Neurokinin Receptors

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. Neurokinin-1 Receptor Antagonist

    SLV-317 is a selective antagonist of the neurokinin-1 receptor, exhibiting oral bioavailability. It effectively inhibits substance P-induced responses, making it a valuable compound for studying neurokinin signaling pathways. This compound is particularly relevant in research focused on pain, anxiety, and other neurogenic conditions.
  29. NK1/NK3 Antagonist

    RO4583298 is a potent dual antagonist of NK1 and NK3 receptors, exhibiting oral bioavailability. This compound effectively inhibits senktide-induced enhancement of the spontaneous activity of dopaminergic neurons, making it valuable for research in neuropharmacology. Additionally, RO4583298 has been shown to block foot tapping responses in gerbils and inhibit tail whips in mice, supporting its utility in behavioral studies related to neurokinin receptor modulation.
  30. Tachykinin Antagonist

    [D-Pro4,D-Trp7,9,10] Substance P (4-11) is a potent antagonist of tachykinin receptors. This peptide plays a crucial role in the modulation of neuropeptide signaling pathways and is utilized in research investigating pain perception, inflammation, and neurogenic processes. Its ability to inhibit tachykinin-mediated activities makes it valuable for studies exploring the therapeutic potential in various neurological disorders.
  31. Neurokinin Receptor Antagonist

    MEN 10208 is a neurokinin A antagonist that effectively targets neurokinin receptors, inhibiting their activity. This compound is primarily utilized in research focused on neurobiology and the regulation of pain, anxiety, and other neurological disorders. MEN 10208 can serve as a valuable tool for exploring the physiological roles of neurokinin signaling in various biological contexts.
  32. Substance P Antagonist

    [D-Pro4,D-Trp7,9] Substance P (4-11) is a potent antagonist of Substance P, targeting neurokinin receptors involved in pain and inflammatory responses. It has been shown to effectively decrease plasma aldosterone concentrations, indicating a role in modulating vascular and endocrine functions. This compound is valuable for research applications focused on pain management, neurobiology, and hormonal regulation.
  33. NK2 Antagonist

    UK-224671 is a selective antagonist of the neurokinin-2 (NK2) receptor. This compound exhibits significant potential in modulating NK2 receptor-related pathways, making it valuable for research focused on neurokinin signaling and its implications in various physiological and pathological conditions. It is noteworthy that UK-224671 is influenced by P-glycoprotein efflux and has limited intrinsic membrane permeability, which may affect its oral bioavailability in experimental contexts.
  34. NK1 Receptor Antagonist

    CP 122721 is an orally active antagonist of the neurokinin-1 (NK1) receptor. It exhibits significant antiemetic effects, effectively reducing cisplatin-induced vomiting in ferrets, with an ID50 of 0.08 mg/kg. Additionally, CP 122721 inhibits kainate-induced seizure activity and protects against CA1 neuronal cell death in rat models. This compound is valuable for research applications in depression, asthma, and irritable bowel syndrome (IBS).
  35. NK-1 Receptor Antagonist

    L-733060 is a selective neurokinin-1 (NK-1) receptor antagonist that effectively inhibits the binding of Substance P to its receptor. This compound modulates pain transmission and neural plasticity, making it particularly relevant for chronic pain research. L-733060 has demonstrated efficacy in reversing orofacial hyperalgesia and inhibits neurogenic plasma extravasation without causing cardiovascular side effects in animal models. Its potential applications extend to studies involving chronic orofacial pain and neurogenic inflammation.
  36. Neurokinin 2 Receptor Agonist

    L 363851 is a potent agonist of the neurokinin 2 receptor, demonstrating a significant contractile response in tracheal smooth muscle tissue devoid of epithelium with an IC50 value of 3.2 nM. Additionally, it stimulates phosphoinositide hydrolysis with an IC50 of 36 μM. This compound is valuable for research applications focusing on respiratory physiology and neurogenic inflammation.
  37. Substance P Agonist

    Substance P (4-11) is a Substance P agonist that specifically targets and activates NK1 receptors. This C-terminal fragment of Substance P exhibits potent biological activity, making it valuable for research in neurobiology, pain modulation, and inflammation. Its selective interaction with NK1 receptors offers insights into neurokinin signaling pathways and potential therapeutic applications.
  38. NK-1 Receptor Antagonist

    Lanepitant is a selective neurokinin-1 (NK-1) receptor antagonist. It inhibits neurogenic inflammation and pain transmission by blocking the interaction of substance P with NK-1 receptors found in both neuronal and non-neuronal tissues. Lanepitant is particularly useful in research related to osteoarthritis and understanding pain mechanisms.
  39. Substance P Inhibitor

