Catalog No.
Product Name
Application
Product Information
Citations
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Opioid Receptor Antagonist
Naltrexone is a long-acting antagonist of opioid receptors, including μ, κ, and δ subtypes. It effectively blocks the euphoric effects of exogenous opioids and diminishes alcohol cravings by antagonizing these receptors. Clinically, low doses of Naltrexone are utilized for chronic pain management, the treatment of inflammatory conditions, and potentially inhibiting tumor growth. Additionally, it is employed to alleviate intractable pruritus associated with psoriasis and atopic dermatitis, while its combination with Bupropion may contribute to reduced food cravings and body weight management. -
δ-opioid Receptor Agonist
SNC80 is a highly selective and potent non-peptide δ-opioid receptor agonist, demonstrating a Ki of 1.78 nM and an IC50 of 2.73 nM. This compound selectively activates the μ-δ heteromer in HEK293 cells, exhibiting an EC50 of 52.8 nM. SNC80 is characterized by its antinociceptive, antihyperalgesic, and antidepressant-like activities, making it a valuable tool for research in the treatment of various headache disorders. -
DOR Agonist
DPDPE is a selective δ-opioid receptor (DOR) agonist known for its anticonvulsant properties. This opioid peptide is utilized in research to explore its potential therapeutic effects in pain management and seizure disorders. Its specificity for DORs makes DPDPE a valuable tool for investigating opioid receptor signaling pathways and their implications in neurological studies. -
μ-Opioid Receptor Agonist
Endomorphin 1 is a selective agonist of the μ-opioid receptor, exhibiting a high affinity with a Ki value of 1.11 nM. It also shows moderate affinities for kappa3 binding sites, with Ki values ranging from 20 to 30 nM. This compound is known for its antinociceptive properties, making it relevant for research focused on pain modulation and opioid receptor signaling pathways. -
μ-opioid Receptor Antagonist
Naldemedine tosylate is a selective μ-opioid receptor antagonist, classified as a peripherally acting mu-opioid receptor antagonist (PAMORA). It exhibits high binding affinities for human μ-, δ-, and κ-opioid receptors, making it a valuable reagent for studying opioid-related pathways. Its primary application includes research on opioid-induced constipation (OIC). Additionally, Naldemedine tosylate has the potential to interact with the 3CLpro protease encoded by the SARS-CoV2 genome, suggesting further avenues for investigation in viral studies. -
Kappa-opioid Receptor Antagonist
Nor-Binaltorphimine is a selective antagonist of the kappa-opioid receptor, known for its role in modulating nociception and mood regulation. This compound exhibits prolonged effects in vivo, making it a valuable tool in research related to pain management, addiction, and psychiatric disorders. Its specificity for kappa-opioid receptors supports studies focused on understanding their physiological and pathological roles. -
KOR Agonist
(-)-U-50488 hydrochloride is a selective agonist of the kappa-opioid receptor (KOR), exhibiting a binding affinity (Kd) of 2.2 nM, significantly higher than its affinity for the μ-opioid receptor (MOR) at 430 nM. This compound serves as a more active enantiomer compared to its (+) counterpart and the racemic mixture. In research applications, (-)-U-50488 hydrochloride demonstrates potent and sustained anti-HIV activity in infected blood monocyte-derived macrophages (MDM), making it a valuable tool for studying kappa-opioid receptor functions and their therapeutic potential in HIV-related research. -
µ-Opioid Receptor Positive Allosteric Modulator
BMS-986122 is a selective positive allosteric modulator of the mu-opioid receptor (µ-OR) that enhances the activity of orthosteric agonists. This compound effectively increases β-arrestin recruitment, inhibits adenylyl cyclase, and activates G protein signaling pathways. BMS-986122 demonstrates the ability to potentiate DAMGO-mediated [35S]GTPγS binding in mouse brain membranes, making it a valuable tool for research in pain management and opioid pharmacology. -
Opioid Receptor Agonist
BW-180C, a δ opioid receptor (DOR) agonist, is a member of the enkephalin family. This compound exhibits neuroprotective properties and reversibly inhibits cellular transcription in neurons while preserving cell integrity. BW-180C is valuable for research applications focused on neuroprotection and opioid receptor signaling. -
Kappa Receptor Ligand
Dynorphin A (1-8) is a potent kappa receptor ligand, playing a critical role in opioid signaling. This peptide exhibits significant binding affinity, inhibiting the binding of 3H-Bremazocine to the purified kappa receptor with an IC50 of 303 nM. It serves as a valuable tool for studying kappa opiate pharmacology and exploring its implications in pain modulation and neurobiology. -
Opioid Receptor Antagonist
