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-P1779
    β-Casomorphin (1-5), bovine
    		99.62%
    β-Casomorphin (1-5), bovine is a peptide of bovine β-Casomorphin.
    β-Casomorphin (1-5), bovine
  • HY-113316A
    (±)-Salsolinol hydrochloride
    		Agonist
    (±)-Salsolinol hydrochloride is the hydrochloride form of (±)-Salsolinol (HY-113316). (±)-Salsolinol hydrochloride is a Dopamine (HY-B0451)-derived endogenous metabolite. (±)-Salsolinol hydrochloride activates μ-opioid receptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA).
    (±)-Salsolinol hydrochloride
  • HY-100122
    Bevenopran
    		Antagonist 99.82%
    Bevenopran is a peripheral μ-opioid receptor antagonist.
    Bevenopran
  • HY-P1334A
    DPDPE TFA
    		Agonist 99.94%
    DPDPE TFA, an opioid peptide, is a selective δ-opioid receptor (DOR) agonist with anticonvulsant effects.
    DPDPE TFA
  • HY-P3445A
    Anrikefon acetate
    		Agonist 99.25%
    Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect.
    Anrikefon acetate
  • HY-P1596
    Gluten Exorphin C
    		Inhibitor 99.86%
    Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.
    Gluten Exorphin C
  • HY-107384
    Asimadoline
    		Agonist 99.36%
    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-107743
    Naloxone benzoylhydrazone
    		Modulator ≥99.0%
    Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect.
    Naloxone benzoylhydrazone
  • HY-A0118
    Naloxegol
    		Antagonist
    Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
    Naloxegol
  • HY-14157
    ADL-5747
    		Agonist 99.82%
    ADL-5747 is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 activates these receptors, thereby playing a role in pain management pathways. ADL-5747 can be used for research into pain management mechanisms.
    ADL-5747
  • HY-107750
    Cyprodime
    		Antagonist
    Cyprodime is a selective μ opioid receptor (MOR) antagonist with Kis of 5.4, 244.6, and 2187 nM for μ, δ, and κ, respectively.
    Cyprodime
  • HY-15536A
    Cebranopadol ((1α,4α)stereoisomer)
    Cebranopadol ((1α,4α)stereoisomer) is a stereoisomer of cebranopadol. Cebranopadol is a potent agonist activity on ORL-1.
    Cebranopadol ((1α,4α)stereoisomer)
  • HY-134189A
    EST73502 monohydrochloride
    		Agonist 99.58%
    EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity.
    EST73502 monohydrochloride
  • HY-P1742
    Gluten Exorphin B5
    		Agonist 98.23%
    Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats.
    Gluten Exorphin B5
  • HY-U00031
    Axomadol
    		Activator 99.74%
    Axomadol (EN3324) is a centrally active analgesic agent with opioid agonistic properties and inhibitory effects on the reuptake of monoamines.
    Axomadol
  • HY-12698
    NNC 63-0532
    		Agonist 99.81%
    NNC63-0532 is a novel non-peptide nociceptin receptor (ORL1) agonist, with EC50s of 305?nM. NNC63-0532 plays important roles in many disorders such as pain, drug addiction.
    NNC 63-0532
  • HY-135230
    LY2444296
    		Antagonist 99.59%
    LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ～1 nM. LY2444296 exhibits anti-anxiety like effects.
    LY2444296
  • HY-P4053
    Dalargin
    		Agonist 99.52%
    Dalargin is a potent δ-opioid receptor agonist. Dalargin mitigates Gentamicin (HY-A0276)-induced cell death. Dalargin shows nephroprotective effects on Gentamicin-induced kidney injury. Dalargin shows antiulcer activity.
    Dalargin
  • HY-17417R
    Naloxone (hydrochloride) (Standard)
    		Antagonist
    Naloxone (hydrochloride) (Standard) is the analytical standard of Naloxone (hydrochloride). This product is intended for research and analytical applications. Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias.
    Naloxone (hydrochloride) (Standard)
  • HY-106147B
    Frakefamide TFA
    		Agonist 99.18%
    Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
    Frakefamide TFA
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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