Catalog No.
Product Name
Application
Product Information
Citations
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κ-opioid Receptor Antagonist
PF-04455242 is a selective antagonist of the κ-opioid receptor, exhibiting a high binding affinity with an average Ki value of 3.0 nM in human tissues. This compound is known for its ability to block κ-opioid receptor-mediated analgesia and has demonstrated antidepressant-like effects in preclinical models. Additionally, PF-04455242 is effective in attenuating behavioral responses associated with stress, making it valuable for research into pain modulation and mood disorders. -
Delta Opioid Receptor Agonist
SYK-1106 is a highly potent delta-opioid receptor (DOR) agonist, exhibiting an EC50 of 89 pM and a Ki of 848 pM. This compound demonstrates selectivity for μ and κ opioid receptors, with Ki values of 9.54 nM and 2.45 nM, respectively. SYK-1106 has been shown to induce dose-dependent antidepressant-like effects, making it a valuable tool for research in the field of depression and related disorders. -
Opioid Receptor
CJ-15208 is a potent and selective κ-opioid receptor antagonist with notable analgesic properties. In preclinical studies, it demonstrated significant analgesic effects in the warm water tail withdrawal test in mice, mediated through multiple opioid receptors. Distinct stereoisomers of CJ-15208 exhibit varying opioid activity characteristics; one stereoisomer antagonizes κ-opioid receptors, while another targets δ-opioid receptors. Importantly, none of the stereoisomers affected respiration or induced drug tolerance, highlighting CJ-15208's potential for development as a safer alternative in opioid analgesics. -
Opioid Receptor Agonist
KK-103 is an opioid receptor agonist that serves as a stable precursor to leucine-enkephalin (Leu-ENK). By significantly enhancing plasma stability in murine models, KK-103 effectively mitigates the high proteolytic instability typically associated with Leu-ENK. Its potent antinociceptive properties make it a valuable tool for research applications focused on pain modulation and the opioid signaling pathway. -
Opioid Agonist
LY-281217 is a potent mu-opioid agonist that primarily targets the mu-opioid receptor. This compound exhibits significant analgesic activity, making it valuable in pain management research. Its mechanism of action provides insights into opioid signaling pathways and the development of therapies for pain-related conditions. -
Opioid Receptor Agonist
JO-1870 hydrochloride is a selective agonist of opioid receptors, specifically designed to induce bladder relaxation through opioid receptor activation. This compound shows potential in the study of urinary incontinence, offering insights into its mechanisms and possible therapeutic interventions. Researchers can utilize JO-1870 hydrochloride to explore its effects on bladder function and its applications in urology. -
Opioid Receptors Positive Allosteric Modulator
MPAM-15 is a positive allosteric modulator of opioid receptors, demonstrating significant selectivity for the μ-opioid receptor over δ and κ receptors. This compound enhances anti-nociceptive effects, providing potential analgesic properties observed in mouse models via intracerebroventricular and intraperitoneal administration. MPAM-15 serves as a valuable tool in pain-related research, offering insights into opioid receptor modulation and its therapeutic implications. -
Opioid Receptor Agonist
AR-M 1000390 is a highly selective and potent agonist of the delta-opioid receptor, demonstrating an EC50 value of 7.2±0.9 nM. This compound serves as a valuable tool for studying opioid receptor signaling and its effects on pain modulation. Its specificity for the δ opioid receptor makes it particularly useful in research applications focused on opioid pharmacology and potential therapeutic interventions for pain-related disorders. -
Kappa Opioid Receptor Agonist
(±)-U-50488 is a selective agonist of the kappa opioid receptor. It has been shown to improve symptoms associated with status epilepticus, while exhibiting minimal impact on spontaneous seizure occurrences. This compound is valuable for research focused on epilepsy and its underlying mechanisms. -
Opioid Peptide
N-Acetyl-α-Endorphin is an acetylated form of the endogenous opioid peptide α-Endorphin, modified at the N-terminal. This compound primarily targets opioid receptors and exhibits significant analgesic properties. It is widely utilized in research focusing on pain management, addiction, and the modulation of neuronal signaling pathways associated with opioid activity. -
