Catalog No.
Product Name
Application
Product Information
Citations
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μ opioid receptors
N-Desmethyl-loperamide is a significant metabolite of loperamide, primarily targeting μ-opioid receptors with a Ki value of 0.16 nM. This compound exhibits activity as a substrate for the ATP-dependent efflux transporter P-glycoprotein. It is useful for studies examining peripheral μ-opioid receptor activation and the role of P-glycoprotein in drug transport. -
μ-opioid Receptor Agonist
(-)-9-Hydroxycorynantheidine is a selective partial agonist of the μ-opioid receptor. It exhibits significant biological activity by inhibiting electrically stimulated twitch contractions in the guinea-pig ileum, making it relevant for research into opioid receptor function and pharmacology. This compound is useful for studies assessing the effects of μ-opioid receptor modulation in various biological contexts. -
κ-Opioid Receptor Agonist
6'-GNTI dihydrochloride is a selective κ-opioid receptor (KOR) agonist that preferentially activates G protein-mediated signaling while minimizing β-arrestin2 recruitment. This compound specifically induces activation of the Akt signaling pathway in striatal neurons, making it a valuable tool for investigating KOR-related mechanisms. Its unique bias in signaling provides insights into the therapeutic potential of KOR modulation in pain management and neurological research. -
Nociception/Mu Opioid Receptor Agonist
AT-121 is a bifunctional agonist targeting nociception and the mu opioid receptor, demonstrating dissociation constants (Kis) of 3.67 and 16.49 nM, respectively. This compound exhibits significant antinociceptive and antiallodynic properties while maintaining a profile indicative of safety and non-addictiveness. AT-121 is of particular interest in pain management research, providing potential avenues for developing effective analgesics without the risks associated with traditional opioids. -
δ-opioid Receptor Agonist
TAN-67 dihydrobromide is a potent and selective nonpeptidic agonist of the δ-opioid receptor, exhibiting a Ki value of 0.647 nM. This compound demonstrates neuroprotective effects, making it a valuable tool in research focused on ischemic stroke and related neurological conditions. Its specificity for the δ-opioid receptor positions TAN-67 dihydrobromide as a significant reagent for exploring opioid receptor signaling and potential therapeutic interventions. -
μ-opioid Agonist
Acetyl tetrapeptide-15 is a synthetic peptide that functions as a μ-opioid agonist. It mimics the action of endomorphin-2, promoting selective anti-nociceptive effects that alleviate skin hyperreactivity associated with inflammatory, chronic, and neuropathic pain. By enhancing the threshold of neuronal excitability through μ-opioid receptor pathways, Acetyl tetrapeptide-15 is primarily utilized in cosmetic formulations aimed at sensitive skin. -
µ-opioid Receptor Antagonist
Naldemedine is a potent μ-opioid receptor antagonist, designed for the treatment of opioid-induced constipation (OIC). It exhibits high binding affinities for μ-, δ-, and κ-opioid receptors, with Ki values of 0.34, 0.43, and 0.94 nM, respectively, and shows significant antagonist activity with IC50 values of 25.57, 7.09, and 16.1 nM. Additionally, Naldemedine is predicted to interact with 3CLpro, an enzyme encoded by the SARS-CoV-2 genome, making it a valuable tool for various research applications in opioid receptor mechanisms and viral interactions. -
Opioid Receptor Agonist
α-Casein (90-95) is a partial agonist of opioid receptors, exhibiting significant biological activity through its effects on mast cells and prostate cancer cells. It inhibits the secretion of β-hexosaminidase from rat peritoneal mast cells with an IC50 of 0.1 μM and demonstrates antiproliferative effects on LNCaP, DU145, and PC3 prostate cancer cells with IC50 values of 0.94 nM, 137 nM, and 6.92 nM, respectively. This reagent activates Gi-like proteins via a receptor-independent mechanism and promotes intracellular calcium release. α-Casein (90-95) is valuable for investigating mechanisms underlying allergic diseases and prostate cancer. -
Delta-opioid Receptor Antagonist
ICI 154129 is a potent antagonist of the delta-opioid receptor, primarily utilized in research investigating opioid receptor signaling pathways. Its ability to inhibit delta-opioid receptor activity makes it valuable for studying the role of these receptors in seizure mechanisms and related neurological conditions. This compound serves as an important tool in understanding the therapeutic potential of delta-opioid receptor modulation. -
κ3-opioid Receptor Agonist
Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, exhibiting mixed agonist/antagonist properties. It acts as a partial agonist at cloned μ and δ opioid receptors while functioning as an antagonist at NOP receptors. Its pharmacological profile suggests significant analgesic effects, making it valuable for research into pain modulation and opioid receptor interactions. -
Opioid Receptor Antagonist
Naloxegol is a μ-opioid receptor antagonist that specifically targets opioid receptors in the gastrointestinal tract. It effectively inhibits opioid binding, thereby alleviating symptoms of opioid-induced constipation. Naloxegol is useful in research applications related to pain management and gastrointestinal health. -
Opioid Receptor Antagonist
(S,S)-J-113397 is a selective antagonist of opioid receptors, specifically targeting the mu and delta receptor subtypes. This compound inhibits the binding of opioid peptides, making it valuable for research applications focused on pain management, addiction studies, and the exploration of opioid receptor signaling pathways. Its unique structural isomerism distinguishes it from related compounds, providing crucial insights into receptor dynamics and interactions. -
Opioid Antagonist
6β-Naltrexol is a potent peripherally selective opioid antagonist, primarily recognized as the major metabolite of Naltrexone. It effectively inhibits opioid effects in the gastrointestinal tract, demonstrating significant potential in counteracting Morphine-induced delays in gastrointestinal transit. This compound is valuable for research applications focused on opioid receptor dynamics and gastrointestinal motility. -
δ1-opioid Receptor Antagonist
BNTX maleate is a potent δ1-opioid receptor antagonist, exhibiting Ki values of 0.1 nM for the δ1 receptor, alongside 10.8 nM for δ2, 13.3 nM for μ, and 58.6 nM for κ-opioid receptors. This compound demonstrates significant antinociceptive activity, making it valuable for research in pain modulation and opioid receptor signaling. Its specificity for the δ1-opioid receptor positions BNTX maleate as a useful tool in studying the physiological and pharmacological roles of opioid receptors in various biological contexts. -
mu-Opioid Receptor Antagonist
Methyl-6-alpha-Naltrexol is a potent mu-opioid receptor antagonist and a metabolite of Methylnaltrexone (MNTX). It primarily acts as a peripherally acting receptor antagonist within the gastrointestinal tract, making it valuable for studying opioid receptor dynamics and gastrointestinal function. This compound is useful in research focused on opioid-induced constipation and opioid receptor modulation in peripheral tissues. -
Opioid Compound
N-Propionitrile Chlorphine hydrochloride is an opioid compound that exhibits affinity for opioid receptors, primarily influencing pain modulation pathways. Its structural similarity to known opioids facilitates exploration in pain management and analgesic research. This compound is suitable for studies investigating opioid receptor signaling and the development of novel analgesics. -
Opioid Receptor
Alvimopan metabolite is a selective μ opioid receptor antagonist that primarily targets peripheral μ receptors. This compound exhibits significant inhibitory activity, making it a promising candidate for mitigating the adverse effects associated with opioid use. Its specificity for μ opioid receptors highlights its potential applications in pain management and opioid-related side effect amelioration. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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). -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
