Catalog No.
Product Name
Application
Product Information
Citations
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Opioid Receptor Agonist
AWL 60 is an opioid receptor agonist that also exhibits properties as a substance P (SP) antagonist. This compound has been shown to antagonize SP agonists in vitro, as well as attenuate hypotension induced by SP agonists in vivo. AWL 60 is relevant for research applications focused on pain modulation, opioid receptor signaling, and neuroinflammatory responses. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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). -
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. -
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. -
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. -
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. -
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. -
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. -
Opioid Receptor Agonist
SR16835 is a selective agonist targeting the nociceptin/orphanin FQ peptide (NOPr) and mu-opioid receptor (MOPr). It exhibits full agonist activity at NOPr and partial agonist activity at MOPr, allowing for detailed exploration of opioid receptor mechanisms. Notably, SR16835 does not produce analgesic effects, making it a valuable tool for research into receptor-specific functions and therapeutic applications in pain management and opioid signaling pathways. -
NOP Receptor Agonist
[Arg14,Lys15]Nociceptin is a highly potent and selective agonist of the NOP receptor (also known as ORL1 or OP4), exhibiting an EC50 of 1 nM. This compound demonstrates exceptional specificity for the NOP receptor, with IC50 values of 0.32 nM for NOP and significantly higher values for μ (280 nM), δ (>10,000 nM), and κ (1500 nM) opioid receptors. [Arg14,Lys15]Nociceptin is valuable for research applications exploring pain modulation, neuropharmacology, and the role of nociceptin in various physiological processes. -
NOP Antagonist
NOP Antagonist 1 is a nociceptin opioid peptide (NOP) antagonist with a binding affinity characterized by a Kb of 8.65 nM. This compound is valuable for research focused on neuropsychiatric disorders, as it modulates nociceptin receptor activity, providing insights into pain signaling and potential therapeutic strategies. Its specificity and potency make it an essential tool for exploring the role of the NOP system in various physiological and pathological conditions. -
μ-opioid Receptor Antagonist
Mu Opioid Receptor Antagonist 8 is a selective antagonist of the μ-opioid receptor. This compound effectively inhibits met-enkephalin-induced activation of the receptor via the Gi signaling pathway, making it valuable for research in pain management and addiction studies. Its ability to modulate μ-opioid receptor activity positions it as a critical tool for understanding opioid receptor pharmacology and potential therapeutic interventions. -
κ Opioid Receptor Agonist
Riminkefon is a κ-opioid receptor agonist that selectively binds to and activates the κ-opioid receptor, leading to various physiological effects. It exhibits significant analgesic properties and has been employed in research related to pain management, mood regulation, and the study of addictive behaviors. Riminkefon serves as a valuable tool for exploring the therapeutic potential of κ-opioid receptor modulation in various neurological and psychological conditions. -
MOR Agonist
SR-14968 is a full allosteric and non-competitive agonist of the mu-opioid receptor (MOR), exhibiting an EC50 of 88 nM in mouse brainstem assays. This compound stabilizes the MOR in a G protein signaling state that demonstrates resistance to washout, while remaining reversible by antagonists. SR-14968 is capable of inducing respiratory depression in murine models, making it a valuable tool for exploring pain-related mechanisms and the pharmacological effects of MOR activation in research settings. -
Kappa-Opioid Receptor Agonist
LPK-26 hydrochloride is a selective kappa-opioid receptor agonist, exhibiting a Ki of 0.68 nM. This compound demonstrates significant antinociceptive properties while showing low potential for physical dependence. It is valuable for research into pain management and the mechanisms of opioid receptor activation. -
µ-Opioid Receptor Agonist
Bilaid A1e is a tetrapeptide that acts as an agonist of the µ-opioid receptor, exhibiting a binding affinity with a Ki value of 750 nM. Isolated from an Australian estuarine strain of Penicillium sp., Bilaid A1e holds potential for applications in pain research. Its ability to modulate µ-opioid receptor activity makes it a valuable tool for studying analgesic pathways and developing pain management strategies. -
Urotensin II Antagonist
Urotensin-II receptor antagonist-1 is a selective antagonist of the human Urotensin II receptor, exhibiting a Ki value of 16 nM in HEK293 cells expressing the recombinant receptor. This compound demonstrates significant biological activity by inhibiting cytochrome P450 enzymes, CYP2D6 and CYP3A4, with IC50 values of 0.75 μM and 1.4 μM, respectively. Additionally, it inhibits the κ-opioid receptor with an EC50 of 3.2 μM and targets cardiac sodium channels with a Ki of 2.5 μM. Research applications include studies of cardiovascular physiology and drug metabolism. -
Opioid Receptor
Faxeladol is an opioid receptor modulator that exhibits significant analgesic activity. In clinical trials, it demonstrated a reduction in mean pain intensity in patients suffering from painful polyneuropathy, supporting its potential as an effective pain management agent. The compound is characterized by a favorable safety profile, making it a candidate for further research in pain relief applications. -
Opioid Receptor Antagonist
LY2048978 is a non-selective opioid receptor antagonist that exhibits Ki values of 0.287 nM, 0.471 nM, and 1.05 nM for human mu, kappa, and delta opioid receptors, respectively. This compound is relevant for studying the physiological roles of opioid receptors and is applied in research related to major depressive disorder and alcohol use disorder. Its antagonistic properties make it a valuable tool for investigating opioid-mediated pathways and potential therapeutic interventions. -
Opioid Agonist
D-Ala2-Met-Enkephalinamide is an opioid peptide that functions as a potent opioid agonist. It exerts analgesic effects and is known to decrease bile flow through central mechanisms. This compound is valuable in research applications focused on pain management and opioid receptor activity. -
Mu-Opioid Receptor Antagonist
Mu Opioid Receptor Antagonist 5 is a selective antagonist of the μ-opioid receptor (MOR) with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. This compound is capable of penetrating the blood-brain barrier, making it a valuable tool for studying the mechanisms underlying opioid use disorders (OUD). Its high potency and specificity for the MOR facilitate insightful research into opioid-related signaling pathways and potential therapeutic interventions. -
Opioid Peptide
Biphalin TFA is a potent opioid peptide analog designed for effective interaction with opioid receptors, demonstrating a dual enkephalin pharmacophore structure that facilitates blood-brain barrier penetration. This compound exhibits significant analgesic properties in various pain models, including acute, neuropathic, and chronic settings. Additionally, Biphalin TFA has been shown to possess antiviral, antiproliferative, anti-inflammatory, and neuroprotective activities, making it a valuable tool for research in pain management and related therapeutic areas.
