Catalog No.
Product Name
Application
Product Information
Citations
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μ-Opioid Receptor Agonist
Lexanopadol is a μ-opioid receptor agonist with additional activity at nociceptor receptors (ORL-1). It demonstrates significant analgesic properties and is utilized in pain research. This compound aids in the investigation of pain pathways and the evaluation of potential therapeutic interventions for pain management. -
Opioid Agonist
[D-Ala2]-Met-Enkephalin is a synthetic opioid peptide that acts as a potent agonist at opioid receptors. It has demonstrated effectiveness in inhibiting acetylcholine-induced and suckling-induced release of oxytocin, highlighting its role in modulating pain and neuroendocrine functions. This compound is valuable for research applications exploring opioid receptor activity and its physiological impacts in neurobiology. -
KOR Agonist
MOR agonist-4 is a G protein signaling-biased agonist of the Kappa opioid receptor (KOR) with an EC50 value of 11 nM. This compound features an electron-withdrawing CF3 group and exhibits a bias factor of 38 based on triazole structure. It is primarily utilized in research related to pruritus and pain relief, facilitating the study of analgesic pathways and mechanisms. -
Opioid Receptor
SR-8993 is a highly selective agonist of the nociceptin receptor, capable of crossing the blood-brain barrier. This compound demonstrates significant biological activity by reducing alcohol intake and alleviating withdrawal anxiety in animal models. Research applications of SR-8993 include the evaluation of its effects on restricted drinking behaviors, operant responses for alcohol, and its potential to mitigate alcohol-seeking behavior linked to stress and cues following withdrawal. -
σ1 Antagonist/μ Opioid Agonist
σ1 Receptor/μ Opioid Receptor Modulator 1 is a potent antagonist of the σ1 receptor and an agonist of the μ opioid receptor, with binding affinities (Kis) of 1.86 nM and 2.1 nM, respectively. This compound demonstrates significant analgesic effects, making it a valuable tool for research focused on neuropathic pain mechanisms. Its dual action highlights its potential in studying pain pathways and developing innovative pain management therapies. -
KOR Agonist
Enadoline hydrochloride is a highly selective kappa-opioid receptor (KOR) agonist with a Ki value of 1.25 nM. This nonpeptide compound has demonstrated significant antinociceptive effects, making it valuable for studying pain mechanisms and potential therapeutic applications in pain management. Its ability to penetrate the blood-brain barrier further enhances its utility in neurological and pharmacological research. -
Cholecystokinin Analog
SNF 9007 is a cholecystokinin analog that primarily targets δ-1, δ-2, and μ opioid receptors. It demonstrates significant analgesic activity by modulating pain signaling pathways in the central nervous system. This compound is suitable for research applications studying pain mechanisms and opioid receptor interactions in preclinical models. -
Opioid Receptor
MR2034, a selective κ-opioid receptor agonist, modulates the hypothalamic-pituitary-adrenal axis. Its biological activity has demonstrated potential to enhance mood and reduce addictive behaviors in animal models. MR2034 is a valuable tool for investigating therapeutic strategies targeting mood regulation and addiction disorders in research settings. -
ORL1 Receptor Agonist
Nociceptin (1-13), amide is a selective agonist of the ORL1 receptor (opioid receptor-like 1 receptor, OP4). It exhibits strong affinity, with a pEC50 value of 7.9 in mouse vas deferens assays and a binding Ki of 0.75 nM in rat forebrain membranes. This compound is valuable in studies exploring nociception, pain modulation, and potential therapeutic applications in nervous system disorders. -
Mu-Opioid Receptor Antagonist
Mu opioid receptor antagonist 4 is a highly selective antagonist of the μ-opioid receptor (MOR), exhibiting a Ki of 0.38 nM and an EC50 of 1.07 nM. This compound demonstrates significant central nervous system antagonism against morphine while inducing fewer withdrawal symptoms compared to Naloxone. Mu opioid receptor antagonist 4 is suitable for research applications focused on opioid use disorders (OUD). -
ORL-1 Inhibitor
SB-612111 is a potent antagonist of the opiate receptor-like orphan receptor (ORL-1), exhibiting high affinity for human ORL-1 with a Ki of 0.33 nM. It demonstrates selectivity towards μ-, κ-, and δ-opioid receptors, with Ki values of 57.6 nM, 160.5 nM, and 2109 nM, respectively. SB-612111 effectively antagonizes the pronociceptive effects of nociceptin in acute pain models, making it a valuable tool for research into pain modulation and opioid receptor pathways. -
κ Opioid Receptor Agonist
Leumorphin, human is a potent κ opioid receptor agonist that demonstrates significant activity in modulating pain and stress responses. This compound specifically inhibits contractions in the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum, providing insights into gastrointestinal motility and receptor pharmacology. Its distinctive action makes Leumorphin, human a valuable reagent for research involving opioid receptor signaling and the effects of κ agonism in various biological contexts. -
Opioid Peptide