Opioid Receptor Agonist
BW443C is a selective agonist of opioid receptors, primarily targeting the mu-opioid receptor. This compound exhibits significant antinociceptive properties, making it valuable for research into pain management and analgesic therapies. BW443C is suitable for studying opioid receptor signaling pathways and evaluating the therapeutic potential of opioid agonists in various preclinical models. -
Opioid Receptor Agonist
(rel)-RSD 921 is a potent κ-opioid receptor agonist known for its role in modulating pain and reward pathways. Research indicates that (rel)-RSD 921 has differential effects on appetite regulation, evidenced by similar food-inducing responses in both obese and lean Zucker rats, with lean rats exhibiting heightened sensitivity to its initial effects. This compound is valuable for studies focused on opioid signaling, appetite modulation, and related physiological responses. -
δ1 Opioid Receptor Antagonist
BNTX (7-Benzylidenenaltrexone) is a selective antagonist of the δ1 opioid receptor. It effectively inhibits the antinociceptive effects mediated by spinal δ1 receptors while leaving the actions at δ2, μ, and κ opioid receptors unchanged at specific concentrations. This compound is useful in studying pain pathways and the role of δ1 receptors in analgesia, making it a valuable tool for research in pain management and opioid receptor pharmacology. -
δ-Opioid Receptor Antagonist
TRK-851 is a highly selective δ-opioid receptor antagonist, with a pA2 value of 8.84, indicating strong binding affinity. It exhibits over 100-fold selectivity for the δ-opioid receptor compared to μ or κ receptors. This compound demonstrates significant antitussive effects in preclinical models, particularly in capsaicin-induced cough assays. TRK-851 is suitable for research focused on the mechanisms of cough suppression and the role of δ-opioid receptors in pain modulation. -
κ-opioid Receptor Agonist
Spiradoline is a selective κ-opioid receptor (KOR) agonist, demonstrating a Ki of 8.6 nM in guinea pig models. With significantly higher Ki values for μ and δ receptors at 252 nM and 9400 nM, respectively, Spiradoline exhibits notable biological activities, including analgesic, diuretic, antiarrhythmic, antitussive, and neuroprotective effects. Its ability to effectively penetrate the blood-brain barrier makes it a valuable reagent for research in pain management and neurological studies. -
Opioid Receptor
Samidorphan isoquinoline dioxolane is an analog of cyclazocine that primarily targets opioid receptors. This compound exhibits significant opioid receptor binding activity, making it a valuable tool in the study of opioid pharmacology. Its unique structure and mechanism of action contribute to research applications in pain management, addiction studies, and the exploration of novel therapeutics related to the opioid system. -
Opioid Receptor Agonist
BU72 is a potent and long-acting agonist of the μ and κ opioid receptors, exhibiting partial agonist activity at δ opioid receptors with EC50 values of 0.054, 0.033, and 0.58 nM, respectively. This compound is characterized by its strong and sustained analgesic effects primarily mediated through μ opioid receptor activation. Additionally, BU72 has the capability to partially reverse morphine-induced analgesia, making it a valuable tool for research on opioid dependence and pain management strategies. -
μ Opioid Receptor Antagonist
Acetalin-1 is a hexapeptide that acts as a μ opioid receptor antagonist, demonstrating high affinity for both μ and κ3 opioid receptors, while exhibiting weak affinity for κ1 receptors and no binding to κ2 receptors. Its inhibitory action on μ opioid receptors makes it a valuable tool for studying pain pathways and opioid receptor pharmacology. Acetalin-1's specificity and receptor binding profile support its use in research related to addiction, pain management, and opioid-related signaling pathways. -
Opioid Receptor Agonist
β-Endorphin, equine is an endogenous opioid peptide that acts as a high-affinity agonist for μ and δ opioid receptors. It exhibits notable analgesic properties, making it valuable for research into pain modulation and opioid signaling pathways. This reagent is applicable in various in vitro and in vivo studies focused on opioid receptor function and related therapeutic applications in pain management and addiction research. -
μ-Opioid Receptor Antagonist
