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 99.87%
    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 99.92%
    [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-17609S1
    Difelikefalin-d5 hydrochloride
    		Agonist
    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-d<sub>5</sub> hydrochloride
  • HY-19070
    BRL-52656
    		Agonist
    BRL-52656 is a blood-brain barrier (BBB)-penetrable KOR receptor agonist that exhibits a biphasic effect. At low doses, BRL-52656 decreases blood pressure, whereas high doses have the opposite effect in spontaneously hypertensive rats. Additionally, BRL-52656 induces water diuresis by inhibiting the secretion of vasopressin (AVP).
    BRL-52656
  • HY-115500
    PL265
    		Activator
    PL265 is an orally active dual enkephalinase inhibitor. PL265 is a prodrug of PL254, which can simultaneously and efficiently inhibit neutral endopeptidase (Neprilysin) and Aminopeptidase N. PL265 can effectively protect and significantly increase the local concentration of enkephalins (such as Met-Enkephalin and Leu-Enkephalin) released by cells at the pain or inflammation sites, thereby activating μ and δ opioid receptors to produce a potent analgesic effect. PL254 can also inhibit leukotriene A4 hydrolase (LTA4H), which may contribute to its additional anti-inflammatory effect by reducing the production of pro-inflammatory mediator leukotriene B4 (LTB4). PL265 can be used in non-addictive chronic pain research.
    PL265
  • HY-15122
    Sinomenine
    		Activator 99.96%
    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 99.59%
    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 99.56%
    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-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-17417A
    Naloxone
    		Antagonist 99.71%
    Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias.
    Naloxone
  • 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-110252
    Salvinorin B
    		Agonist 99.90%
    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-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
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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