α-Neoendorphin (1-8) is an octapeptide derived from the N-terminal region of the endogenous opioid peptide α-Neoendorphin. It primarily targets opioid receptors, exerting analgesic effects and modulating pain responses in various biological systems. This peptide is utilized in research applications focused on pain management, neurobiology, and the study of opioid signaling pathways. -
μ Opioid Receptor Agonist
PL-017 is a potent and selective μ opioid receptor agonist, exhibiting an IC50 of 5.5 nM for the binding of 125I-FK 33,824 to the μ receptor site. This compound demonstrates significant analgesic activity, producing long-lasting and reversible pain relief in rat models. PL-017 is valuable for research applications in pain management and the study of opiate receptor pharmacology. -
MOPr Agonist
Bilaid C is a tetrapeptide recognized for its selective agonist activity at the μ-Opioid Receptor (MOPr), with a binding affinity (Ki) of 210 nM for the human receptor. Isolated from the Australian estuarine strain of Penicillium sp. MST-MF667, Bilaid C demonstrates significant potential in research applications targeting pain modulation, addiction, and opioid receptor signaling pathways. Its molecular properties make it a valuable tool for investigating the role of MOPr in various biological processes. -
Petide
Dynorphin B 29 (pig) is a peptide that primarily targets opioid receptors in the brain, contributing to its diverse biological effects. This compound exhibits key activities related to pain modulation and stress response, making it valuable for investigations in neuropharmacology. It can also be utilized in immunoreaction studies, allowing for deeper insights into receptor interactions and signaling pathways. -
MOR Agonist
Dermorphin TFA is a natural heptapeptide that acts as a potent agonist at the μ-opioid receptor (MOR). It has been shown to effectively inhibit neuropathic pain, making it a valuable tool for research in pain management and opioid receptor studies. Its unique properties provide insights into opioid signaling and therapeutic potential in alleviating chronic pain conditions. -
Anti-nociceptive Agent
AH 8532 is an opioid that functions as an anti-nociceptive agent, effectively inhibiting chemical-induced pain responses. It demonstrates significant analgesic properties, with an ED50 value of 16 mg/kg when administered orally in murine models. This compound is valuable for research applications exploring pain mechanisms and potential therapeutic interventions for pain management. -
Mu-opioid Agonist
DALDA is a potent and highly selective μ-opioid receptor agonist with a binding affinity (Ki) of 1.69 nM. It demonstrates significant antinociceptive effects, making it useful in pain management research. Additionally, DALDA has implications in studying respiratory effects related to μ-opioid receptor activation. -
MOR Receptor Agonist
μ Opioid Receptor Agonist 2 (Compound H-3) is an optically pure oxaspiro ring-substituted pyrrolopyrazole derivative that functions as a selective agonist for the μ-opioid receptor (MOR). This compound exhibits significant analgesic activity and is instrumental in research related to pain mechanisms and pain-related disorders. Its specificity for MOR makes it a valuable tool for studying opioid receptor pathways and developing new therapeutic strategies for pain management. -
Analgesics
AH 7959 is an orally active N-substituted cyclohexyl methyl benzamide that acts as an analgesic. It demonstrates significant analgesic effects, with an ED50 greater than 100 mg/kg for both oral and subcutaneous administration in murine models. This compound is a valuable tool for research in pain management and the development of novel analgesic therapies. -
μ Opioid Receptor Antagonist
Acetalin-3 (Ac-RFMWMT-NH2) is a hexapeptide that functions as a potent antagonist of the μ opioid receptor. It exhibits high affinity for both the μ and κ3 opioid receptors, while demonstrating weak affinity for the κ1 receptor and lack of affinity for the κ2 receptor. This compound is valuable in research applications focused on opioid signaling pathways and the development of analgesics while providing insights into opioid receptor interactions. -
Opioid Antagonist
β-Endorphin (1-27) (human) is an opioid antagonist that selectively targets μ-, δ-, and κ-opioid receptors, exhibiting IC50 values of 5.31, 6.17, and 39.82 nM, respectively. This peptide effectively inhibits analgesic responses induced by both β-Endorphin and etorphine. Its biological activity is instrumental in opioid research, particularly in studies focusing on pain modulation and receptor interactions. -
Dynorphin Derivative
Dynorphin (2-17), amide (porcine) is a dynorphin derivative that acts primarily on opioid receptors to exhibit analgesic properties. This peptide plays a significant role in modulating pain perception, addiction pathways, and mood regulation. It is utilized in various research applications studying opioid mechanisms and neuropharmacology. -
KOR Activator
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator, exhibiting a Ki of 21 nM and an EC50 of 45 nM. It demonstrates significant KOR-specific peripheral analgesic activity in mouse models of chronic visceral pain. This compound is valuable for investigating the role of KOR in pain modulation and may provide insights into therapeutic approaches for pain management. -
