Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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.
