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κ-opioid agonists

" in MedChemExpress (MCE) Product Catalog:

107

Inhibitors & Agonists

16

Peptides

7

Natural
Products

8

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-110252

    Opioid Receptor Neurological Disease Inflammation/Immunology
    Salvinorin B is a selective and brain-penetrant kappa opioid receptor (KOPr) agonist with an EC50 of 248 nM and Ki of 2.95 μM. Salvinorin B activates downstream signaling pathways by binding to KOPr, inhibits pain transmission and reduces inflammatory response. Salvinorin B can be used for the researches of inflammation, immunology and neurological disease, such as neuropathic pain, multiple sclerosis and anxiety .
    Salvinorin B
  • HY-B0188A
    Mianserin hydrochloride
    1 Publications Verification

    Org GB 94

    Histamine Receptor Opioid Receptor ERK p38 MAPK Neurological Disease Metabolic Disease
    Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .
    Mianserin hydrochloride
  • HY-17609
    Difelikefalin
    1 Publications Verification

    CR-845; FE-202845

    Opioid Receptor Neurological Disease Inflammation/Immunology
    Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
    Difelikefalin
  • HY-10487
    JDTic dihydrochloride
    3 Publications Verification

    Opioid Receptor Neurological Disease
    JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
    JDTic dihydrochloride
  • HY-P1333
    Dynorphin A
    1 Publications Verification

    Opioid Receptor Apoptosis Caspase Endogenous Metabolite Neurological Disease
    Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
    Dynorphin A
  • HY-100903

    nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride

    Opioid Receptor Neurological Disease
    Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .
    Norbinaltorphimine dihydrochloride
  • HY-117040
    nor-Binaltorphimine
    5+ Cited Publications

    Norbinaltorphimine; NorBNI

    Opioid Receptor Neurological Disease
    nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain .
    nor-Binaltorphimine
  • HY-B0188
    Mianserin
    1 Publications Verification

    Mianserine

    Histamine Receptor Opioid Receptor ERK p38 MAPK Neurological Disease
    Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
    Mianserin
  • HY-145404
    Mitragynine pseudoindoxyl
    1 Publications Verification

    Opioid Receptor Metabolic Disease
    Mitragynine pseudoindoxyl is a potent orally active agonist of the μ-opioid receptor (MOR-1, Ki=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, Ki=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, Ki=24 nM) and does not recruit β-arrestin-2, acting through G protein-mediated signaling pathways without β-arrestin-2-related activation. Mitragynine pseudoindoxyl produces potent analgesic activity through a mixed μ-agonist/δ-antagonist mechanism, with low side effects such as physical dependence, respiratory depression, and constipation, and no rewarding or aversive behaviors. Mitragynine pseudoindoxyl reduces hyperactivity, inhibits GI transit, and enhances characteristics, making it a potential analgesic .
    Mitragynine pseudoindoxyl
  • HY-P2159

    Opioid Receptor Endogenous Metabolite Neurological Disease
    Dynorphin A (1-8) is a ligand with preference for the κ-opioid receptor, and its IC50 value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .
    Dynorphin A (1-8)
  • HY-P3445A

    HSK21542 acetate

    Opioid Receptor Neurological Disease
    Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect .
    Anrikefon acetate
  • HY-P3609
    CR 665
    2 Publications Verification

    JNJ 38488502; FE 200665

    Opioid Receptor Neurological Disease
    CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
    CR 665
  • HY-100845

    Divinorin A

    Opioid Receptor Cardiovascular Disease
    Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with Ki value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum.
    Salvinorin A
  • HY-176710

    Protein Arginine Deiminase Opioid Receptor mAChR Neurological Disease Inflammation/Immunology Cancer
    PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC50 = 12.3 μM). The IC50 values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca 2+-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer .
    PAD-PF2
  • HY-130118

    Mas-related G-protein-coupled Receptor (MRGPR) Neurological Disease
    MRGPRX1 agonist 1 is a highly potent MRGPRX1 agonist (EC50=50 nM) with greater than 50-fold selectivity for δ, μ, and κ opioid receptors. MRGPRX1 agonist 1 is inactive against MRGPRC11. MRGPRC11 inhibits high voltage-activated (HVA) Ca 2+ currents, reduces neurotransmitter release, and mitigates nociceptive transmission in the spinal cord. MRGPRX1 agonist 1 is useful for the study of chronic pain, especially neuropathic pain .
    MRGPRX1 agonist 1
  • HY-101231

    Opioid Receptor Neurological Disease
    ICI-204448 is a κ-opioid agonist with limited access to the CNS, ICI-204448 can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes .
    ICI-204448
  • HY-107384A

    EMD-61753 hydrochloride

    Opioid Receptor Neurological Disease Metabolic Disease Inflammation/Immunology
    Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
    Asimadoline hydrochloride
  • HY-P3445

    HSK21542

    Opioid Receptor Neurological Disease
    Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effect .
    Anrikefon
  • HY-P0088

    Dynorphin A Porcine Fragment 1-13

    Opioid Receptor Others
    Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
    Porcine dynorphin A(1-13)
  • HY-123689

    ALKS-33; RDC-0313

    Opioid Receptor Neurological Disease
    Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo. Samidorphan can improve the behavior of depressed animals .
    Samidorphan
  • HY-101205

    Opioid Receptor Cardiovascular Disease Neurological Disease
    ICI-199441 hydrochloride is a potent and selective κ-opioid receptor agonist with analgesic effects. ICI 199441 hydrochloride can improve heart resistance to ischemia/reperfusion .
    ICI-199441 hydrochloride
  • HY-101079

