Catalog No.
Product Name
Application
Product Information
Citations
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κ-opioid agonists
ICI-204448 is a κ-opioid receptor agonist that demonstrates limited central nervous system penetration. This compound effectively displaces the binding of the κ-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes. It is valuable for research applications focused on the role of κ-opioid receptors in pain modulation and neuropharmacology studies. -
NOP/OP4 Receptor Agonist
Orphanin FQ(1-11) is a potent agonist of the NOP (nociceptin/orphanin FQ peptide) receptor, with a Ki value of 55 nM. This fragment exhibits selective activity, showing no affinity for μ, δ, κ1, or κ3 opioid receptors (Ki > 1000 nM). Orphanin FQ(1-11) has demonstrated analgesic effects in CD-1 mouse models, making it a valuable tool for studying pain modulation and the nociceptin system in various research applications. -
μ Opioid Receptor Agonist
Loperamide is a selective μ opioid receptor agonist with Ki values of 3, 48, and 1156 nM for μ, δ, and κ opioid receptors, respectively. It demonstrates significant antinociceptive and antihyperalgesic properties, along with peripheral selectivity that enhances fluid, electrolyte, and glucose absorption. Loperamide effectively mitigates intestinal secretion induced by PGE2 and cholera toxin while reducing intestinal motility. This compound is applicable in research focused on inflammatory pain and chronic diarrhea. -
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. -
NOP Receptor Antagonist
LY2940094 tartrate is a potent and selective antagonist of the nociceptin/orphanin FQ (NOP) receptor, characterized by a high binding affinity (Ki=0.105 nM) and effective antagonistic potency (Kb=0.166 nM). This compound exhibits significant brain penetration and is orally bioavailable, making it suitable for in vivo studies. LY2940094 tartrate has demonstrated efficacy in reducing ethanol self-administration and seeking behaviors in animal models, providing valuable insights for research in addiction and neuropharmacology. -
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. -
Tramadol Active Metabolite
O-Desmethyltramadol hydrochloride is the primary active metabolite of tramadol, functioning primarily by activating the µ-opioid receptor (µ-OR). This compound effectively crosses the blood-brain barrier, contributing to its significant analgesic properties. O-Desmethyltramadol is utilized in various research applications focused on pain management and opioid pharmacology. -
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. -
KOPr Agonist
Salvinorin A is a selective kappa-opioid receptor (KOPr) agonist with a Ki value of 4.3 nM, demonstrating significant potency and a unique non-nitrogenous neoclerodane structure. Isolated from Salvia divinorum, this compound exhibits marked biological activity, making it valuable for research on pain modulation, addiction, and the neuropharmacology of opioids. Salvinorin A serves as an important tool for investigating the effects of KOPr activation in various biological systems. -
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. -
DOR Agonist
DPDPE TFA is a selective δ-opioid receptor (DOR) agonist known for its anticonvulsant activity. This compound is utilized in research focusing on pain relief and neuroprotection, making it valuable in the study of opioid signaling pathways and related neurological disorders. DPDPE TFA provides a potent tool for investigating the physiological and therapeutic roles of δ-opioid receptors in various biological contexts. -
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. -
KOR Antagonist
ML 190 is a selective antagonist of the κ opioid receptor (KOR), exhibiting an IC50 of 120 nM. As a KOR antagonist, ML 190 plays a crucial role in the investigation of pain modulation, mood disorders, and addiction. This compound is valuable for research in exploring the physiological and pharmacological roles of KOR in various biological settings. -
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. -
KOR Agonist
(1R,2R)-U-50488 hydrochloride is a selective κ-opioid receptor (KOR) agonist. This compound exhibits potent activity at KOR, contributing to its potential therapeutic applications in pain management and neuromodulation research. Its distinct stereochemistry may provide valuable insights into the structure-activity relationships within opioid pharmacology. -
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-SAM
