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-P1793A
    α-Casein (90-95) TFA
    		Agonist 99.58%
    α-Casein (90-95) TFA is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) TFA inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) TFA inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) TFA activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) TFA can be used in the study of the mechanisms of allergic diseases and prostate cancer.
    α-Casein (90-95) TFA
  • HY-118416
    BMS-986124
    		Antagonist 99.00%
    BMS-986124 is a μ-opioid receptor silent allosteric modulator (μ-SAMs). BMS-986124 antagonizes positive allosteric modulator effect of BMS-986122 (µ-OR PAM).
    BMS-986124
  • HY-B0418AS
    Loperamide-d6 hydrochloride
    		Agonist 99.10%
    Loperamide-d6 (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea.
    Loperamide-d<sub>6</sub> hydrochloride
  • HY-19627
    Naldemedine
    		Antagonist
    Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine can be used in opioid-induced constipation (OIC) research. Naldemedine is predicted to bind to 3CLpro encoded by SARS-CoV2 genome.
    Naldemedine
  • HY-P0318
    Hemorphin-7
    		Activator
    Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).
    Hemorphin-7
  • 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-109054
    O-Desmethyltramadol
    		Agonist
    O-Desmethyltramadol is the main active metabolite of tramadol (Tramadol) and can cross the blood-brain barrier. O-Desmethyltramadol mainly exerts its analgesic effect by activating the µ-opioid receptor (µ-OR).
    O-Desmethyltramadol
  • HY-P1793
    α-Casein (90-95)
    		Agonist 99.51%
    α-Casein (90-95) is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) can be used in the study of the mechanisms of allergic diseases and prostate cancer.
    α-Casein (90-95)
  • HY-101233
    ICI 154129
    ICI 154 129 is a delta-opioid receptor antagonist and can be used for seizure research.
    ICI 154129
  • HY-168350
    Chlorphine
    		99.2%
    Chlorphine is a neuroactive halogenated opioid analog.
    Chlorphine
  • 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 an orally active peripherally acting μ-opioid receptor antagonist with a target Ki of 7.42 nM. Naloxegol inhibits the binding of opioids to μ-opioid receptors in the gastrointestinal tract, and alleviates opioid-induced gastrointestinal hypomotility, delayed transit, hypertonicity, and increased fluid reabsorption. Naloxegol is applicable to research related to opioid-induced constipation.
    Naloxegol
  • 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-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-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-168351
    Fluorphine
    		Ligand 99.1%
    Fluorphine is an analogue of Brorphine and can bind to μ-opioid receptor (MOR) (Ki: 12.5 nM). Fluorphine has GTPγS binding (EC50: 75 nM) and βarrestin 2 recruitment (EC50: 377 nM) activity. Fluorphine induces respiratory depressant effects.
    Fluorphine
  • 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 99.26%
    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-101223
    DIPPA hydrochloride
    		Antagonist 99.7%
    DIPPA hydrochloride is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA hydrochloride can be used for the research of anxiety and antidepressant.
    DIPPA hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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