Catalog No.
Product Name
Application
Product Information
Citations
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Opioid Receptor
Faxeladol is an opioid receptor modulator that exhibits significant analgesic activity. In clinical trials, it demonstrated a reduction in mean pain intensity in patients suffering from painful polyneuropathy, supporting its potential as an effective pain management agent. The compound is characterized by a favorable safety profile, making it a candidate for further research in pain relief applications. -
Opioid Receptor Antagonist
LY2048978 is a non-selective opioid receptor antagonist that exhibits Ki values of 0.287 nM, 0.471 nM, and 1.05 nM for human mu, kappa, and delta opioid receptors, respectively. This compound is relevant for studying the physiological roles of opioid receptors and is applied in research related to major depressive disorder and alcohol use disorder. Its antagonistic properties make it a valuable tool for investigating opioid-mediated pathways and potential therapeutic interventions. -
Opioid Agonist
D-Ala2-Met-Enkephalinamide is an opioid peptide that functions as a potent opioid agonist. It exerts analgesic effects and is known to decrease bile flow through central mechanisms. This compound is valuable in research applications focused on pain management and opioid receptor activity. -
Mu-Opioid Receptor Antagonist
Mu Opioid Receptor Antagonist 5 is a selective antagonist of the μ-opioid receptor (MOR) with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. This compound is capable of penetrating the blood-brain barrier, making it a valuable tool for studying the mechanisms underlying opioid use disorders (OUD). Its high potency and specificity for the MOR facilitate insightful research into opioid-related signaling pathways and potential therapeutic interventions. -
Opioid Peptide
Biphalin TFA is a potent opioid peptide analog designed for effective interaction with opioid receptors, demonstrating a dual enkephalin pharmacophore structure that facilitates blood-brain barrier penetration. This compound exhibits significant analgesic properties in various pain models, including acute, neuropathic, and chronic settings. Additionally, Biphalin TFA has been shown to possess antiviral, antiproliferative, anti-inflammatory, and neuroprotective activities, making it a valuable tool for research in pain management and related therapeutic areas. -
μ-Opioid Receptor Agonist
Perillyl acetate is a monoterpene that acts as an agonist at the μ-opioid receptor. It demonstrates significant analgesic properties, making it valuable for studying pain management. This compound is also relevant in research related to inflammation and neurological conditions such as arthritis. -
Opioid Receptor Agonist
BAM-22P is a highly potent opioid receptor agonist that selectively engages the mu-opioid receptor. It exhibits significant analgesic properties, making it a valuable tool for research on pain modulation and opioid signaling pathways. This compound is applicable in studies exploring opioid receptor pharmacodynamics and the development of pain therapies. -
AVP Release Inhibitor/Kappa Opioid Receptor Agonist
Niravoline is an arginine vasopressin (AVP) release inhibitor and a selective kappa opioid receptor agonist. This compound is notable for inducing a pure water diuresis effect while minimizing electrolyte loss. Additionally, Niravoline has demonstrated efficacy in reducing brain edema following transient forebrain ischemia in rodent models, making it a valuable tool for research in neuroprotection and fluid balance mechanisms. -
μ Opioid Receptor Agonist
μ Opioid Receptor Agonist 4 acts as a selective agonist for the μ-opioid receptor (MOP), effectively enhancing pain relief mechanisms. Demonstrating a potency 2300-fold higher than Meperidine, this compound exhibits significant analgesic properties in murine models. It is a valuable tool for researching pain management and opioid receptor-related pathways. -
δ Opioid Receptor Antagonist
Boc-YPGFL(O-tBu) is a selective antagonist of the δ opioid receptor (DOR), which plays a crucial role in modulating pain perception and emotional responses. This compound is of significant interest for research applications related to pain management and opioid receptor signaling pathways. Its ability to selectively inhibit DOR activity makes it a valuable tool in studying the pharmacological effects of opioid receptors and developing novel therapeutic agents. -
Opioid Receptor Agonist
