation, and other physiological processes mediated by tachykinins. -
NK1 Receptor Agonist
Phyllomedusin is a tachykinin decapeptide that acts as an NK1 receptor agonist. It exhibits vasodilating properties and induces contraction of the pylorus, making it valuable for studying gastrointestinal motility and vascular biology. Research applications include investigations into neurokinin signaling pathways and potential therapeutic approaches for modulating blood flow and gut function. -
NK1 Receptor Antagonist
Lanepitant dihydrochloride is a non-peptide antagonist of the neurokinin-1 (NK1) receptor. It exhibits analgesic and anti-inflammatory properties, making it a valuable tool for research into pain pathways and inflammatory responses. This compound is useful in exploring the role of NK1 receptors in various biological processes and potential therapeutic applications in pain management. -
NK1 Antagonist
[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) is a potent antagonist of the neurokinin NK1 receptor. This peptide effectively inhibits the biological activities of substance P (SP) and gold-protein-substance P (GPSP), making it a valuable tool for research on pain signaling and neurogenic inflammation. Its application in studying the modulation of neurokinin-related pathways provides insights into potential therapeutic targets for various neuropsychiatric and inflammatory conditions. -
NK1 receptor Antagonist
NK1 receptor antagonist 2 acts as a selective antagonist for the neurokinin-1 (NK1) receptor, which plays a critical role in mediating pain and inflammatory responses. This compound demonstrates significant biological activity in reducing NK1 receptor signaling, making it relevant for research applications involving tinnitus and hearing loss. Its use may facilitate the exploration of therapeutic interventions targeting these auditory conditions. -
NK1 Receptor Antagonist
Imnopitant is a potent NK1 receptor antagonist known for its selective inhibition of the neurokinin-1 receptor. This compound demonstrates significant biological activity in modulating pain, anxiety, and depression-related pathways. It is primarily utilized in pharmacological research to explore therapeutic approaches for stress-related disorders and other conditions linked to neurokinin signaling. -
NK Receptor Antagonist
L-741671 is a selective antagonist of the neurokinin-1 (NK-1) receptor, exhibiting significant brain permeability. It demonstrates binding affinities (Kis) of 64 nM, 0.03 nM, and 0.7 nM in rat, human, and ferret models, respectively. This compound is primarily utilized in research to investigate the role of NK-1 receptors in various neurological conditions and to explore potential therapeutic applications in pain and mood disorders. -
NK-1 Receptor Antagonist
Ezlopitant is a selective non-peptidic antagonist of the neurokinin-1 (NK-1) receptor. It effectively inhibits both acute and delayed emetic responses induced by cisplatin in animal models by targeting NK-1 receptors in the central nervous system. This compound shows potential for research applications in pain management, chemotherapy-induced nausea and vomiting, and the study of irritable bowel syndrome. -
Neurokinin Receptor Inhibitor
NK3R-IN-1 is a potent inhibitor of the Neurokinin Receptor NK3R, characterized as an imidazolepiperazine derivative with oral bioavailability. This compound effectively lowers blood luteinizing hormone levels in ovariectomized models, demonstrating significant influence on neuroendocrine regulation. It serves as a valuable tool for research in reproductive biology and neurobiology, particularly in studies involving hormone modulation and neurological signaling pathways. -
NK-2 Antagonist
GR 83074 is a selective antagonist for the neurokinin 2 (NK-2) receptor, exhibiting a pKB of 8.23. It demonstrates significant potency with a 340-fold selectivity over the NK-1 receptor and is inactive as an NK-3 antagonist. This compound is valuable for research focused on the modulation of neurokinin pathways and their implications in various physiological and pathological conditions. -
NK1 Receptor Antagonist
CJ-17493 is a neurokinin-1 (NK1) receptor antagonist with a potent Ki of 0.2 nM. This compound also exhibits moderate affinity for the verapamil-binding site of L-type calcium channels (IC50 = 164 nM) and site 2 of sodium channels (IC50 = 48 nM). CJ-17493 is valuable for research applications focused on neurological disorders, providing insights into receptor signaling and potential therapeutic interventions. -
Tachykinin Analogue
Uperolein is a tachykinin analogue derived from the skin of Uperoleia rugosa and Uperoleia marmorata. This endecapeptide exhibits a potent spasmodic effect on gastrointestinal tissues and longitudinal muscles, making it a valuable tool for studying gut motility and muscle contraction mechanisms. Uperolein is useful in research applications focused on gastrointestinal disorders and neuropeptide signaling pathways. -
Neurokinin Receptor Agonist
[Nle11]-Substance P is an agonist of neurokinin receptors, designed to circumvent the oxidation issues associated with methionine in natural Substance P. This analog exhibits enhanced stability and retains biological activity, making it suitable for research studies focused on pain modulation, neurogenic inflammation, and neuropsychiatric disorders. Its application in various in vitro and in vivo models supports investigations into neurokinin signaling pathways and their implications in therapeutic interventions. -
Reversed Substance P
MLGFFQQPKPR-NH2 is a reversed Substance P peptide that acts as an antagonist to its neuropeptide target. This compound has demonstrated the ability to interfere with neurogenic inflammation and modulate pain response, making it a valuable tool for studies of nociception and neuropeptide signaling. Research applications include investigations into pain mechanisms and the development of potential therapeutic strategies for pain management. -
NK1/NK2 Antagonist
WIN 66306 is a cyclic heptapeptide that acts as an antagonist for neurokinin 1 (NK1) and neurokinin 2 (NK2) receptors. This compound exhibits significant antagonistic activity, making it a valuable tool for studies related to pain, inflammation, and various neurological disorders. Its role in modulating neurokinin signaling pathways supports research applications in pharmacology and neuroscience. -
hNK1 Antagonist
L 743310 is a selective non-peptide antagonist of the human neurokinin 1 (hNK1) receptor, exhibiting high affinity for both primate and cloned human receptors while displaying lower affinity for rodent NK1 receptors. This compound has demonstrated efficacy in inhibiting resiniferatoxin-induced plasma protein extravasation in guinea pig esophagus. Additionally, L 743310 exhibits a dose-dependent inhibitory effect on cisplatin-induced emesis, making it a valuable tool for research in neurokinin signaling and anti-emetic drug development. -
Neurokinin B Analogue
Tyr0-Neurokinin B is a Neurokinin B analogue that primarily targets neurokinin receptors. This compound has been shown to induce contractions in bladder smooth muscle, making it valuable for studying bladder physiology and potential therapeutic applications in urinary disorders. Researchers may utilize Tyr0-Neurokinin B to investigate the role of neurokinins in various biological processes and conditions related to smooth muscle function. -
Neurokinin Receptor Agonist
Scyliorhinin II is a selective neurokinin-3 receptor agonist, exhibiting a Ki value of 2.5 nM for the neurokinin-3 receptor in rat cerebral cortex. This compound plays a significant role in modulating neurogenic inflammatory processes and has potential applications in the study of neurokinin signaling pathways. It is valuable for researching the physiological and pharmacological roles of neurokinin receptors in various biological systems. -
Tachykinin NK1 Receptor Antagonist
GR 82334 is a potent and selective reversible antagonist of the tachykinin NK1 receptor. This compound effectively inhibits substance P-induced sensitization by blocking NK1 receptors, demonstrating its utility in research related to pain modulation and neurobiology. The specific mechanism of action makes GR 82334 a valuable tool for investigating the role of tachykinins in various biological processes and for exploring potential therapeutic applications.