    Opioid Receptor Neurological Disease
    BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with Kis of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage .
    BRL 52537 hydrochloride
  • HY-15997B

    (±)-Trans-(1R,2R)-U-50488 hydrochloride

    Opioid Receptor Neurological Disease
    (±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist .
    (±)-U-50488 hydrochloride
  • HY-15691

    Opioid Receptor mTOR Neurological Disease Metabolic Disease
    PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal .
    PF-04455242
  • HY-110302

    Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .
    6'-GNTI dihydrochloride
  • HY-121800

    Opioid Receptor Others
    ML138, a κ opioid receptor agonist, is a MLPCN probe .
    ML138
  • HY-B0188AR

    Org GB 94 (Standard)

    Reference Standards Histamine Receptor Opioid Receptor ERK p38 MAPK Neurological Disease Metabolic Disease
    Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .
    Mianserin hydrochloride (Standard)
  • HY-B0188S

    Mianserine-d3

    Histamine Receptor Isotope-Labeled Compounds Opioid Receptor ERK p38 MAPK Neurological Disease
    Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
    Mianserin-d3
  • HY-19231

    Org 41793

    Opioid Receptor Neurological Disease
    DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively. DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity .
    DPI-3290
  • HY-107384

    EMD-61753

    Opioid Receptor Neurological Disease Metabolic Disease Inflammation/Immunology
    Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
    Asimadoline
  • HY-15997C

    (±)-Trans-(1R,2R)-U-50488 hydrate hydrochloride

    Opioid Receptor Neurological Disease
    (±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist .
    (±)-U-50488 hydrate hydrochloride
  • HY-105235

    CI-977

    Opioid Receptor Neurological Disease
    Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
    Enadoline
  • HY-120949

    Opioid Receptor Neurological Disease
    (1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist .
    (1R,2R)-U-50488 hydrochloride
  • HY-170973

    Opioid Receptor
    KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .
    KOR agonist 4
  • HY-106756

    U-62066

    Opioid Receptor Neurological Disease
    Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
    Spiradoline
  • HY-17609S1

    CR-845-d5 hydrochloride; FE-202845-d5 hydrochloride

    Isotope-Labeled Compounds Opioid Receptor Neurological Disease Inflammation/Immunology
    Difelikefalin-d5 (CR-845-d5) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
    Difelikefalin-d5 hydrochloride
  • HY-145128

    Opioid Receptor Neurological Disease
    GR103545 is a potent and selective agonist of the κ-opioid receptor (κ-OR). 11GR103545 is a radiotracer for imaging κ-OR in vivo [1]
    GR103545 fumarate
  • HY-B0188AS

    Org GB 94-d3

    Isotope-Labeled Compounds Histamine Receptor Opioid Receptor ERK p38 MAPK Neurological Disease Metabolic Disease
    Mianserin-d3 hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
    Mianserin-d3 hydrochloride
  • HY-126063

    Opioid Receptor Neurological Disease
    ICI-204448 free acid is a κ-opioid agonist with limited access to the CNS, ICI-204448 free acid can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes .
    ICI-204448 free acid
  • HY-163017

    Opioid Receptor Neurological Disease
    NP-5497-KA is a κ-opioid receptor agonist. NP-5497-KA has orally activity[1].
    NP-5497-KA
  • HY-106605

    LY 120363

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Flumezapine (LY 120363) is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine can be used in antipsychotic research .
    Flumezapine
  • HY-101582

    Opioid Receptor Neurological Disease
    ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye.
    ZT 52656A hydrochloride
  • HY-123689S1

    ALKS-33-d5; RDC-0313-d5

    Isotope-Labeled Compounds Opioid Receptor Neurological Disease
    Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .
    Samidorphan-d5
  • HY-108043

    Opioid Receptor Neurological Disease
    AZD-2327 is a potent and selective δ-opioid receptor agonist. AZD-2327 binds to the human opioid receptor (Ki of 0.49 and 0.75 nM and EC50 of 24 and 9.2 nM at the C27 and F27 isoforms, respectively). AZD-2327 shows selectivity of >1000-fold over the human μ- and κ-opioid receptor subtypes as well as >130 other receptors and channels. AZD-2327 exhibits antidepressant and anxiolytic activities and can be used for the research of neurological disease .
    AZD-2327
  • HY-178945

    Opioid Receptor Interleukin Related TNF Receptor Sigma Receptor Neurological Disease Inflammation/Immunology
    KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (Ki = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation .
    KOR agonist 7
  • HY-136786

    Dopamine Receptor Opioid Receptor Neurological Disease
    RU-24213 hydrochloride is a selective D-2 dopamine receptor agonist. RU-24213 hydrochloride is also a KAPPA-opioid receptor antagonist. RU-24213 hydrochloride induces stereotyped behaviors .
    RU-24213 hydrochloride
  • HY-171236

    Opioid Receptor
    FEKAP is a brain-penetrant and selective kappa opioid receptor (KOR) agonist (Ki = 0.43 nM) which isotope labeled form exhibits excellent imaging properties. 11C-FEKAP can be utilized as a radiotracer for imaging KOR .
    FEKAP
  • HY-124959

    U-62066 mesylate

    Opioid Receptor Neurological Disease
    Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
    Spiradoline mesylate
  • HY-163277

    Opioid Receptor Inflammation/Immunology
    PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .
    PIPE-3297
  • HY-17609S

    CR-845-d5; FE-202845-d5

    Isotope-Labeled Compounds Opioid Receptor Neurological Disease
    Difelikefalin-d5 (CR-845-d5) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
    Difelikefalin-d5

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