CR 665 acetate is a selective kappa-opioid receptor agonist that targets opioid receptors to effectively manage visceral pain. By activating receptors on afferent nerves within the gut, CR 665 acetate enhances pain tolerance without the central nervous system effects typical of non-selective opioids. This compound is particularly useful in the context of postoperative pain management, offering a fast-acting analgesic alternative without the delayed response associated with other opioids. Its peripheral selectivity may provide significant advantages in pain relief while minimizing potential side effects. -
Mu-Opioid Receptor Antagonist
Mu opioid receptor antagonist 3 is a highly potent and selective antagonist of the μ opioid receptor (MOR), with a Ki value of 0.24 nM and an EC50 of 0.54 nM. This compound exhibits strong central nervous system antagonism against morphine and produces fewer withdrawal symptoms compared to traditional antagonists like Naloxone. Mu opioid receptor antagonist 3 is valuable for research applications focused on opioid use disorders (OUD) and studying the mechanisms of opioid dependence and withdrawal. -
Opioid Receptor Antagonist
CP-866087 is a selective antagonist of the mu-opioid receptor, primarily designed to investigate female sexual dysfunction. This compound demonstrates significant blocking activity, making it a valuable tool in the study of opioid-mediated signaling pathways and their effects on sexual health. Its specificity for the mu-opioid receptor supports research aimed at understanding the implications of opioid interactions in reproductive biology and therapeutic interventions. -
Opioid Receptor Agonist
[Dmt1]DALDA is a potent mu-opioid receptor agonist known for its long-acting analgesic properties. It exhibits high affinity and selectivity for the human mu-opioid receptor (hMOR) with a Kd value of 0.199 nM, and acts as a full agonist at both hMOR and human delta-opioid receptor (hDOR), while functioning as a partial agonist at the human kappa-opioid receptor (hKOR). This compound is valuable in pain management research and studies focused on opioid receptor signaling pathways. -
Opioid Receptor Agonist
ADL5859 is a selective and orally active δ-opioid receptor (DOR) agonist, exhibiting a Ki of 0.84 nM and an EC50 value of 20 nM. In addition, it demonstrates inhibitory activity on the hERG channel with an IC50 of 78 μM. This compound is primarily utilized in pain research, providing insight into opioid receptor mechanisms and potential therapeutic applications. -
Opioid Receptor Agonist
(Rac)-Enadoline is a selective K-opioid receptor agonist known for its ability to modulate opioid pathways. It has been shown to stereoselectively antagonize clonic seizures induced by the administration of N-methyl-DL-aspartate in murine models. This compound serves as a valuable research tool for studying K-opioid receptor function and potential therapeutic applications in seizure disorders and other neurological conditions. -
Opioid Receptors Agonist
Anilopam is an opioid analgesic that acts as an agonist at opioid receptors, specifically within the benzazepine class. This compound is utilized in research to study pain management and the modulation of opioid receptor activity. Its key biological activity involves providing analgesic effects, making it relevant for investigations into pain pathways and therapeutic approaches in pain relief. -
Nociception/Mu opioid receptor Agonist
AT-121 hydrochloride is a bifunctional mu opioid receptor agonist that targets nociception with Kis of 3.67 nM and 16.49 nM, respectively. This compound demonstrates significant antinociceptive and antiallodynic effects, representing a promising non-addictive analgesic option for pain management. It is suitable for research applications focused on pain modulation and opioid receptor dynamics. -
μ-opioid receptor Agonist
Bilaid A is a μ-opioid receptor agonist derived from Penicillium, exhibiting a Ki value of 3.1 μM. This compound demonstrates significant biological activity in modulating opioid receptor signaling and is applicable in pain research focused on opioid pharmacology. Its potential use in investigations of analgesic pathways may contribute to the development of novel pain management therapies. -
Opioid Receptor Inhibitor
Neuropeptide AF (human) is an endogenous peptide that acts as an opioid receptor inhibitor. This neuropeptide plays a critical role in modulating pain and stress responses, making it a valuable tool for studies focused on opioid signaling pathways. Research applications include investigations into pain management, addiction, and the physiological effects of endogenous opioid peptides. -
Opioid Receptor Agonist
Alimadol is an orally active opioid receptor agonist that exhibits significant analgesic properties. This compound is primarily utilized in research focused on pain management and the mechanisms of opioid action. Its ability to selectively activate opioid receptors makes it a valuable tool for studying pain signaling pathways and potential therapeutic interventions. -
