Catalog No.
Product Name
Application
Product Information
Citations
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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. -
MOR Receptor Agonist
μ Opioid Receptor Agonist 1 (Compound H-1a) is an optically pure oxaspiro ring-substituted pyrrolopyrazole derivative that selectively targets the μ-opioid receptor (MOR). This compound exhibits significant agonistic activity, making it a valuable tool for investigating pain mechanisms and the pharmacological effects related to pain management and associated disorders. Its specificity towards the MOR facilitates research applications in analgesic development and opioid receptor signaling pathways. -
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. -
Opiate δ-receptor Agonist
D-Ala-Gly-Phe-Met-NH2 is a potent agonist of the opioid δ-receptor, functioning primarily through its interaction with opioid receptors. This compound exhibits significant biological activity, making it a valuable tool in the study of pain modulation and opioid pharmacology. Its utility extends to research applications exploring the mechanisms of addiction, analgesia, and the development of novel therapeutic agents targeting opioid receptors. -
KOR Agonist
(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) functions as a potent kappa opioid receptor (KOR) agonist. This stable analog of Dynorphin A (1-8) exhibits significant biological activity in modulating pain and stress response pathways. Its application in research extends to studying opioid system dynamics and potential therapeutic strategies in pain management and neurobiology. -
Analgesic
DDD-028 is a potent non-opioid, non-cannabinoid analgesic that targets pain pathways to alleviate neuropathic and inflammatory pain. Its mechanism minimizes the risk of side effects and abuse commonly associated with traditional opioid or cannabinoid treatments. DDD-028 is suitable for research applications focused on developing alternative analgesic 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. -
Opiate δ-receptor Agonist
D-Ala-Gly-Phe-Met-NH2 monoacetate is a potent agonist of the opioid δ-receptor. This synthetic peptide demonstrates notable analgesic properties, making it valuable for research on pain management and the modulation of opioid signaling pathways. Its specific action on δ-receptors positions it as an important tool for investigating opioid receptor pharmacology and developing targeted therapeutic strategies. -
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. -
μOR Agonist/σ1R Antagonist
σ1 Receptor/μ Opioid receptor modulator 2 is a dual μ-opioid receptor (μOR) agonist and σ1 receptor (σ1R) antagonist. It demonstrates potent μOR agonistic activity with an EC50 value of 0.6 ± 0.2 nM and effective σ1R inhibitory activity at a Ki of 363.7 ± 5.6 nM. This compound exhibits significant analgesic effects in multiple preclinical pain models, making it a valuable tool for research in pain management and opioid receptor pharmacology. -
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. -
MOR Agonist
AP-238 is a synthetic opioid that primarily targets the μ-opioid receptor (MOR), exhibiting an EC50 value of 248 nM. This compound demonstrates significant analgesic properties, making it relevant for research focused on pain management and opioid receptor pharmacology. Its ability to activate MOR positions AP-238 as a valuable tool for studying the effects of opioids in various biological contexts. -
ORL-1 Receptor Modulator
6-Fluoro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole is an ORL-1 receptor modulator that influences signaling pathways associated with nociception, cognition, and various physiological processes. This compound is valuable for investigating central nervous system disorders and pain-related conditions, including anxiety, depression, Alzheimer's disease, and attention deficit disorder. Its effects on the ORL-1 receptor make it an essential tool for researchers studying these complex biological processes. -
Dynorphin
Daeatal (Dynorphin A ethylamide (1-9)) functions as a selective agonist for kappa opioid receptors (KOR) and is involved in key neurobiological processes. This modified dynorphin fragment is utilized in research applications focusing on analgesia, addiction, and depression. Additionally, Daeatal’s actions at other opioid receptors, including mu (MOR) and delta (DOR), make it relevant for studying neurodegenerative diseases and neuronal apoptosis. -
