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-P0210
    DAMGO
    		Agonist 99.90%
    DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR.
    DAMGO
  • HY-B0418A
    Loperamide hydrochloride
    		Agonist 99.89%
    Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist. Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect.
    Loperamide hydrochloride
  • HY-17417
    Naloxone hydrochloride
    		Antagonist 99.96%
    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
  • HY-N0164
    Matrine
    		Agonist ≥98.0%
    Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).
    Matrine
  • HY-P0288
    [Leu5]-Enkephalin
    		Agonist 99.85%
    [Leu5]-Enkephalin is a pentapeptide with morphine like properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
    [Leu5]-Enkephalin
  • 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-101318
    β-Funaltrexamine hydrochloride
    		Antagonist 98.0%
    β-Funaltrexamine (β-FNA) hydrochloride is a selective μ opioid receptor antagonist. β-Funaltrexamine hydrochloride also inhibits cytokine-induced iNOS activation. β-Funaltrexamine hydrochloride inhibits neuroinflammation and ameliorated neuronal degeneration. β-Funaltrexamine hydrochloride has anti-inflammatory and neuroprotective effects and can be used for research of neurodegenerative diseases (eg: stroke)[1][2]
    β-Funaltrexamine hydrochloride
  • HY-13716A
    Noscapine hydrochloride
    		Agonist 99.87%
    Noscapine ((S,R)-Noscapine) hydrochloride is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
    Noscapine hydrochloride
  • HY-15122
    Sinomenine
    		Activator 99.94%
    Sinomenine, an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
    Sinomenine
  • HY-101718
    Aticaprant
    		Antagonist 99.87%
    Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
    Aticaprant
  • HY-100903
    Norbinaltorphimine dihydrochloride
    		Antagonist 98.91%
    Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
    Norbinaltorphimine dihydrochloride
  • HY-P1333
    Dynorphin A
    		Agonist
    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-P0073
    Tyr-Gly-Gly-Phe-Met-OH
    		Activator 99.80%
    Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
    Tyr-Gly-Gly-Phe-Met-OH
  • HY-15122A
    Sinomenine hydrochloride
    		Activator 99.89%
    Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
    Sinomenine hydrochloride
  • HY-P1502
    β-Endorphin, human
    		Agonist 98.12%
    β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
    β-Endorphin, human
  • HY-P0183
    Nociceptin
    		Agonist 98.70%
    Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.
    Nociceptin
  • HY-13274
    JTC-801
    		Antagonist 98.91%
    JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM.
    JTC-801
  • HY-101202
    SNC80
    		Agonist 99.82%
    SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.
    SNC80
  • HY-10487
    JDTic dihydrochloride
    		Antagonist 98.03%
    JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
    JDTic dihydrochloride
  • HY-B0557
    Bisacodyl
    		Inhibitor 99.71%
    Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.
    Bisacodyl
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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