Naloxone methiodide is a peripherally restricted, nonselective competitive antagonist of opioid receptors. Its lack of ability to penetrate the blood-brain barrier allows for targeted effects in peripheral tissues. This compound is primarily used in research applications investigating opioid receptor activity and the modulation of peripheral opioid effects, making it valuable for studying pain management and opioid-related responses. -
ORL1 Receptor Antagonist
(±)-J-113397 is a selective non-peptidyl antagonist of the ORL1 receptor, exhibiting a Ki value of 1.8 nM for cloned human ORL1. It effectively inhibits nociceptin/orphanin FQ-stimulated GTPγS binding in CHO cells expressing ORL1, with an IC50 of 5.3 nM. This compound is valuable for investigating the physiological roles and functions of the nociceptin/orphanin FQ system in various biological contexts. -
δ-opioid Receptor Agonist
SNC162 is a potent δ-opioid receptor agonist with an IC50 of 0.94 nM. This compound demonstrates significant antidepressant-like and antinociceptive properties, making it a valuable tool in the investigation of pain management and mood disorders. Its efficacy in modulating δ-opioid receptor activity supports research into therapeutic applications for treatment-resistant depression and chronic pain syndromes. -
KOR Agonist
(±)-U-50488 hydrochloride is a selective agonist of the κ opioid receptor (KOR). It exhibits significant analgesic and anti-inflammatory properties, making it valuable for studies related to pain management and opioid receptor signaling pathways. This compound is ideal for research applications investigating the role of KOR in various physiological processes and potential therapeutic interventions. -
δ-opioid Receptor Antagonist
TAN-452 is a selective, orally active δ-opioid receptor antagonist, exhibiting a Ki of 0.47 nM and a Kb of 0.21 nM. This reagent also shows antagonistic properties toward μ-opioid receptors, with a Ki of 36.56 nM, and κ-opioid receptors, with a Ki of 5.31 nM. TAN-452 is designed to attenuate morphine-induced side effects while maintaining analgesic efficacy, making it valuable for research in pain management and opioid-related studies. Its low brain penetrability further supports peripheral applications, minimizing central nervous system interactions. -
MOR Activator
(±)-Salsolinol hydrochloride is a potent μ-opioid receptor (MOR) activator derived from dopamine. This compound modulates neuronal activity by reducing GABAergic transmission and enhancing the excitability of dopamine neurons. Its effects on neuronal firing rates in the posterior ventral tegmental area (pVTA) make it valuable for research applications focused on opioid signaling and dopamine-related pathways. -
Morphine (μ) Receptor Agonist
Morphiceptin is a potent and selective agonist for the morphine (μ) receptors, exhibiting significant morphine-like activity. This synthetic peptide, derived from a fragment of the milk protein β-casein, possesses high specificity for μ receptors while showing minimal interaction with enkephalin receptors. Morphiceptin is primarily utilized in research focused on pain management and opioid receptor signaling pathways, providing valuable insights into receptor pharmacology. -
Mu-opioid Receptor Antagonist
Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with a reported IC50 of 5.4 nM. This compound not only inhibits μ-opioid receptor activity but also demonstrates anti-leishmanial properties, making it relevant for studies on pain management and parasitic infections. Its unique profile supports research applications in opioid receptor modulation and leishmaniasis treatment development. -
κ-opioid Agonist
CR 665 is a peripherally selective κ-opioid agonist that targets the kappa opioid receptor, exhibiting an EC50 value of 10.9 nM. This compound is primarily utilized in research focused on peripheral pain mechanisms, making it a valuable tool for studying pain modulation and analgesic pathways. Its selective action offers potential for exploring new analgesic therapies with reduced central side effects. -
Opioid Receptor Agonist
Adrenorphin is an opioid octapeptide that functions primarily as a potent agonist of the μ-opioid receptor, exhibiting a binding affinity with a Ki value of 12 nM. This compound is significant for its role in research related to pain modulation, addiction, and neuroprotection. Its properties make it an essential tool for studying opioid receptor dynamics and related biological pathways. -
ORL1 Receptor Antagonist
J-113397 is a potent and selective nonpeptidyl antagonist of the ORL1 receptor, exhibiting a binding affinity with a Ki of 1.8 nM for cloned human ORL1. This compound is notable for its lack of agonistic activity on other opioid receptors, making it a valuable tool for studying the physiological and pharmacological roles of the ORL1 receptor. J-113397 is applicable in research focused on pain modulation, addiction, and various neurodegenerative diseases. -
Opioid Receptor Antagonist