Gβγ-subunit Inhibitor
M119 (NSC 119910) is a selective Gβγ-subunit inhibitor that modulates μ-opioid receptor signaling. This compound has been shown to enhance μ-opioid-dependent antinociception by inhibiting μ-receptor-dependent phospholipase (PLC) activation. M119 is useful in pain research, particularly in studies investigating opioid analgesia, as well as in the assessment of acute tolerance and dependence in animal models. -
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. -
KOR Agonist
KOR Agonist 2 (Compound 23p) is a potent agonist of the κ-opioid receptor (KOR) with a Ki value of 1.9 nM. It demonstrates significant analgesic properties in mouse models, exhibiting an effective dose (ED50) of 1.30 mg/kg. Additionally, KOR Agonist 2 shows a high clearance rate when administered intravenously at 2 mg/kg and undergoes substantial metabolism in liver microsomes, making it a valuable tool for research in pain management and opioid receptor pharmacology. -
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. -
MOR Agonist
Piperidylthiambutene is a potent µ-opioid receptor (MOR) agonist, exhibiting a Ki value of 2.75 nM. This compound demonstrates significant analgesic and antitussive activity, making it valuable for research related to pain management and cough suppression. Its applications include studies focused on opioid receptor interactions and the development of novel therapeutic agents. -
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. -
Neuroprotective Agent
(-)-P7C3-S243 is an orally bioavailable neuroprotective agent that effectively crosses the blood-brain barrier. This compound primarily binds to the μ-opioid receptor and translocator protein (TSPO), demonstrating the ability to inhibit premature apoptosis in newborn hippocampal neurons while safeguarding mature nigral dopaminergic neurons. (-)-P7C3-S243 not only promotes neuronal survival but also mitigates cognitive impairments and alleviates depression-like behaviors in rat models. It is a valuable tool for research focused on neurodegenerative diseases such as Parkinson's and Alzheimer's disease. -
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. -
KOR Full Agonist
SalA-VS-08 is a full agonist of the kappa-opioid receptor (KOR) known for its selectivity and G-protein bias. This compound exhibits significant analgesic activity, making it a valuable tool for research into pain management and opioid receptor signaling. SalA-VS-08 can be utilized in studies investigating the therapeutic potential of KOR activation in various pain conditions. -
Analgesic
MDAN-21 is a bivalent ligand that targets the μ-opioid receptor as an agonist and the δ-opioid receptor as an antagonist. This compound exhibits significant analgesic properties, demonstrating effectiveness in reducing pain without the development of tolerance in preclinical mouse models. Additionally, MDAN-21 has shown potential in mitigating morphine withdrawal symptoms in dependent primates and alleviating abnormal pain responses in studies involving rhesus monkeys. It serves as a valuable tool for research on allodynia and pain modulation. -
Na+ Channel Blocker
RSD-921 is a potent sodium (Na+) channel blocker exhibiting significant anti-arrhythmic properties. It acts with state- and voltage-dependent inhibition on the open states of cardiac, skeletal muscle, and neuronal Na+ channels. Additionally, RSD-921 has a low affinity for κ-opioid receptors and shows weak κ-agonistic activity in vitro. This reagent is valuable for research focusing on cardiac arrhythmias and the modulation of Na+ channels in various biological models. -
NOP Receptor Agonist
Nociceptin(1-7) is a potent agonist of the NOP receptor (ORL1), derived from the N-terminal region of the nociceptin peptide. This compound displays significant antinociceptive properties, making it useful for studying pain modulation and related pathways. Research indicates that Nociceptin(1-7) effectively decreases hyperalgesia in vivo, providing insights into its potential therapeutic applications in pain management. -
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. -
MOR Modulator
