Catalog No.
Product Name
Application
Product Information
Citations
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δ-opioid Agonist
KNT-127 is a selective δ-opioid receptor (DOR) agonist that effectively crosses the blood-brain barrier (Ki = 0.16 nM). It demonstrates high selectivity for the δ receptor, with Ki values of 0.16 nM, 21.3 nM, and 153 nM for δ, μ, and κ receptors, respectively. As a biased ligand, KNT-127 primarily activates cyclic adenosine monophosphate (cAMP) signaling while exhibiting lower beta-arrestin signaling. This compound enhances the release of dopamine and L-glutamate in key brain regions, including the striatum, nucleus accumbens, and prefrontal cortex, and is relevant for studies on neurological diseases due to its antidepressant and anxiolytic-like effects. -
Kappa Opioid Receptor Agonist
Anrikefon acetate is an agonist of the kappa opioid receptor, demonstrating notable analgesic activity. This compound is of interest in researching pain management and the modulation of mood disorders. Its selective action on kappa receptors makes it a valuable tool for investigating pathways involved in opioid receptor signaling and potential therapeutic applications. -
Opioid Receptor Agonist
[D-Ala2]leucine-enkephalin is a delta opioid receptor agonist designed for investigating opioid signaling pathways. This stable analog of Leu-enkephalin exhibits prolonged biological activity, making it a valuable tool for researchers studying the pharmacological effects and physiological roles of delta opioid receptors in various biological systems. Its resistance to enzymatic degradation allows for extended experiments without loss of efficacy. -
κ-opioid Receptor Agonist
Spiradoline mesylate is a selective kappa-opioid receptor (KOR) agonist with a Ki of 8.6 nM, demonstrating strong receptor affinity. It exhibits significant diuretic, analgesic, antiarrhythmic, antitussive, and neuroprotective activities, allowing it to effectively penetrate the blood-brain barrier. This compound is valuable for research applications focusing on pain management, addiction studies, and neuroprotection related to opioid activity. -
Opioid Receptor Modulator
Mitragynine pseudoindoxyl functions primarily as a μ-opioid receptor agonist with a Ki of 0.8 nM, while also acting as an antagonist at the δ-opioid receptor (Ki=3.0 nM). This compound exhibits moderate affinity for the κ-opioid receptor (Ki=24 nM) and operates through G protein-mediated signaling without β-arrestin-2 recruitment. Characterized by significant analgesic effects via a mixed μ-agonist/δ-antagonist mechanism, Mitragynine pseudoindoxyl demonstrates a reduced risk of common opioid side effects such as respiratory depression and dependency. Its potential applications include the management of hyperactivity and gastrointestinal transit inhibition, making it a candidate for therapeutic pain relief. -
Opioid Receptor Antagonist
Axelopran sulfate is a potent opioid receptor antagonist, exhibiting pKi values of 9.8, 8.8, and 9.9 for human recombinant μ and δ opioid receptors, as well as the guinea pig κ receptor. This compound is valuable for research focused on opioid signaling mechanisms and may aid in the investigation of pain management and addiction pathways. Its activity makes it a useful tool for elucidating the role of opioid receptors in various biological processes. -
Opioid Receptor Antagonist
LY255582 is a pan-opioid receptor antagonist, exhibiting high affinity for mu, delta, and kappa opioid receptors (Ki values of 0.4 nM, 5.2 nM, and 2.0 nM, respectively). This compound has been shown to reduce food intake and body weight, making it a valuable tool in obesity research. Its role in modulating opioid receptor activity offers potential insights into the mechanisms underlying appetite regulation and weight management. -
μ Opioid Receptor Modulator
BMS-986121 is a positive allosteric modulator of the μ opioid receptor, derived from innovative chemical scaffolds that represent a novel chemotype for this receptor. This compound enhances receptor activity and has potential applications in pain management research and the development of alternative analgesics. BMS-986121 is valuable for studies focused on the modulation of mu opioid receptor signaling pathways. -
Opioid Receptor Ligand
R-6890 is an opioid receptor ligand that acts as a selective antagonist, displaying significant binding affinity to rat opioid receptors with an IC50 of 4.6 nM in Tris buffer at pH 7.4. Its ability to displace radiolabeled opioids from receptors is notable, although its binding affinity is influenced by environmental conditions, particularly sodium chloride concentrations. R-6890 effectively crosses the blood-brain barrier and demonstrates analgesic properties in the warm water-induced tail-flick reflex assay in male Wistar rats, making it a valuable tool for research into pain mechanisms and opioid pharmacology. -
Opioid Receptor Agonist
Gluten Exorphin B5 is an opioid receptor agonist derived from wheat gluten. This peptide exhibits significant biological activity by enhancing postprandial plasma insulin levels in rodent models. It is used in research to investigate the role of opioid systems in metabolic processes and their potential implications for insulin regulation. -
κ-Opioid Receptor Antagonist
DIPPA hydrochloride is a selective, irreversible antagonist of the κ-opioid receptor, known for its high affinity and long-lasting effects. This compound demonstrates significant potential in research focused on anxiety and depression, facilitating investigations into its underlying mechanisms and therapeutic applications. Its unique pharmacological profile makes DIPPA hydrochloride a valuable tool for exploring the role of κ-opioid receptors in various neuropsychiatric conditions. -
δ-Opioid Receptor Agonist
Dalargin is a potent δ-opioid receptor agonist that exhibits significant biological activities, including nephroprotection. It mitigates cell death induced by gentamicin, thereby demonstrating protective effects against gentamicin-induced kidney injury. Additionally, Dalargin has shown antiulcer activity, making it a valuable compound for research applications in nephrology and gastrointestinal studies. -
Opioid Receptor Antagonist
Alvimopan metabolite hydrochloride is a peripherally selective opioid receptor antagonist that effectively reduces the amplitude of electrically induced contractions and spontaneous mechanical activity in guinea pig ileum. This compound is valuable for research applications investigating gastrointestinal motility and the pharmacological modulation of opioid receptors. Its ability to specifically target peripheral opioid receptors makes it a useful tool in studies related to pain management and gastrointestinal function. -
δ-Opioid Receptor Agonist
Deltorphin 2 is a selective agonist of the δ-opioid receptor, known for its potent biological activity in modulating pain and sensory perception. Its mechanism of action involves the activation of δ-opioid receptors, leading to analgesic effects. This compound is widely utilized in research applications focusing on pain management, neurobiology, and the exploration of opioid receptor signaling pathways. -
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.
