Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Opiate Agonist
(D-Met2,Pro5)-Enkephalinamide is a potent opiate agonist that primarily targets opioid receptors, exhibiting significant antinociceptive activity. This compound plays a crucial role in pain modulation and is widely used in research to study pain pathways and opioid receptor functions. Its efficacy in pain relief makes it a valuable tool for investigating the molecular mechanisms underlying analgesia. -
Kappa Opioid Receptor Agonist
Anrikefon (HSK21542) is a potent kappa opioid receptor agonist that facilitates analgesic effects through modulation of pain pathways. This compound has been utilized in research to explore its potential therapeutic applications in pain management and opioid-related disorders. Its selective action on the kappa receptor makes it a valuable tool for studies investigating receptor-specific mechanisms in pain modulation. -
μ-Opioid Receptor Agonist
FK 33-824 is a synthetic analogue of Met-enkephalin that serves as a selective agonist of the μ-opioid receptor (μ-OR). This compound is utilized in research to explore pain modulation and the mechanisms underlying opioid receptor signaling. Its targeted activity positions it as a valuable tool in studies related to analgesia and opioid receptor pharmacology. -
KOR Antagonist
CSD-CH2(1,8)-NH2 is a selective and competitive antagonist of the kappa opioid receptor (KOR), exhibiting a binding affinity with a Ki value of 6.8 nM. This compound effectively inhibits calcium mobilization in dorsal root ganglion (DRG) neurons and counteracts the antinociceptive effects of U50,488. CSD-CH2(1,8)-NH2 is valuable for research focused on neuropsychiatric disorders and pain modulation. -
μ/δ Opioid Receptor Agonist
Amdakefalin is a potent agonist of the μ and δ opioid receptors, exhibiting notable analgesic properties. Its mechanism of action involves the modulation of pain pathways, making it a valuable tool for research into pain management and opioid pharmacology. Amdakefalin serves as a promising candidate for investigating therapeutic interventions for various pain-related conditions. -
Dynorphin (1-13) Analogue
Dafphedyn is an analogue of Dynorphin (1-13) that primarily targets opioid receptors. It exhibits diuretic properties and provides significant analgesic effects, which can be inhibited by the centrally administered antagonists Naltrexone or Naloxone. Dafphedyn is suitable for research into pain management and opioid receptor signaling pathways. -
ORL1 Receptor agonist
ZP 120C is a potent partial agonist of the ORL1 receptor. It effectively inhibits electrically induced contractions, making it valuable for studies related to neuromodulation. This compound is particularly useful in research investigating hyponatremia and hypokalemia. -
Opioid Receptor Antagonist
LY-99335 is an opioid receptor antagonist that demonstrates behavioral inhibitory activity. This compound exhibits significant dose separation at specific concentrations, highlighting its potential utility in anesthetic antagonism. LY-99335 can be used for research applications related to pain management and the modulation of opioid receptor activity. -
Opioid Receptor Binding Compound
3-Carboxamidonaltrexone is a potent opioid receptor binding compound that exhibits Ki values of 1.9 nM for the μ-opioid receptor, 110 nM for the δ-opioid receptor, and 22 nM for the K-opioid receptor. This compound serves as a valuable tool for studying opioid receptor interactions and is applicable in research exploring pain modulation, addiction, and opioid receptor pharmacology. Its selective binding affinities make it suitable for investigating diverse biological pathways associated with opioid signaling. -
μ-Opioid Receptor Agoinst/AChE Inhibitor
Eseroline is a potent μ-opioid receptor agonist and a selective, competitive inhibitor of acetylcholinesterase (AChE), with Ki values of 0.1 μM for AChE and 200 μM for butyrylcholinesterase (BuChE). This compound also acts as a nicotinic acetylcholine receptor allosteric enhancing ligand, enhancing acetylcholine signal transduction without directly activating the receptor. Eseroline's neurotoxic effects include cell membrane damage and energy metabolism disruption, making it a valuable tool for investigating Alzheimer's disease pathology and cholinergic signaling. -
Opioid Peptide Derivative
[DAla2, DArg6] Dynorphin A (1-13) (porcine) is a modified opioid peptide targeting opioid receptors in the peripheral nervous system. This derivative exhibits enhanced stability compared to its parent compound, dynorphin (1-13), demonstrating increased resistance to enzymatic degradation. Its unique properties make it a valuable tool for studying opioid receptor signaling and evaluating potential therapeutic applications in pain management and neuropharmacology. -
Opioid Receptor Antagonist