CTOP is a potent and highly selective μ-opioid receptor antagonist. It effectively counteracts the acute analgesic effects of morphine and mitigates hypermotility associated with opioid administration. Additionally, CTOP has been shown to enhance extracellular dopamine levels in the nucleus accumbens and dose-dependently increase locomotor activity, making it a valuable tool for research on opioid receptor functions and dopamine activity in the context of pain and addiction studies. -
Opioid Receptor Antagonist
Axelopran is a potent opioid receptor antagonist that exhibits high affinity for human recombinant μ (pKi 9.8), δ (pKi 8.8) receptors, as well as the guinea pig κ receptor (pKi 9.9). This compound is primarily utilized in analgesic research and studies involving opioid receptor modulation. Its antagonistic properties make it valuable for investigating pain pathways and potential therapeutic applications in opioid overdose and addiction. -
Opioid Receptor Antagonist
Opioid receptor antagonist 1 is an Orvinol-based compound that acts as an opioid receptor antagonist. This reagent demonstrates effective antagonistic activity against the analgesic effects of Morphine, making it a valuable tool for investigating opioid signaling pathways and the mechanisms underlying opioid addiction and tolerance. Its applications extend to research focused on pain management and the development of new therapeutic strategies for opioid-related disorders. -
δ2-opioid Receptor Antagonist/TRPM7 Activator
Naltriben is a selective antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It has been shown to enhance migration and invasion of glioblastoma cells, making it a valuable tool for studying tumor biology. This compound is suited for research into neurological disorders and cancer mechanisms, providing insights into therapeutic approaches targeting these areas. -
Opioid Receptor Antagonist
Ondelopran is a non-selective opioid receptor antagonist that modulates opioid signaling pathways. This compound effectively inhibits dopamine release in the nucleus accumbens, counteracting the rewarding effects of alcohol consumption and reducing cravings associated with alcohol use disorder (AUD). Ondelopran is primarily utilized in research focused on addiction and the neurobiological mechanisms underlying substance use disorders. -
δ-opioid Receptor Agonist
(Rac)-SNC80 is a racemic compound that acts as a potent and selective agonist of the δ-opioid receptor, exhibiting a Ki value of 1.78 nM and an IC50 of 2.73 nM. This compound demonstrates significant antinociceptive, antihyperalgesic, and antidepressant-like effects, making it a valuable tool for research in pain management and mood disorders. Furthermore, (Rac)-SNC80 may have therapeutic potential for treating various headache disorders, facilitating studies focused on opioid receptor modulation and its implications in analgesia. -
Opioid Receptor
Naloxone-d5 is a deuterium-labeled derivative of Naloxone, a potent antagonist of opioid receptors. This compound selectively binds to opioid receptors, effectively reversing the effects of opioid overdose. It is particularly useful in pharmacological studies investigating opioid receptor dynamics and in the development of analytical methods for opioid detection and quantification. Naloxone-d5 serves as a critical tool for researchers studying opioid receptor interactions and opioid-related disorders. -
Opioid Receptor Blocker
β-Chlornaltrexamine dihydrochloride is a potent antagonist targeting opioid receptors, specifically effective in blocking the effects of κ-opioid receptor agonists. This compound significantly inhibits the inhibitory action on dopamine release, making it a valuable tool for investigating pain perception mechanisms. Its utilization in research provides insights into opioid signaling pathways and potential therapeutic approaches for pain management. -
Opioid Receptor
Valorphin is a peptide fragment derived from the hemoglobin β-chain (33-39) that acts as an agonist at the mu-opioid receptor. It exhibits potent analgesic properties, with an IC50 of 14 nM in binding assays. In addition to its opioid activity, Valorphin demonstrates significant anti-tumor effects, making it valuable for research in pain management and cancer biology. -
Kappa-Opioid Receptor Antagonist
BU09059 is a potent and selective antagonist of the kappa-opioid receptor (KOR), displaying a pA2 value of 8.62. It exhibits nanomolar affinity specifically for the κ-receptor, demonstrating 15-fold selectivity over the μ-opioid receptor and 616-fold selectivity over the δ-opioid receptor. BU09059 effectively inhibits U50488-induced antinociception, making it a valuable tool for studying pain pathways and opioid receptor pharmacology. This compound is essential for researchers investigating the role of kappa-opioid receptors in various biological contexts. -
