Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Analgesic Agent
Viminol is a centrally acting analgesic agent that inhibits pain perception through modulation of central nervous system pathways. In addition to its analgesic properties, Viminol exhibits antitussive activity, making it useful in research related to pain management and cough suppression. Its mechanisms of action provide valuable insights for studies involving analgesia and respiratory control. -
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. -
NOP Partial Agonist
Ac-RYYRWK-NH2 TFA serves as a potent and selective partial agonist for the nociceptin receptor (NOP). It exhibits significant binding affinity, with a Kd of 0.071 nM for rat cortical membranes (ORL1), while demonstrating no affinity for μ-, κ-, or δ-opioid receptors. This compound is valuable for research investigating nociceptin signaling pathways and their implications in pain modulation and various neurological disorders. -
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. -
µOR Agonist
μ Opioid Receptor Agonist 3 is a potent agonist of the μ opioid receptor (µOR) with an EC50 of 0.87 nM. This compound has demonstrated significant biological activity, indicating its potential for use in the research of pain management and neuropsychiatric disorders. Its high affinity for µOR makes it a valuable tool for exploring the therapeutic applications of opioid-targeted therapies. -
Prodrug of BPRMU191
DBPR116 is a prodrug of BPRMU191 designed for efficient penetration of the blood-brain barrier. This compound enhances the delivery of centrally acting analgesics and has been shown to provide superior safety and analgesic efficacy in combination with Naltrexone compared to traditional opioids such as morphine. In various in vivo pharmacological models, DBPR116 effectively alleviates pain related to thermal and cancer sources while minimizing adverse effects, suggesting its potential as a safer alternative in opioid analgesia. -
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. -
μ Receptor Agonist
Frakefamide is a selective μ-opioid receptor agonist, primarily functioning as a potent analgesic. Its design allows for peripheral action without penetrating the blood-brain barrier, thereby minimizing central nervous system side effects. This compound is primarily utilized in research focused on pain management and the modulation of peripheral pain pathways. -
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. -
KOR Agonist
Enadoline (CI-977) is a highly selective nonpeptide agonist of the kappa-opioid receptor (KOR) with a Ki value of 1.25 nM, enabling effective brain penetration. It exhibits significant antinociceptive activity, making it a valuable tool for researching pain mechanisms and potential therapeutic applications in pain management and opioid research. -
MOR modulator
MOR modulator-1 is a potent and selective modulator of the μ opioid receptor (MOR). This compound demonstrates enhanced receptor selectivity and improved antagonistic effects in vivo, resulting in fewer withdrawal symptoms compared to traditional opioids like NAT. With binding affinities (Kis) of 0.25 nM for MOR, 41.1 nM for δ, and 1.30 nM for γ receptors, MOR modulator-1 is a valuable tool for research in pain management and opioid receptor pharmacology. -
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. -
Peptide
[DAla2] Dynorphin A (1-13), amide (porcine) is a peptide that primarily targets the κ opioid receptors. This compound exhibits potential agonist activity, making it valuable for exploring the physiological roles of dynorphins in the nervous system. Its utility spans various research applications, including studies on pain modulation, stress response, and neuropharmacology. -
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. -
NOP Receptor Antagonist
UFP-101 is a selective and competitive antagonist of the NOP receptor, exhibiting a pKi of 10.24. It demonstrates greater than 3000-fold selectivity over delta, mu, and kappa opioid receptors. UFP-101 has been shown to produce antidepressant-like effects, making it a valuable tool for research into mood disorders and the role of NOP receptor signaling. -
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. -
Ociceptin Receptor Antagonist
[Nphe1]Nociceptin(1-13)NH2 is a selective nociceptin receptor antagonist that exhibits competitive inhibition without any agonistic effects. It binds specifically to recombinant nociceptin receptors with a binding affinity (pKi) of 8.4 and effectively antagonizes nociceptin-induced inhibition of cyclic AMP accumulation in CHO cells (pA2=6.0). This compound shows promise for research applications related to pain modulation and the exploration of nociceptin signaling pathways. -
DOR Agonist
ADL-5747 hydrochloride is a selective and orally active agonist of the δ-opioid receptor (DOR). By activating DOR, it modulates pain management pathways, making it a valuable tool for investigating analgesic mechanisms. This compound is suitable for research focused on pain relief and the pharmacological implications of opioid receptors. -
MOR Activator
(RS)-Salsolinol hydrobromide is a μ-opioid receptor (MOR) activator derived from dopamine. It has been shown to reduce GABAergic transmission and increase the excitability of dopamine neurons, subsequently enhancing the sustained firing of neurons in the posterior ventral tegmental area (pVTA). This compound is useful in research applications investigating the modulation of dopaminergic signaling and its implications in various neurological conditions. -
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. -
KOR Agonist
(+)-U-50488 is a selective κ-opioid receptor (KOR) agonist exhibiting reduced potency compared to its enantiomer, (-)-Trans-(1S,2S)-U-50488. This compound is utilized in pharmacological research to investigate the role of KOR in pain modulation, mood disorders, and substance use disorders. Its ability to activate KOR provides a valuable tool for studying the physiological and pathophysiological functions of the opioid system. -
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. -
KOR Agonist
(+)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist. It exhibits key biological activity in modulating pain pathways and is utilized in research focused on opioid receptor mechanisms. This compound is an important tool for studying the effects of KOR activation in various biological contexts. -
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. -
MOR Agonist/σ1R Antagonist
EST73502 is a selective dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, demonstrating effective blood-brain barrier penetration. With binding affinities (Kis) of 64 nM for MOR and 118 nM for σ1R, EST73502 exhibits notable antinociceptive properties. This compound is pertinent for research applications in pain management and neurological studies, allowing for the exploration of opioid receptor pathways and σ1R interactions. -
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. -
Local anesthesia/analgesic
Sameridine hydrochloride is a local anesthetic that primarily targets sodium channels to block nerve impulse transmission. It exhibits potent analgesic properties, making it effective for pain management in various clinical settings. This compound is commonly utilized in research focused on anesthetic development and pain relief mechanisms. -
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. -
Analgesic Agent
α-Endorphin (human) is a neuropeptide that primarily acts on the μ-opioid receptors in the central and peripheral nervous systems. It demonstrates significant analgesic properties, making it a valuable agent in pain management research. Additionally, α-Endorphin (human) plays a role in the modulation of sexual behaviors and feelings of pleasure, further underscoring its importance in behavioral studies and neurobiology. -
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.