Opioid Receptor Antagonist 2 is a potent antagonist targeting opioid receptors, providing a crucial research tool in the study of opioid pharmacology. This compound effectively reverses ventilatory depression and vocal cord closure induced by fentanyl analogs in murine models. Its properties make it a valuable candidate for investigating acute poisoning scenarios, particularly those involving respiratory depression due to opioid overdose. -
Opioid Receptor Agonist
[Met5]-Enkephalin, amide is a potent agonist targeting δ opioid receptors and putative ζ opioid receptors. This compound is critical for studying pain modulation and the role of endogenous opioids in various physiological processes. Its applications extend to research on neurobiology, pain management, and the development of opioid-based therapeutics. -
NOP/μ-opioid Receptor Agonist
SR-16434 is a partial agonist of the nociceptin/orphanin FQ (NOP) and μ-opioid receptors, exhibiting high binding affinity with Ki values of 7.49 for the NOP receptor and 2.70 for the μ-opioid receptor. This compound demonstrates significant analgesic properties, making it a valuable tool for studying pain mechanisms and developing new pain management strategies. Its dual receptor activity provides insights into the interplay between nociceptive and opioid signaling pathways in research applications. -
δ-Opioid Receptor Agonist
AZD-2327 is a potent and selective agonist of the δ-opioid receptor. It demonstrates high affinity with Ki values of 0.49 nM and 0.75 nM for the C27 and F27 isoforms, respectively, and effective concentration EC50 values of 24 nM and 9.2 nM. AZD-2327 is more than 1000-fold selective over human μ- and κ-opioid receptor subtypes, as well as over 130 other receptors and channels. This compound exhibits notable antidepressant and anxiolytic properties, making it valuable for research in neurological disorders. -
MOR Antagonist
MOR Antagonist 2 Hydrochloride is a selective μ-opioid receptor (MOR) antagonist that effectively penetrates the blood-brain barrier, exhibiting an IC50 of 28.37 nM and a Ki value of 0.18 nM. This compound stabilizes the inactive state of MOR, thereby reducing receptor activation. It has demonstrated efficacy in antagonizing analgesic effects in the mouse warm-water tail-flick test and shows a reduced incidence of withdrawal symptoms in mice subjected to opioid withdrawal. MOR Antagonist 2 Hydrochloride is valuable for research into opioid use disorder and related therapeutic applications. -
Analgesic Agent
Met-Enkephalin-Arg-Phe is a naturally occurring heptapeptide that functions as an analgesic agent through its action on opioid receptors. This compound is implicated in modulating pain perception and has been utilized in research to explore its potential therapeutic applications in pain management. Its biological activity makes it a valuable tool for studies involving endogenous opioid systems and pain-related pathways. -
MOR Agonist
(D-Arg2, Sar 4)-Dermorphin (1-4) is a tetrapeptide derivative with high affinity for the μ-opioid receptor (MOR), functioning as a potent agonist. It exhibits significant analgesic properties, making it an important compound for research into pain management and the development of novel analgesic therapies. Researchers may utilize (D-Arg2, Sar 4)-Dermorphin (1-4) to explore mechanisms of opioid action and to investigate the potential for therapeutic applications in pain relief. -
κ-Opioid Receptor Agonist
CJ-15161 is a κ-opioid receptor agonist, primarily involved in modulating pain perception and emotional responses. This compound serves as a valuable tool for investigating the physiological functions associated with κ-opioid receptor activation, including analgesia and the regulation of mood. Its use in research contributes to a deeper understanding of opioid receptor pathways and their implications in pain management and mental health disorders. -
Antidepressant Agent
[Des-Tyr1]-gamma-Endorphin is a neuropeptide that functions as an antidepressant agent. This compound displays notable antidepressant efficacy by facilitating the extinction of active avoidance behaviors while attenuating passive avoidance in rodent models. Its applications extend to research in neuropharmacology and behavioral studies focused on mood disorders. -
µOR Antagonist
Mu opioid receptor antagonist 7 is a potent antagonist of the µ-opioid receptor (µOR), demonstrating an IC50 value of 29 ± 3.0 nM. This compound is highly permeable to the central nervous system, making it suitable for investigating pain mechanisms and the pharmacology of opioid use disorder. Its efficacy in modulating µOR activity supports its use in preclinical research settings focused on opioid receptor signaling and related therapeutic interventions. -
Opioid Receptor Antagonist