BMS-986124 is a μ-opioid receptor silent allosteric modulator (μ-SAM) that functions by inhibiting the positive allosteric modulation exerted by BMS-986122, a μ-opioid receptor positive allosteric modulator (PAM). This compound is valuable for studying the modulation of μ-opioid receptor signaling pathways and offers insights into the development of therapeutics for pain management and addiction. Its unique mechanism makes it a useful tool in research applications focused on opioid receptor biology and pharmacology. -
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. -
β-Casomorphin Fragment
β-Casomorphin (1-5), bovine is a peptide derived from bovine β-Casomorphin, acting primarily as an opioid receptor agonist. This fragment exhibits significant affinity for the mu-opioid receptor, contributing to its analgesic and anti-stress properties. It is commonly utilized in research exploring opioid signaling pathways, pain modulation, and the physiological effects of milk-derived peptides. -
Tramadol Active Metabolite
O-Desmethyltramadol is the primary active metabolite of tramadol, known for its ability to penetrate the blood-brain barrier. This compound primarily activates the µ-opioid receptor (µ-OR), contributing to its potent analgesic effects. O-Desmethyltramadol is utilized in research for its insights into pain modulation and the pharmacological mechanisms underlying opioid action. -
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. -
MOR Antagonist
Cyprodime is a selective μ opioid receptor (MOR) antagonist with a Ki value of 5.4 nM for MOR, and significantly lower affinities for δ and κ receptors, measuring 244.6 nM and 2187 nM, respectively. This compound is primarily utilized in research to investigate the role of MOR in pain modulation, addiction studies, and the exploration of opioid receptor pathways. Cyprodime serves as a valuable tool in pharmacological studies aimed at understanding the nuances of opioid receptor signaling. -
MOR Agonist/σ1R Antagonist
EST73502 monohydrochloride acts as a selective μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, exhibiting Kis of 64 nM and 118 nM for each target, respectively. This compound is orally bioavailable and can effectively cross the blood-brain barrier. EST73502 demonstrates notable antinociceptive properties, making it a valuable tool for research into pain modulation and neurobiology. -
Analgesic Agent
Axomadol is a centrally acting analgesic agent that exhibits opioid agonistic properties while also inhibiting the reuptake of monoamines. It demonstrates significant analgesic activity, making it a valuable compound for research focused on pain management and the mechanisms underlying pain perception. Axomadol can be utilized in studies aimed at exploring novel therapeutic approaches for analgesia and related neurological conditions. -
ORL1 Agonist
NNC 63-0532 is a selective non-peptide agonist of the nociceptin receptor (ORL1), exhibiting an EC50 of 305 nM. This compound has demonstrated significant biological activity in modulating pain pathways and may provide insights into the mechanisms of drug addiction. NNC 63-0532 serves as a valuable tool for research into the therapeutic potential of ORL1 modulation in various neurological and behavioral disorders. -
KOPR Antagonist
LY2444296 is a selective, orally bioavailable kappa opioid receptor (KOPR) antagonist, characterized by a high binding affinity with a Ki value of approximately 1 nM. This compound is noted for its potential to produce anti-anxiety-like effects, making it a valuable tool in the study of anxiety-related disorders and the role of KOPR in neuropsychiatric research. -
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. -
Nociceptin/Orphanin FQ-Receptor Selective Agonist
(S)-MCOPPB is a selective agonist of the Nociceptin/Orphanin FQ-Receptor (NOP). This compound is orally active and has been shown to inhibit signaling through the NOP receptor in the mouse brain. (S)-MCOPPB is primarily utilized in research focused on anxiety disorders, providing insights into the NOP receptor's role in anxiety modulation. -
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. -
DOR Agonist
JNJ-20788560 is a selective, orally active agonist of the delta opioid receptor (DOR) with a high affinity of 2.0 nM, as demonstrated in rat brain cortex binding assays. This compound exhibits potent antihyperalgesic properties and is notable for its lack of respiratory depression, pharmacologic tolerance, and physical dependence. JNJ-20788560 is suitable for research applications focused on the mechanisms underlying inflammatory hyperalgesia and pain relief strategies. -
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.
