Catalog No.
Product Name
Application
Product Information
Citations
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NOP Partial Agonist
Sunobinop is a selective partial agonist of the human nociceptin/orphanin FQ receptor (NOP), exhibiting high affinity for human targets (Ki=3.3 nM; EC50=4.03 nM; Emax=47.8%) while not engaging μ or κ opioid receptors. This compound significantly reduces wakefulness and enhances non-rapid eye movement sleep in rodent models, demonstrating a favorable side effect profile with no notable impacts on learning, memory, respiration, or intestinal function. Sunobinop also acts as a competitive antagonist in certain signaling pathways, particularly β-arrestin 2 recruitment, making it a valuable tool for research into conditions such as insomnia, alcohol use disorder, and overactive bladder-induced urinary incontinence. -
Enkephalinase Inhibitor
PL37 is a potent orally active enkephalinase inhibitor that targets both Neutral Endopeptidase and Aminopeptidase N, providing dual inhibition. This compound exhibits significant anti-hyperalgesic activity through the activation of μ-opioid receptors, demonstrating an ED50 of 13.4 mg/kg for analgesic effects in murine models. PL37 is valuable for research into the mechanisms underlying diabetic neuropathic pain and related pain management strategies. -
Prodrug Of The Loperamide
Loperamide oxide is a prodrug of Loperamide, designed to enhance its therapeutic efficacy. Upon ingestion, Loperamide oxide exhibits significant inhibition of fluid secretion in the intestinal lumen under aerobic conditions, making it valuable in research related to gastrointestinal disorders. This compound is utilized in studies focused on diarrhea management and related physiological mechanisms. -
κ2 Opioid Receptor Agonist
GR 89696 free base is a selective κ2 opioid receptor agonist that demonstrates potential in alleviating pruritus. Its specificity for the κ2 receptor underscores its utility in pharmacological research aimed at understanding pain modulation and itch signaling pathways. This compound is of interest in studies exploring therapeutic strategies for itch-related disorders. -
Opioid Receptor Antagonist
Icalcaprant is a kappa-opioid receptor antagonist that selectively inhibits kappa-opioid receptor activity. This compound exhibits potential applications in the modulation of pain response and substance abuse research. Its use in preclinical studies may aid in developing new therapeutic strategies for opioid-related disorders. -
μ-opioid Receptor Activator, hERG (Kv11.1) Potassium Channel Inhibitor
ERG-IN-6 is a potent μ-opioid receptor activator, exhibiting an EC50 of 0.12 nM, which makes it an effective tool for studies related to pain modulation. Additionally, ERG-IN-6 functions as a hERG (Kv11.1) potassium channel inhibitor with an IC50 of 0.681 μM. This compound is valuable for research applications investigating the interplay between opioid signaling and ion channel regulation. -
Opioid Receptor Antagonist
AT-076 is a potent pan antagonist of opioid receptors, specifically binding to nociception (NOP), mu (MOP), kappa (KOP), and delta (DOP) opioid receptors with Ki values of 1.75 nM, 1.67 nM, 1.14 nM, and 19.6 nM, respectively. It exhibits significant biological activity, making it a valuable tool for research in pain management and opioid receptor functionality. AT-076 is useful in studies investigating the roles of opioid receptors in various physiological and pathological conditions. -
Opioid Mixed Agonist-Antagonist
Picenadol hydrochloride is an opioid mixed agonist-antagonist primarily targeting the μ-opioid receptor. The compound consists of a racemic mixture, with the d-isomer (LY-136596) exhibiting potent agonistic activity, while the l-isomer (LY-136595) functions as a weak competitive antagonist, potentially mitigating the risk of opioid dependence. In addition to its analgesic properties, Picenadol hydrochloride possesses anticholinergic activity, making it relevant for research in pain management and addiction studies. -
κ-OR Agonist
GR103545 is a potent and selective agonist of the κ-opioid receptor (κ-OR). This compound exhibits significant activity in mediating κ-OR signaling pathways, making it valuable for investigating pain modulation and potential treatments for substance use disorders. Additionally, GR103545 serves as an effective radiotracer for in vivo imaging of κ-OR, facilitating the study of this receptor's distribution and function in various biological contexts. -
Opioid Receptor Agonist
SC13 is a novel mitragynine analog that functions as a low-efficacy agonist of the Mu opioid receptor. It exhibits significant antinociceptive properties while minimizing common adverse effects typically associated with opioid receptor activation. This compound is suitable for research applications focused on pain management and the pharmacological characterization of opioid receptor interactions. -
β-Casomorphin Fragment
β-Casomorphin (1-5), bovine TFA is a bioactive peptide derived from bovine β-Casomorphin. This compound primarily targets opioid receptors, exhibiting significant analgesic and neuroprotective activities. Research applications include studies on pain modulation, the effects of milk-derived peptides, and investigations into opioid receptor signaling pathways. -
Opioid Receptor Agonist
Loperamide phenyl is an opioid receptor agonist that serves as an impurity of Loperamide. It exhibits key biological activity by modulating opioid receptors, which can affect pain perception and gastrointestinal function. This compound is primarily used in research applications involving opioid receptor signaling and the pharmacological understanding of opioid-related effects. -
KOR Receptor Agonist
BRL-52656 is a potent Kappa opioid receptor (KOR) agonist with the ability to cross the blood-brain barrier. This compound exhibits a biphasic impact on blood pressure, reducing it at lower doses while causing an increase at higher doses in spontaneously hypertensive rats. Furthermore, BRL-52656 induces water diuresis by inhibiting vasopressin (AVP) secretion, making it relevant for research in cardiovascular and renal physiology. -
Endomorphin-1 Modifiers
N-terminally acetylated Endomorphin-1 is a modified form of the endogenous opioid peptide Endomorphin-1. This compound exhibits high binding affinity for μ-opioid receptors, contributing to its analgesic properties. It is utilized in research focused on pain modulation, opioid receptor signaling, and the development of novel analgesics. -
KOR Agonist
SalA-VS-07 is a G protein-biased partial agonist specifically targeting the kappa-opioid receptor (KOR). It demonstrates significant analgesic properties and is utilized in research exploring pain management and various related disorders. This compound serves as a valuable tool for studies investigating the therapeutic potentials of KOR modulation. -
ORL1 Agonist
GRT2932Q is a nonpeptidic agonist targeting the opioid receptor-like 1 (ORL1). This compound exhibits significant biological activity in modulating ORL1 receptor pathways, making it valuable for research in pain management and neurobiology. Its specificity for ORL1 allows for exploration of its potential therapeutic applications in anxiety, depression, and other neuropsychiatric disorders. -
Opioid Receptor Ligand
LY164929 is a highly selective ligand for opioid receptors, specifically targeting the low-affinity binding site of [3H]D-Ala2-D-Leu-5-enkephalin. It demonstrates an exceptional 1,986-fold selectivity over other opioid ligands, making it a valuable tool for studying opioid receptor function and pharmacology. This compound is ideal for research applications involving pain management, addiction studies, and the development of novel analgesics. -
Opiate δ-receptor Agonist
Deltakephalin is a selective agonist of the opiate δ-receptor. It exhibits significant analgesic properties and is utilized in research to explore pain management and opioid receptor dynamics. This compound is valuable for studying δ-receptor-mediated pathways and their implications in analgesia and potential therapeutic applications. -
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.
