Catalog No.
Product Name
Application
Product Information
Citations
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Opioid Agent
AH-8533 is an opioid agent that primarily targets μ-opioid receptors. This compound exhibits potent analgesic properties, making it valuable for pain management research. Its pharmacological profile may facilitate studies on opioid signaling pathways and the development of novel therapeutic strategies for pain relief. -
Analgesics
Sameridine is a weak partial agonist of the μ-opioid receptor, primarily utilized in analgesic applications. Exhibiting local anesthetic and analgesic properties, Sameridine provides a unique profile with minimal respiratory depression at low doses, though higher doses may suppress ventilatory response. This compound is valuable for research focused on exploring analgesic effects and opioid receptor pharmacology. -
Opioid Receptor Antagonist
N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu is a selective antagonist of the δ-opioid receptor, effectively inhibiting the actions of enkephalins such as [D-Pen2,D-Pen5] enkephalin in vivo. This compound is suitable for behavioral experiments aimed at studying opioid receptor functions and exploring potential therapeutic approaches for opioid-related disorders. Its unique structure supports research into the modulation of pain pathways and addiction mechanisms. -
δ-opioid Receptor Agonist
BW373U86 is a highly selective δ-opioid receptor agonist with an IC50 value of 1.49 nM. It has demonstrated antidepressant-like effects in preclinical studies, making it a valuable tool for research into mood disorders and the underlying mechanisms of opioid receptor signaling. This compound is particularly relevant for investigations into pain management and the modulation of emotional states. -
Analgesic
Allyphenyline oxalate acts primarily as an analgesic, enhancing the analgesic effects of Morphine. It demonstrates affinity for adrenergic α2 receptor subtypes with pKi values of 7.24 for α2A, 6.47 for α2B, and 7.07 for α2C. This compound is valuable for research focused on pain management and the modulation of opioid analgesia. -
Opioid Receptor Agonist
SR16835 is a selective agonist targeting the nociceptin/orphanin FQ peptide (NOPr) and mu-opioid receptor (MOPr). It exhibits full agonist activity at NOPr and partial agonist activity at MOPr, allowing for detailed exploration of opioid receptor mechanisms. Notably, SR16835 does not produce analgesic effects, making it a valuable tool for research into receptor-specific functions and therapeutic applications in pain management and opioid signaling pathways. -
NOP Receptor Agonist
[Arg14,Lys15]Nociceptin is a highly potent and selective agonist of the NOP receptor (also known as ORL1 or OP4), exhibiting an EC50 of 1 nM. This compound demonstrates exceptional specificity for the NOP receptor, with IC50 values of 0.32 nM for NOP and significantly higher values for μ (280 nM), δ (>10,000 nM), and κ (1500 nM) opioid receptors. [Arg14,Lys15]Nociceptin is valuable for research applications exploring pain modulation, neuropharmacology, and the role of nociceptin in various physiological processes. -
NOP Antagonist
NOP Antagonist 1 is a nociceptin opioid peptide (NOP) antagonist with a binding affinity characterized by a Kb of 8.65 nM. This compound is valuable for research focused on neuropsychiatric disorders, as it modulates nociceptin receptor activity, providing insights into pain signaling and potential therapeutic strategies. Its specificity and potency make it an essential tool for exploring the role of the NOP system in various physiological and pathological conditions. -
μ-opioid Receptor Antagonist
Mu Opioid Receptor Antagonist 8 is a selective antagonist of the μ-opioid receptor. This compound effectively inhibits met-enkephalin-induced activation of the receptor via the Gi signaling pathway, making it valuable for research in pain management and addiction studies. Its ability to modulate μ-opioid receptor activity positions it as a critical tool for understanding opioid receptor pharmacology and potential therapeutic interventions. -
κ Opioid Receptor Agonist
Riminkefon is a κ-opioid receptor agonist that selectively binds to and activates the κ-opioid receptor, leading to various physiological effects. It exhibits significant analgesic properties and has been employed in research related to pain management, mood regulation, and the study of addictive behaviors. Riminkefon serves as a valuable tool for exploring the therapeutic potential of κ-opioid receptor modulation in various neurological and psychological conditions. -
MOR Agonist
SR-14968 is a full allosteric and non-competitive agonist of the mu-opioid receptor (MOR), exhibiting an EC50 of 88 nM in mouse brainstem assays. This compound stabilizes the MOR in a G protein signaling state that demonstrates resistance to washout, while remaining reversible by antagonists. SR-14968 is capable of inducing respiratory depression in murine models, making it a valuable tool for exploring pain-related mechanisms and the pharmacological effects of MOR activation in research settings. -
Kappa-Opioid Receptor Agonist
LPK-26 hydrochloride is a selective kappa-opioid receptor agonist, exhibiting a Ki of 0.68 nM. This compound demonstrates significant antinociceptive properties while showing low potential for physical dependence. It is valuable for research into pain management and the mechanisms of opioid receptor activation. -
µ-Opioid Receptor Agonist
Bilaid A1e is a tetrapeptide that acts as an agonist of the µ-opioid receptor, exhibiting a binding affinity with a Ki value of 750 nM. Isolated from an Australian estuarine strain of Penicillium sp., Bilaid A1e holds potential for applications in pain research. Its ability to modulate µ-opioid receptor activity makes it a valuable tool for studying analgesic pathways and developing pain management strategies. -
Urotensin II Antagonist
Urotensin-II receptor antagonist-1 is a selective antagonist of the human Urotensin II receptor, exhibiting a Ki value of 16 nM in HEK293 cells expressing the recombinant receptor. This compound demonstrates significant biological activity by inhibiting cytochrome P450 enzymes, CYP2D6 and CYP3A4, with IC50 values of 0.75 μM and 1.4 μM, respectively. Additionally, it inhibits the κ-opioid receptor with an EC50 of 3.2 μM and targets cardiac sodium channels with a Ki of 2.5 μM. Research applications include studies of cardiovascular physiology and drug metabolism. -
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. -
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.