Opioid Receptor Agonist
β-Endorphin (6-31) is an opioid receptor agonist that primarily targets μ-opioid receptors. This endogenous neuropeptide is produced in select neurons of both the central and peripheral nervous systems and plays a crucial role in modulating pain perception, stress responses, and maintaining homeostatic balance. Its biological activities make it a valuable reagent for research into pain management and opioid signaling pathways. -
Opioid Receptor Antagonist
TIPP is a highly selective δ-opioid receptor antagonist, exhibiting a Ki value of 1.22 nM. It effectively blocks δ-opioid receptor activity, making it a valuable tool for studying opioid signaling pathways and the effects of opioid modulation in various physiological contexts. Its unique properties facilitate research into pain management, addiction, and potential therapeutic interventions targeting the opioid system. -
Opioid Receptor Agonist
Dermorphin Analog is a synthetic heptapeptide that serves as a potent μ-opioid receptor agonist. This compound demonstrates significant analgesic activity through its high affinity for opioid receptors, making it a valuable tool for studying pain mechanisms and opioid signaling pathways. Researchers may utilize Dermorphin Analog in investigations of pain management therapies and the development of novel analgesics. -
Opioid Agonist
β-Lipotropin (60-65) is an opioid peptide that functions as a potent opioid agonist. It is known to interact with the opioid receptors, influencing pain modulation and various neurobiological processes. This reagent is valuable for research applications focused on opioid signaling pathways, pain management studies, and the exploration of its physiological roles in the body. -
Opioid Peptide
β-Casomorphin is an opioid peptide that primarily acts as an agonist at opioid receptors. This compound exhibits biological activity associated with pain modulation, gastrointestinal function, and is relevant in studies of addiction and opioid signaling pathways. β-Casomorphin serves as a valuable tool in pharmacological research to understand the implications of opioid peptides in various physiological processes. -
κ-Opioid Receptor Agonist
ICI-199441 is a potent and selective κ-opioid receptor agonist, primarily involved in mediating analgesic effects. This compound has demonstrated the ability to enhance cardiac resilience in models of ischemia/reperfusion, making it a valuable tool for investigating pain modulation and cardiovascular protection. Its specificity for the κ-opioid receptor supports targeted research in pain management and heart disease. -
Opioid Receptor
3,4-Difluoro-N,N-didesmethyl U-47700 TFA is a synthetic opioid compound that selectively targets opioid receptors. It exhibits potent analgesic activity, making it valuable for research into pain management and opioid receptor modulation. This compound can be utilized in studies exploring receptor binding affinity, signaling pathways, and drug formulation in opioid research. -
Opioid Receptor
2-(Di-sec-butylamino)-1-(1-(2-fluorobenzyl)-1H-pyrrol-2-yl)ethan-1-ol functions as a selective ligand for opioid receptors. This compound exhibits significant affinity and activity, making it valuable for studies on pain management and analgesic pathways. Its structural similarities to known opioids allow for exploration of the receptor interactions and potential therapeutic applications in opioid research. -
κ-opioid agonists
ICI-204448 free acid is a potent κ-opioid agonist that demonstrates limited central nervous system penetration. It effectively displaces the binding of the kappa-opioid ligand ^3H-bremazocine from guinea pig cerebellum membranes, making it a valuable tool for exploring κ-opioid receptor interactions. This compound is useful in research applications focused on pain modulation, neuropsychiatric disorders, and the pharmacological profiling of κ-opioid receptors. -
Opioid Receptor Modulator
Opioid Receptor Modulator 1 functions as a selective modulator of opioid receptors, primarily influencing mu and delta subtypes. This compound demonstrates significant biological activity in pain relief and modulation of reward pathways, making it a valuable tool for research into analgesics and addiction therapies. Its applications extend to studies on the pharmacological effects of opioid modulation in various neurological conditions. -
Opioid Receptor Control
