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