Opioid Receptor Activator
Bromadoline maleate is a selective activator of the μ-opioid receptor, demonstrating potent analgesic activity across diverse biological matrices. This compound is effective for pain management studies and has been successfully quantified alongside its N-demethylated metabolites in both human and canine biological samples, making it a valuable tool for pharmaceutical research and opioid pharmacokinetics. -
Mu-Opioid Agonist
Loxicodegol is a selective mu-opioid agonist with unique structural features that enhance its long-acting, orally active profile while limiting its penetration across the blood-brain barrier relative to conventional mu-opioid agonists. This compound demonstrates significant potential for pain management applications, providing an innovative approach to opioid therapy with reduced central nervous system side effects. Its pharmacological properties make it a valuable tool for research into opioid-related analgesic mechanisms and the assessment of therapeutic strategies in chronic pain conditions. -
Opioid Receptor Activator
Ro-48-6791 is an opioid receptor activator that functions by binding to and activating opioid receptors. This compound is known to enhance physiological effects associated with opioid signaling, potentially influencing both therapeutic and adverse outcomes. Research applications include studying opioid receptor-mediated pathways and exploring the pharmacological effects of opioid agonists. -
Mu-Opioid Receptor Antagonist
Mu Opioid Receptor Antagonist 2 is a highly potent and selective antagonist of the μ opioid receptor (MOR), exhibiting a Ki of 0.37 nM and an EC50 of 0.44 nM. This compound effectively penetrates the blood-brain barrier and demonstrates strong central nervous system antagonism against morphine, inducing fewer withdrawal symptoms compared to traditional remedies. Mu Opioid Receptor Antagonist 2 is valuable for research focused on opioid use disorders (OUD), enabling a better understanding of opioid dependency and potential therapeutic interventions. -
δ-Opioid Receptor Analog
[DPen2, Pen5] Enkephalin is a selective analog of [Leu5]-Enkephalin that targets the δ-opioid receptor. This compound exhibits potent analgesic properties and is utilized in research focused on pain management and the pharmacological modulation of opioid pathways. Its specificity for the δ-opioid receptor makes it a valuable tool for investigating the role of this receptor in various physiological and pathological processes. -
Opioid Receptor Antagonist
Diallyl G is an antagonist of the delta-opioid receptor, exerting its effects by inhibiting GTPase activity. This compound is valuable for research applications focused on elucidating the role of delta-opioid receptors in pain modulation, substance use disorders, and neuropharmacology. Its antagonistic properties make it useful for studying receptor signaling pathways and the physiological impact of opioid receptor modulation. -
κ Opioid Receptor Agonist
ML138 is a selective κ-opioid receptor agonist that serves as a probe for understanding κ-opioid receptor biology. This compound has been shown to modulate pain responses and may play a role in the development of treatments for mood disorders and addiction. Its ability to selectively activate κ-opioid receptors makes it a valuable tool for research in neuropharmacology and related fields. -
Opioid Analog
Phenethyl 4-ANPP is a selective agonist of the μ-opioid receptor (MOR). This compound serves as an analytical reference standard due to its structural similarity to various known opioids. It is primarily utilized in research applications related to opioid pharmacology and receptor signaling studies, contributing to the understanding of opioid mechanisms and potential therapeutic avenues. -
Kappa Opioid Receptor Agonist
Anrikefon (HSK21542) is a potent kappa opioid receptor agonist that facilitates analgesic effects through modulation of pain pathways. This compound has been utilized in research to explore its potential therapeutic applications in pain management and opioid-related disorders. Its selective action on the kappa receptor makes it a valuable tool for studies investigating receptor-specific mechanisms in pain modulation. -
μ-Opioid Receptor Agonist
FK 33-824 is a synthetic analogue of Met-enkephalin that serves as a selective agonist of the μ-opioid receptor (μ-OR). This compound is utilized in research to explore pain modulation and the mechanisms underlying opioid receptor signaling. Its targeted activity positions it as a valuable tool in studies related to analgesia and opioid receptor pharmacology. -