Isopaynantheine is an alkaloid that primarily targets opioid receptors. It demonstrates significant antinociceptive activity, making it valuable for pain management studies. Researchers utilize Isopaynantheine to explore opioid receptor modulation and its therapeutic potential in pain-related research. -
Opioid Receptor agonist
DuP 747 is a selective agonist of the kappa-opioid receptor. It exhibits analgesic properties, making it a valuable compound for research focused on pain management and opioid receptor pharmacology. This reagent is useful in exploring the physiological and therapeutic roles of kappa-opioid receptors in various biological contexts. -
kappa-opioid receptor Agonist
22-Thiocyanatosalvinorin A is a potent and selective kappa-opioid receptor agonist, exhibiting an EC50 of 0.077 nM. This compound demonstrates significant biological activity through its interaction with the kappa-opioid receptor, facilitating applications in pain management and neuropharmacological research. Its specificity makes it a valuable tool for studying kappa-opioid receptor signaling pathways and potential therapeutic effects in various neurological conditions. -
Opioid Receptor Agonist
7-PET is a potent μ-opioid receptor agonist, demonstrating significant efficacy in activating opioid signaling pathways. This compound is primarily utilized in research focused on psychiatric disorders, aiding in the exploration of pain modulation, addiction mechanisms, and potential therapeutic interventions for mood disorders. Its selective action makes it a valuable tool for understanding the complex roles of opioid receptors in the central nervous system. -
Opioid Receptor Antagonist
Naltrindole 5′-isothiocyanate (5'-NTII) is an opioid receptor antagonist with a primary mechanism of non-selective antagonism at delta opioid receptors. This compound effectively inhibits the analgesic effects produced by DSLET, while leaving the analgesic effects mediated by DPDPE unaffected. Naltrindole 5′-isothiocyanate is valuable in research applications focused on understanding the therapeutic potential and mechanisms of opioid receptor modulation. -
Opioid Compound
Bromadoline is a utopioid that primarily targets opioid receptors, exhibiting significant antinociceptive activity in rodent models. This compound is utilized in research to explore pain management mechanisms and the development of novel analgesics. Its specific receptor interactions make it a valuable tool for studying the pharmacological effects of opioids in various biological systems. -
Opioid Receptor
Volazocine is an opioid benzomorphane derivative that selectively targets opioid receptors. This compound exhibits significant analgesic activity, making it a valuable research tool for studying pain mechanisms and opioid pharmacology. It is particularly useful in evaluating the efficacy and safety profiles of new analgesic therapies. -
Opioid Receptor
1-(5-Fluoropentyl)-1H-indazole-3-carboxylic acid is a selective modulator of opioid receptors. This compound exhibits significant affinity for cannabinoid receptor sites and shows potential in studying the therapeutic effects of cannabinoid modulation. It is primarily used in research exploring the pharmacological effects of synthetic cannabinoids and their metabolites. -
Opioid Antagonist
RX809055AX is a potent long-acting opioid antagonist that demonstrates selectivity towards mu and delta opioid receptors. This compound effectively inhibits opioid-induced signaling, making it valuable for research applications in pain management and addiction studies. Its extended duration of action offers a consistent approach to investigating opioid receptor activity and its physiological implications. -
Opioid Receptor
Piperidylthiambutene hydrochloride is an opioid receptor agonist that exhibits significant analgesic activity in various animal models. This compound is primarily utilized in research focused on pain management and the study of opioid receptor signaling pathways. Its utility in pharmacological studies makes it a valuable reagent for investigating opioid-related mechanisms and potential therapeutic applications. -
δ-Opioid Receptor Agonist
AZ 12488024 is a potent δ-opioid receptor agonist that acts as a derivative of SNC80. This compound exhibits significant biological activity related to mood regulation and is primarily utilized in research focused on major depressive disorder. Its specific mechanism of action at the δ-opioid receptor makes it a valuable tool for studying opioid-related pathways and their implications in neuropsychiatric conditions.
