Neurokinin Receptors

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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).
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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