(+)–N-Allylnormetazocine hydrochloride is an opioid receptor antagonist targeting σ1 and σ2 receptors, exhibiting Ki values of 300 nM and 27 μM, respectively. This benzomorphan compound demonstrates psychotomimetic effects and is of particular interest in the study of neurological diseases. It serves as a valuable reagent for research into opioid receptor interactions and their implications in various neuropharmacological conditions. -
Opioid Receptor Modulator
Samidorphan is an opioid receptor modulator with a high affinity for μ-opioid, κ-opioid, and δ-opioid receptors. It functions as an antagonist at μ-opioid receptors while serving as a partial agonist at κ- and δ-opioid receptors. This unique profile allows Samidorphan to primarily act as an opioid antagonist in vivo, demonstrating potential for improving depressive behaviors in animal models. Its mechanistic action makes it a valuable tool for research in the fields of pain management, addiction, and mood disorders. -
Opioid Receptor Agonist
Ro 64-6198 is a selective nonpeptide agonist of the nociceptin/orphanin FQ peptide (NOP) receptor, exhibiting a high affinity with an EC50 value of 25.6 nM. It shows over 100-fold selectivity for the NOP receptor compared to classic opioid receptors. This compound is valuable for research applications related to stress, anxiety, addiction, neuropathic pain, cough modulation, and appetite regulation. -
κ-opioid Agonist
Asimadoline hydrochloride is a selective κ-opioid agonist that exhibits peripheral activity with IC50 values of 5.6 nM in guinea pig tissues and 1.2 nM in human recombinant assays. This compound has limited blood-brain barrier permeability, making it suitable for targeting peripheral anti-inflammatory pathways. Asimadoline hydrochloride has demonstrated effectiveness in alleviating allodynia in diabetic rat models and offers potential therapeutic applications in the treatment of irritable bowel syndrome (IBS). -
κ2 Opioid Receptor Agonist
GR 89696 is a selective κ2 opioid receptor agonist known for its ability to modulate pain and itch responses. This compound has demonstrated potential in preventing pruritus, making it a valuable tool for research in pain management and neurological disorders. Its specificity for the κ2 receptor may facilitate studies aimed at understanding opioid receptor pathways and developing therapeutic strategies for itch-related conditions. -
μ Opioid Receptor Antagonist
CTAP is a potent and highly selective μ opioid receptor antagonist, exhibiting an IC50 of 3.5 nM. It demonstrates over 1200-fold selectivity against δ opioid receptors (IC50 = 4500 nM) and somatostatin receptors. CTAP is valuable for research applications focusing on L-DOPA-induced dyskinesia, as well as studies related to opiate overdose and addiction mechanisms. -
NOP Agonist
SCH 221510 is a selective and potent nociceptin opioid receptor (NOP) agonist, demonstrating an EC50 of 12 nM and a Ki of 0.3 nM. This compound exhibits anxiolytic-like effects, making it valuable for research applications in anxiety and other neuropsychiatric disorders. Its orally active nature enhances its utility in preclinical studies targeting the NOP signaling pathway. -
κ-Opioid Receptor Agonist
ICI-199441 hydrochloride is a potent and selective κ-opioid receptor agonist that exhibits significant analgesic properties. This compound has been shown to enhance cardiac resistance to ischemia/reperfusion injury, making it valuable in studies related to cardiovascular protection and pain management. Its specific targeting of the κ-opioid receptor underscores its potential utility in research applications focusing on the modulation of pain pathways and ischemic heart conditions. -
Kappa Opioid Receptor Antagonist
5'-Guanidinonaltrindole hydrochloride is a potent and selective κ-opioid receptor antagonist, exhibiting a Ki of 0.18 nM for the human κ-opioid receptor. This compound is employed in research to explore the roles of κ-opioid receptors in pain modulation, mood disorders, and addiction pathways. Its high affinity makes it a valuable tool for studies investigating the pharmacological effects of κ-opioid receptor inhibition. -
Opioid Receptor Agonist
[Leu5]-Enkephalin, amide is a selective agonist of the δ-opioid receptor. This compound exhibits significant analgesic properties and is involved in modulating pain pathways. It is commonly used in research to study opioid receptor signaling and its implications in pain management and addiction. -
Opioid Receptor Agonist
BPR1M97 is a dual-acting agonist for the mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor, exhibiting Ki values of 1.8 nM and 4.2 nM, respectively. This compound demonstrates significant potency and effective penetration of the blood-brain barrier, resulting in pronounced antinociceptive effects. BPR1M97 serves as a useful tool for research in pain management and opioid receptor biology. -
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.
