2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Opioid Receptor

Opioid Receptor

Opioid Receptor

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Opioid receptors are a group of G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. Opioid receptors are distributed widely in the brain, and are found in the spinal cord and digestive tract. Opioid receptors are molecules, or sites, within the body that are activated by opioid substances. Opioid receptors inhibit the transmission of impulse in excitatory pathways within the human body system. These pathways include the serotonin, catecholamine, and substance P pathways, which are all implicated in pain perception and feelings of well-being. Opioid receptors are further subclassified into mu, delta, and kappa receptors. All the classes, while exhibiting differing modes of action, share some basic similarities. They all are driven by the potassium pump mechanism, which is found on the plasma membrane of the majority of cells.

Opioid Receptor Isoform Specific Products:

Opioid Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-144606
    Mu opioid receptor antagonist 1
    		Antagonist
    Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active μ opioid receptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC).
    Mu opioid receptor antagonist 1
  • HY-136786
    RU-24213 hydrochloride
    		Antagonist
    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-160938
    β-Funaltrexamine
    		Antagonist
    β-Funaltrexamine (β-FNA) is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases.
    β-Funaltrexamine
  • HY-A0118AS
    Naloxegol-d5 oxalate
    		Antagonist
    Naloxegol-d5 (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
    Naloxegol-d<sub>5</sub> oxalate
  • HY-P1299
    UFP-101
    		Antagonist
    UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect.
    UFP-101
  • HY-P1320
    [Nphe1]Nociceptin(1-13)NH2
    		Antagonist
    [Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
    [Nphe1]Nociceptin(1-13)NH2
  • HY-169867
    BNTX
    		Antagonist
    BNTX (7-Benzylidenenaltrexone) is a highly selective δ1 opioid receptor antagonist. BNTX selectively antagonizes the antinociceptive activity mediated by spinal δ1 opioid receptors, and does not alter the antinociceptive effects mediated by δ2, μ or κ opioid receptors at selective doses.
    BNTX
  • HY-16979
    TRK-851
    		Antagonist
    RK-851 is a highly selective and orally active δ-opioid receptor antagonist, with a negative logarithm of the antagonist concentration (pA2) of 8.84. TRK-851 exhibits the selectivity for the δ receptor of more than 100 times higher than that for the μ or κ receptors. TRK-851 exhibits a potent antitussive effect in a rat model of capsaicin-induced cough. TRK-851 can be used for research on antitussive effects.
    TRK-851
  • HY-P10175
    Acetalin-1
    		Antagonist
    Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors.
    Acetalin-1
  • HY-16765
    Axelopran
    		Antagonist
    Axelopran (TD-1211) is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
    Axelopran
  • HY-170654
    Opioid receptor antagonist 1
    		Antagonist
    Opioid receptor antagonist 1 (Compound 10) is an Orvinol (HY-D0168)-based opioid receptor antagonist. Opioid receptor antagonist 1 has antagonistic activity to the analgesic properties of Morphine.
    Opioid receptor antagonist 1
  • HY-133717
    Naltriben
    		Antagonist
    Naltriben is a selective δ2-opioid receptor antagonist and TRPM7 activator. Naltriben enhances glioblastoma cell migration and invasion. Naltriben can be used in research into neurological diseases and cancer.
    Naltriben
  • HY-163895
    δ opioid receptor antagonist 1
    		Antagonist
    δ opioid receptor antagonist 1 (compound 6-Cy3) is a fluorescent antagonist probe with high selectivity for δ opioid receptor (DOR) (Ki=1.7 nM). δ opioid receptor antagonist 1 can be used to study the mechanism of pain perception.
    δ opioid receptor antagonist 1
  • HY-107121
    Ondelopran
    		Antagonist
    Ondelopran (LY 2196044) is a non-selective opioid receptor antagonist. Ondelopran inhibits the release of dopamine in the nucleus accumbens induced by alcohol, reduces the rewarding effect of alcohol consumption, and lowers the craving. Ondelopran can be used for alcohol use disorder (AUD).
    Ondelopran
  • HY-119733
    BU09059
    		Antagonist
    BU09059 is a potent and selective Kappa-opioid receptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception.
    BU09059
  • HY-120277
    TIPP
    		Antagonist
    TIPP is a potent and selective δ-opioid antagonist with a Ki value of 1.22 nM.
    TIPP
  • HY-P5061
    Dynorphin A (1-13) amide
    		Antagonist
    Dynorphin A (1-13) amide is an endogenous opioid peptide that antagonizes morphine-induced analgesia.
    Dynorphin A (1-13) amide
  • HY-112263
    ORL1 antagonist 1
    		Antagonist
    ORL1 antagonist 1 is an opioid receptor-like 1 (ORL1) antagonist with an IC50 of 61 nM.
    ORL1 antagonist 1
  • HY-172149
    Naltrindole 5′-isothiocyanate
    		Antagonist
    Naltrindole 5′-isothiocyanate (5'-NTII) is a non-selective delta opioid receptor antagonist that can antagonize the analgesic effects induced by DSLET (HY-P1332) without affecting the analgesic effects induced by DPDPE (HY-P1334).
    Naltrindole 5′-isothiocyanate
  • HY-101718R
    Aticaprant (Standard)
    		Antagonist
    Aticaprant (Standard) (CERC-501 (Standard)) is the analytical standard of Aticaprant (HY-101718). This product is intended for research and analytical applications. Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
    Aticaprant (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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