PF-4455242 hydrochloride is a selective antagonist of the κ-opioid receptor, known for its potential analgesic properties. This compound was developed using a strategy that combines parallel chemistry and physicochemical property design. PF-4455242 hydrochloride has shown confirmed potency and selectivity in preclinical models such as the tail-flick analgesia test, making it a valuable tool for research into pain mechanisms and opioid receptor interactions. -
δ2 Opioid Receptor Antagonist
N-Benzylnaltrindole hydrochloride is a potent and selective antagonist of the δ2 opioid receptor. It exhibits a longer duration of action in vivo compared to Naltriben (NTB), making it valuable for studies involving the δ-opioid receptor. This compound serves as an important reagent for the pharmacologic characterization of δ-opioid receptor function, facilitating research in pain management and opioid signaling pathways. -
MOR Ligand
Fluorphine is a potent μ-opioid receptor (MOR) ligand that exhibits a binding affinity with a Ki value of 12.5 nM. This compound demonstrates biological activity by promoting GTPγS binding with an EC50 of 75 nM and facilitating β-arrestin 2 recruitment with an EC50 of 377 nM. Fluorphine is primarily used in research to investigate opioid signaling pathways and their physiological effects, including respiratory depression. -
Opioid Receptor Agonist
TAN-67 is a non-peptidic agonist of the delta-opioid receptor, demonstrating significant antinociceptive activity in both diabetic and non-diabetic mouse models. It effectively reduces acetic acid-induced abdominal constrictions in a dose-dependent manner, exhibiting a stronger response in diabetic mice. The analgesic properties of TAN-67 are primarily mediated through the activation of delta 1-opioid receptors, as evidenced by the pronounced antagonism when a selective delta 1-opioid receptor antagonist is administered. This compound is useful for research into pain mechanisms and the potential therapeutic applications of delta-opioid receptor modulation. -
μ-opioid Receptor Antagonist
Cyprodime hydrochloride is a selective μ-opioid receptor antagonist, demonstrating a Ki value of 5.4 nM for the μ-opioid receptor while exhibiting considerably lower affinities for δ- and κ-opioid receptors (244.6 nM and 2187 nM, respectively). This compound has been shown to produce anti-depressant-like effects, making it a valuable tool for investigating the roles of opioid receptors in mood disorders and other neuropharmacological research applications. -
KOP-r Agonist
Mesyl Salvinorin B is a selective agonist of the kappa opioid receptor (KOP-r) that exhibits significant biological activity in the modulation of alcohol consumption. It effectively prevents the alcohol deprivation effect (ADE) in murine models and demonstrates a dose-dependent reduction in both alcohol intake and preference in chronic escalation drinking (CED) mice. This compound is valuable for research into addiction pathways and the pharmacological modulation of substance use behaviors. -
Opioid Agonist
β-Lipotropin (61-69) is a potent opioid agonist that selectively binds to opioid receptors, exerting significant analgesic effects. This peptide demonstrates key biological activities relevant to pain management and neurobiology research. Its application in studying opioid receptor signaling pathways makes it a valuable reagent for exploring the mechanisms of pain modulation and addiction. -
KOR Agonist
SHR0687 is a selective tetrapeptide kappa opioid receptor (KOR) agonist, exhibiting an EC50 of 0.53 pM. This compound demonstrates high potency and selectivity for KOR over mu opioid receptors (MOR) and delta opioid receptors (DOR), with minimal penetration of the blood-brain barrier. SHR0687 selectively activates KOR, which may enable the modulation of neurological pathways while minimizing central nervous system side effects. It is suitable for research applications focused on pain modulation and the exploration of KOR-related mechanisms. -
Analgesic Agent
DS39201083 is a Conolidine derivative with potent analgesic properties that operates independently of mu opioid receptor activation. This compound has demonstrated significant efficacy as an oral agent for pain relief, making it a valuable tool in the investigation of neurological disorders. Its unique mechanism and lack of interaction with traditional opioid pathways provide opportunities for research into alternative analgesic therapies. -
Opioid Receptor Agonist
Dynorphin A (1-10) is an endogenous opioid neuropeptide that acts as an agonist at the κ-opioid receptor, specifically binding to extracellular loop 2. Its biological activity includes the modulation of pain pathways and effects on mood regulation. Additionally, Dynorphin A (1-10) inhibits NMDA receptor-activated currents with an IC50 of 42.0 μM, making it a valuable tool for research into pain, addiction, and neuroprotection. This peptide is essential for studying opioid receptor dynamics and their implications in neurological disorders.