μ/δ Opioid Receptor Agonist
Amdakefalin is a potent agonist of the μ and δ opioid receptors, exhibiting notable analgesic properties. Its mechanism of action involves the modulation of pain pathways, making it a valuable tool for research into pain management and opioid pharmacology. Amdakefalin serves as a promising candidate for investigating therapeutic interventions for various pain-related conditions. -
Opioid Receptor Antagonist
LY-99335 is an opioid receptor antagonist that demonstrates behavioral inhibitory activity. This compound exhibits significant dose separation at specific concentrations, highlighting its potential utility in anesthetic antagonism. LY-99335 can be used for research applications related to pain management and the modulation of opioid receptor activity. -
Opioid Receptor Binding Compound
3-Carboxamidonaltrexone is a potent opioid receptor binding compound that exhibits Ki values of 1.9 nM for the μ-opioid receptor, 110 nM for the δ-opioid receptor, and 22 nM for the K-opioid receptor. This compound serves as a valuable tool for studying opioid receptor interactions and is applicable in research exploring pain modulation, addiction, and opioid receptor pharmacology. Its selective binding affinities make it suitable for investigating diverse biological pathways associated with opioid signaling. -
μ-Opioid Receptor Agoinst/AChE Inhibitor
Eseroline is a potent μ-opioid receptor agonist and a selective, competitive inhibitor of acetylcholinesterase (AChE), with Ki values of 0.1 μM for AChE and 200 μM for butyrylcholinesterase (BuChE). This compound also acts as a nicotinic acetylcholine receptor allosteric enhancing ligand, enhancing acetylcholine signal transduction without directly activating the receptor. Eseroline's neurotoxic effects include cell membrane damage and energy metabolism disruption, making it a valuable tool for investigating Alzheimer's disease pathology and cholinergic signaling. -
Opioid Peptide Derivative
[DAla2, DArg6] Dynorphin A (1-13) (porcine) is a modified opioid peptide targeting opioid receptors in the peripheral nervous system. This derivative exhibits enhanced stability compared to its parent compound, dynorphin (1-13), demonstrating increased resistance to enzymatic degradation. Its unique properties make it a valuable tool for studying opioid receptor signaling and evaluating potential therapeutic applications in pain management and neuropharmacology. -
Opioid Receptor Antagonist
Opioid Receptor Antagonist 2 is a potent antagonist targeting opioid receptors, providing a crucial research tool in the study of opioid pharmacology. This compound effectively reverses ventilatory depression and vocal cord closure induced by fentanyl analogs in murine models. Its properties make it a valuable candidate for investigating acute poisoning scenarios, particularly those involving respiratory depression due to opioid overdose. -
Opioid Receptor Agonist
[Met5]-Enkephalin, amide is a potent agonist targeting δ opioid receptors and putative ζ opioid receptors. This compound is critical for studying pain modulation and the role of endogenous opioids in various physiological processes. Its applications extend to research on neurobiology, pain management, and the development of opioid-based therapeutics. -
NOP/μ-opioid Receptor Agonist
SR-16434 is a partial agonist of the nociceptin/orphanin FQ (NOP) and μ-opioid receptors, exhibiting high binding affinity with Ki values of 7.49 for the NOP receptor and 2.70 for the μ-opioid receptor. This compound demonstrates significant analgesic properties, making it a valuable tool for studying pain mechanisms and developing new pain management strategies. Its dual receptor activity provides insights into the interplay between nociceptive and opioid signaling pathways in research applications. -
δ-Opioid Receptor Agonist
AZD-2327 is a potent and selective agonist of the δ-opioid receptor. It demonstrates high affinity with Ki values of 0.49 nM and 0.75 nM for the C27 and F27 isoforms, respectively, and effective concentration EC50 values of 24 nM and 9.2 nM. AZD-2327 is more than 1000-fold selective over human μ- and κ-opioid receptor subtypes, as well as over 130 other receptors and channels. This compound exhibits notable antidepressant and anxiolytic properties, making it valuable for research in neurological disorders. -
κ-Opioid Receptor Agonist
CJ-15161 is a κ-opioid receptor agonist, primarily involved in modulating pain perception and emotional responses. This compound serves as a valuable tool for investigating the physiological functions associated with κ-opioid receptor activation, including analgesia and the regulation of mood. Its use in research contributes to a deeper understanding of opioid receptor pathways and their implications in pain management and mental health disorders. -