Opioid Receptor Modulator
DS34942424 is an opioid receptor modulator that functions as a potent analgesic while demonstrating no mu opioid receptor agonist activity. This unique profile makes it a valuable candidate for research focused on pain management and opioid alternatives, potentially reducing the risk of addiction associated with traditional opioid therapies. It is suitable for studies aimed at investigating new pathways in pain relief and the modulation of opioid receptor activity. -
Opioid Neuropeptide
β-Endorphin (rat) is an endogenous opioid neuropeptide that primarily targets opioid receptors, playing a key role in pain modulation. Its analgesic properties make it significant in studies related to pain management and the regulation of food intake in satiated states. This reagent is valuable for research investigating neurological disorders, including analgesia and drug addiction. -
Opioid Mixed Agonist-Antagonist
Picenadol is an opioid mixed agonist-antagonist that primarily targets the μ-opioid receptor. The compound consists of a racemic mixture, with the d-isomer functioning as a potent μ-opioid receptor agonist and the l-isomer acting as a weak competitive antagonist, which diminishes the agonist effect and mitigates the risk of dependence. Additionally, Picenadol exhibits anticholinergic activity, making it relevant for research applications in pain management and opioid pharmacology. -
Opioid Receptor
SR14150 is a partial agonist of the nociceptin/orphanin FQ peptide (NOP) receptor, exhibiting high affinity. This compound demonstrates significant analgesic properties, potentially facilitating the advancement of novel multi-target opioids aimed at enhancing pain relief while minimizing adverse effects. Additionally, SR14150's interaction with various opioid receptors may offer innovative therapeutic strategies for chronic pain management. -
Anticonvulsant
U-54494A is a benzamide derivative that acts as an agonist of the κ-opioid receptor. This compound exhibits notable anticonvulsant activity, making it a valuable tool in the study of seizure disorders. Its unique mechanism of action may provide insights into therapeutic strategies for neurological conditions associated with excessive neuronal excitability. -
NOP Partial Agonist
Ac-RYYRWK-NH2 is a selective partial agonist for the nociceptin receptor (NOP). This compound demonstrates high binding affinity to rat cortical membranes with a Kd value of 0.071 nM, while showing no significant affinity for µ-, κ-, or δ-opioid receptors. Ac-RYYRWK-NH2 is useful for studying nociceptin signaling pathways and exploring potential therapeutic applications in pain management and neurobiology. -
ORL1 Agonist
[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 is a selective agonist for the nociceptin receptor (ORL1). This compound has been demonstrated to significantly inhibit the nociceptive flexor reflex in rodent models, highlighting its potential utility in analgesia studies. [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 is a valuable tool for investigating pain mechanisms and developing therapeutic strategies for pain management. -
Opioid Agent
AH-8533 is an opioid agent that primarily targets μ-opioid receptors. This compound exhibits potent analgesic properties, making it valuable for pain management research. Its pharmacological profile may facilitate studies on opioid signaling pathways and the development of novel therapeutic strategies for pain relief. -
Analgesics
Sameridine is a weak partial agonist of the μ-opioid receptor, primarily utilized in analgesic applications. Exhibiting local anesthetic and analgesic properties, Sameridine provides a unique profile with minimal respiratory depression at low doses, though higher doses may suppress ventilatory response. This compound is valuable for research focused on exploring analgesic effects and opioid receptor pharmacology. -
Opioid Receptor Antagonist
N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu is a selective antagonist of the δ-opioid receptor, effectively inhibiting the actions of enkephalins such as [D-Pen2,D-Pen5] enkephalin in vivo. This compound is suitable for behavioral experiments aimed at studying opioid receptor functions and exploring potential therapeutic approaches for opioid-related disorders. Its unique structure supports research into the modulation of pain pathways and addiction mechanisms. -
δ-opioid Receptor Agonist
BW373U86 is a highly selective δ-opioid receptor agonist with an IC50 value of 1.49 nM. It has demonstrated antidepressant-like effects in preclinical studies, making it a valuable tool for research into mood disorders and the underlying mechanisms of opioid receptor signaling. This compound is particularly relevant for investigations into pain management and the modulation of emotional states. -
Analgesic
Allyphenyline oxalate acts primarily as an analgesic, enhancing the analgesic effects of Morphine. It demonstrates affinity for adrenergic α2 receptor subtypes with pKi values of 7.24 for α2A, 6.47 for α2B, and 7.07 for α2C. This compound is valuable for research focused on pain management and the modulation of opioid analgesia. -
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. -
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.