BPRMU191 is a selective μ-opioid receptor (MOR) modulator that transforms small-molecule morphinan antagonists into G protein-biased MOR agonists. This conversion facilitates MOR-dependent activation, resulting in potent analgesic effects while minimizing adverse side effects such as gastrointestinal issues, antinociceptive tolerance, and dependency risks. BPRMU191, when used in conjunction with morphinan antagonists, provides a valuable tool for exploring severe pain management and the modulation of G protein-coupled receptors in research settings. -
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. -
ORL-1 Inhibitor
rel-SB-612111 hydrochloride is a selective antagonist of the human opiate receptor-like orphan receptor (ORL-1), exhibiting a high binding affinity with a Ki value of 0.33 nM. This compound demonstrates notable selectivity against μ-, κ-, and δ-opioid receptors, with Ki values of 57.6 nM, 160.5 nM, and 2109 nM, respectively. rel-SB-612111 hydrochloride has been shown to effectively inhibit the pronociceptive effects of Nociceptin in acute pain models, making it a valuable tool for research into pain mechanisms and opioid receptor interactions. -
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. -
ORL1 Partial Agonist
Ac-RYYRIK-NH2 serves as a potent partial agonist of the ORL1 receptor, exhibiting a dissociation constant (Kd) of 1.5 nM in CHO cell models. This compound mimics the action of endogenous ligands, facilitating research into ORL1-related pathways. Additionally, it acts as a specific antagonist for G protein activation, competitively inhibiting [35S]-GTPgS binding stimulated by nociceptin/orphanin FQ in rat brain membranes and sections. Applications include studies of pain modulation, neuropharmacology, and the underlying mechanisms of ORL1 receptor signaling. -
NOP Receptor Agonist
[(pF)Phe4]Nociceptin(1-13)NH2 is a potent and selective agonist for the neuropeptide FF receptor (NOP). With a pKi of 10.68 and a pEC50 of 9.31, it demonstrates significant biological activity, showing over 3000-fold selectivity against δ, κ, and μ opioid receptors. This compound is valuable for research applications aiming to explore nociception, pain modulation, and NOP receptor signaling pathways. -
Dynorphin
[DAla2] Dynorphin A (1-9) (porcine) is a modified dynorphin peptide that primarily targets kappa-opioid receptors. This reagent is valuable for investigating the neurobiological mechanisms of analgesia, addiction, and mood disorders such as depression. Its unique structure allows for enhanced affinity and selectivity in research applications focusing on pain management and substance use disorders. -
Analgetic Agent
Prodilidine hydrochloride is a potent analgesic agent that primarily acts by modulating pain signaling pathways. It has demonstrated significant effectiveness in reducing pain and discomfort in various experimental models. This compound is widely used in research applications focused on pain management and the development of novel analgesic therapies. -
MOR Antagonist
Methocinnamox is a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. It binds non-covalently to the orthosteric site of the MOR in a pseudo-irreversible manner, leading to sustained receptor blockade until new receptors are synthesized. Additionally, Methocinnamox serves as a reversible antagonist at both kappa-opioid (KOR) and delta-opioid receptors (DOR), with Ki values of 4.9 nM and 2.2 nM, respectively, without exhibiting intrinsic agonist activity. This compound is applicable in research focused on opioid overdose reversal and addiction prevention. -
MOR Antagonist
Mu opioid receptor antagonist 9 is a selective antagonist of the mu-opioid receptor (MOR) with a Ki of 77.3 nM. This compound demonstrates high selectivity over kappa-opioid (KOR) and delta-opioid receptors (DOR), making it effective in reversing the antinociceptive effects associated with psychoactive substances. Additionally, Mu opioid receptor antagonist 9 has been shown to counteract respiratory depression induced by these substances in murine models. This reagent is valuable for research in Opioid Use Disorder (OUD). -
NOP receptor Antagonist
Trap-101 hydrochloride is a potent and selective antagonist of the nociceptin/orphanin FQ peptide (NOP) receptor. It demonstrates a strong competitive binding affinity, as evidenced by GTPγ35S binding assays in CHOhNOP membranes, with pKi values of 8.65 for NOP and significantly lower values for classical opioid receptors. Trap-101 has been shown to alleviate motor deficits in rat models of Parkinson's disease, positioning it as a valuable tool for studying nervous system disorders and their underlying mechanisms.