Opioid Receptor Antagonist
PF-4455242 hydrochloride is a selective antagonist of the κ-opioid receptor, known for its potential analgesic properties. This compound was developed using a strategy that combines parallel chemistry and physicochemical property design. PF-4455242 hydrochloride has shown confirmed potency and selectivity in preclinical models such as the tail-flick analgesia test, making it a valuable tool for research into pain mechanisms and opioid receptor interactions. -
δ2 Opioid Receptor Antagonist
N-Benzylnaltrindole hydrochloride is a potent and selective antagonist of the δ2 opioid receptor. It exhibits a longer duration of action in vivo compared to Naltriben (NTB), making it valuable for studies involving the δ-opioid receptor. This compound serves as an important reagent for the pharmacologic characterization of δ-opioid receptor function, facilitating research in pain management and opioid signaling pathways. -
Opioid Receptor Agonist
TAN-67 is a non-peptidic agonist of the delta-opioid receptor, demonstrating significant antinociceptive activity in both diabetic and non-diabetic mouse models. It effectively reduces acetic acid-induced abdominal constrictions in a dose-dependent manner, exhibiting a stronger response in diabetic mice. The analgesic properties of TAN-67 are primarily mediated through the activation of delta 1-opioid receptors, as evidenced by the pronounced antagonism when a selective delta 1-opioid receptor antagonist is administered. This compound is useful for research into pain mechanisms and the potential therapeutic applications of delta-opioid receptor modulation. -
μ-opioid Receptor Antagonist
Cyprodime hydrochloride is a selective μ-opioid receptor antagonist, demonstrating a Ki value of 5.4 nM for the μ-opioid receptor while exhibiting considerably lower affinities for δ- and κ-opioid receptors (244.6 nM and 2187 nM, respectively). This compound has been shown to produce anti-depressant-like effects, making it a valuable tool for investigating the roles of opioid receptors in mood disorders and other neuropharmacological research applications. -
Opioid Agonist
β-Lipotropin (61-69) is a potent opioid agonist that selectively binds to opioid receptors, exerting significant analgesic effects. This peptide demonstrates key biological activities relevant to pain management and neurobiology research. Its application in studying opioid receptor signaling pathways makes it a valuable reagent for exploring the mechanisms of pain modulation and addiction. -
Opioid Receptor Agonist
Dynorphin A (1-10) is an endogenous opioid neuropeptide that acts as an agonist at the κ-opioid receptor, specifically binding to extracellular loop 2. Its biological activity includes the modulation of pain pathways and effects on mood regulation. Additionally, Dynorphin A (1-10) inhibits NMDA receptor-activated currents with an IC50 of 42.0 μM, making it a valuable tool for research into pain, addiction, and neuroprotection. This peptide is essential for studying opioid receptor dynamics and their implications in neurological disorders. -
Opioid Receptor Agonist
Herkinorin is a potent and selective agonist of the µ-opioid receptor, exhibiting a Ki value of 45 nM. This compound is primarily utilized in research focused on pain modulation and the mechanisms of opioid receptor activation. Its specificity for the µ-opioid receptor makes it a valuable tool for studying pain pathways and evaluating potential therapeutic interventions in pain management. -
Mu Opioid Receptor Ligand
Mu Opioid Receptor Antagonist 1 is a selective and orally active ligand that targets the mu opioid receptor (MOR), exhibiting a Ki value of 0.58 nM and an EC50 of 1.15 nM. This compound effectively enhances intestinal motility in models of morphine-induced constipation. It serves as a valuable tool for research focused on opioid-induced constipation (OIC) and its related gastrointestinal effects. -
κ-Opioid Receptor Agonist
K-Opioid receptor agonist-1 is a potent agonist of the κ-opioid receptor, with a binding affinity (Ki) of 0.25 nM and an effective concentration (EC50) of 2 nM. This compound effectively crosses the blood-brain barrier, demonstrating brain/plasma ratios between 0.50 and 0.65. K-Opioid receptor agonist-1 shows significant anti-inflammatory properties in various dermatitis models, including those induced by arachidonic acid and oxazolidinone, making it a valuable tool for studying pain modulation and inflammation pathways.