    [D-Pro2,D-Phe7,D-Trp9] Substance P is a synthetic analogue of Substance P that functions as a potent inhibitor of the neuropeptide. It exhibits a significant ability to modulate neurogenic inflammation and pain response by blocking Substance P-mediated signaling pathways. This compound is useful in studying the role of Substance P in pain and gastrointestinal motility research applications, particularly in models involving guinea-pig ileum contraction.
  40. Neurokinin Receptor Agonist

    C14TKL-1 is a tachykinin-like peptide that acts as an agonist for neurokinin receptor 1 (NK-1). This compound is utilized in research to study the physiological roles of NK-1 in neurogenic inflammation and pain pathways. Its activity may provide insights into the underlying mechanisms of various neurological disorders and potential therapeutic targets.
  41. Neurokinin-1 Receptor Antagonist

    TAK-637 is an orally active antagonist of the neurokinin-1 receptor, known for its role in modulating neuronal signaling pathways. This compound has been shown to enhance bladder storage capacity and may provide insights into the treatment of functional bowel diseases, including irritable bowel syndrome. TAK-637 serves as a valuable tool for researchers investigating the therapeutic potential of neurokinin-1 receptor modulation in urological and gastrointestinal disorders.
  42. NK1 Receptor Antagonist

    TKA-731 is an NK1 receptor antagonist that effectively modulates nociceptive signaling. It has demonstrated the ability to reverse mechanical hyperalgesia and exhibit analgesic properties in neuropathic pain models, particularly in guinea pigs. This compound is valuable for research applications focused on understanding and targeting neuropathic pain mechanisms.
  43. NK3 Receptor Antagonist

    SSR 146977 is a selective antagonist of the tachykinin NK3 receptor. It demonstrates potent inhibition of neurokinin B binding to NK3 receptors in Chinese hamster ovary cells, with a Ki value of 0.26 nM. This compound is valuable in research focused on neurokinin signaling pathways and their implications in physiological and pathological conditions.
  44. NK1 Receptor Antagonist

    Rolapitant hydrochloride is a potent and selective neurokinin 1 (NK1) receptor antagonist, demonstrating a Ki value of 0.66 nM. This compound is distinguished by its long-acting and orally active properties. In pharmacological studies, rolapitant hydrochloride exhibits significant anti-emetic activity, as evidenced by its effectiveness in a ferret emesis model. Its unique mechanism makes it a valuable tool for research on emesis and nausea pathways.
  45. NK1R Fragment

    Neurokinin Receptor (393-407), rat, is a fragment of the rat neurokinin 1 receptor (NK1R), which is known for its role in mediating cellular responses to substance P through rapid internalization and subsequent recycling to the plasma membrane. This reagent is essential for investigating neurogenic inflammation and offers insights into the pathways associated with NK1R signaling. It serves as a valuable tool for researchers studying receptor dynamics and neuroinflammatory mechanisms.
  46. NK1 Receptor Antagonist

    L-703606 oxalate is a selective antagonist of the NK1 receptor, effectively inhibiting its activity. This compound plays a significant role in the study of gastric acid secretion, providing insights into neurokinin signaling pathways. Its potent inhibitory effects make it a valuable tool for research in gastrointestinal physiology and related disorders.
  47. NK1 Antagonist

    CP 122721 hydrochloride is a potent, selective non-peptide antagonist of the neurokinin NK1 receptor, exhibiting a pIC50 of 9.8 in human NK1 receptor assays using IM-9 cells. This compound demonstrates significant anxiolytic and antidepressant-like properties, making it a valuable tool for research in anxiety and mood disorder studies. It is suitable for investigating the role of NK1 receptors in neuropsychiatric conditions.
  48. Neurokinin Receptor

    Dapitant is a non-peptide antagonist targeting the neurokinin-1 (NK1) receptor, demonstrating high affinity for the human receptor. By inhibiting the binding of Substance P to NK1 receptors, Dapitant effectively blocks neurokinin-mediated biological effects. This compound serves as a potential therapeutic candidate for various conditions associated with Substance P, including neurogenic inflammation and pain modulation, making it valuable for research in pain management and inflammatory disorders.
  49. NK1 Antagonist

    FK888 is a highly selective dipeptide antagonist of the neurokinin-1 (NK1) receptor. It demonstrates a potent ability to displace [3H]-substance P binding, with a Ki value of 0.69 nM, making it an effective tool for studying NK1-related pathways. FK888 has been shown to inhibit substance P-induced airway edema in guinea pigs following both intravenous and oral administration, offering valuable insights for research in respiratory and inflammatory conditions.
  50. Substance P Analog

    [Glp5,Sar9] Substance P (5-11) is an analog of the neuropeptide Substance P, specifically designed to interact with the neurokinin-1 (NK1) receptor. This compound demonstrates potent biological activity by modulating pain perception and inflammatory responses, making it valuable in research focused on neurobiology and pain management. Its unique structure allows for the exploration of receptor binding and activity, facilitating the development of therapeutic agents targeting NK1 receptors.

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