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-P0288A
    [Leu5]-Enkephalin TFA
    		Agonist
    [Leu5]-Enkephalin TFA is a pentapeptide with morphine like properties. [Leu5]-Enkephalin TFA is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
    [Leu5]-Enkephalin TFA
  • HY-139678
    SC13
    		Agonist
    SC13 is an orally active, selective Flap structure-specific endonuclease 1 (FEN1) inhibitor and mu opioid receptor (MOR) activator. SC13 impairs DNA damage repair and induces apoptosis in cancer cells. SC13 activates cGAS-STING signaling, increases chemokine secretion, and promotes CAR-T cell infiltration at solid tumour sites. SC13 can be used for the research of solid tumours and pain.
    SC13
  • HY-P1779A
    β-Casomorphin (1-5), bovine TFA
    β-Casomorphin (1-5), bovine (TFA) is a peptide of bovine β-Casomorphin.
    β-Casomorphin (1-5), bovine TFA
  • HY-136586
    Loperamide phenyl
    		Antagonist 99.9%
    Loperamide phenyl is an impurity of Loperamide (HY-B0418A). Loperamide is an opioid receptor agonist.
    Loperamide phenyl
  • 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-163916
    SalA-VS-07
    		Agonist
    SalA-VS-07 is a G protein-biased partial agonist for the Kappa-opioid receptor (KOR). SalA-VS-07 can be used for research of pain and other disorders.
    SalA-VS-07
  • HY-P1502F
    Biocytin-β-endorphin, human
    		Agonist
    Biocytin-β-endorphin, human is abiotinylated β-Endorphin, human (HY-P1502). 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.
    Biocytin-β-endorphin, human
  • HY-138984
    GRT2932Q
    GRT2932Q is a nonpeptidic opioid receptor-like 1 (ORL1) agonist.
    GRT2932Q
  • HY-137056
    LY164929
    		Ligand
    LY164929 is a highly selective ligand for the lower affinity [3H]D-Ala2-D-Leu-5-enkephalin binding site, exhibiting 1,986-fold selectivity compared to other ligands.
    LY164929
  • HY-P2572
    Deltakephalin
    		Agonist
    Deltakephalin is a potent, selective opiate δ-receptor agonist. Deltakephalin has analgesic properties.
    Deltakephalin
  • HY-120385
    Lexanopadol
    		Agonist
    Lexanopadol (GRT-6006) is a μ-opioid receptor and nociceptor receptor (ORL-1 receptor) agonist. Lexanopadol can be used to study pain.
    Lexanopadol
  • HY-142570S1
    Nalmefene-d4
    Nalmefene-d4 is the deuterium labeled Nalmefene (HY-107744). Nalmefene is a BBB-penetrable?opioid receptor?modulator. Nalmefene is an antagonist of?MOR?and?DOR, and a partial agonist of?KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders.
    Nalmefene-d<sub>4</sub>
  • HY-P2626
    [D-Ala2]-Met-Enkephalin
    		Agonist
    [D-Ala2]-Met-Enkephalin, an opioid peptide, is a potent opioid agonist. [D-Ala2]-Met-Enkephalin inhibits ACh-induced and suckling-induced oxytocin (OT) release.
    [D-Ala2]-Met-Enkephalin
  • HY-P3045
    Bilaid B
    		Control
    Bilaid B (compound 2a) is a tetrapeptide. Bilaid B resembles opioid peptides albeit with a unique, alternating LDLD amino acid configuration. .
    Bilaid B
  • HY-151811
    NAQ
    		Agonist
    NAQ is a potent and selective μ opioid receptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence.
    NAQ
  • HY-P0073S
    Tyr-Gly-Gly-{Phe-13C9,15N}-Met-OH TFA
    Tyr-Gly-Gly-{Phe-13C9,15N}-Met-OH TFA (Met-Enkephalin-13C9,15N TFA) is the 13C- and 15N-labeled Tyr-Gly-Gly-Phe-Met-OH TFA. Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
    Tyr-Gly-Gly-{Phe-<sup>13</sup>C<sub>9</sub>,<sup>15</sup>N}-Met-OH TFA
  • HY-13716R
    Noscapine (Standard)
    		Agonist
    Noscapine (Standard) is the analytical standard of Noscapine. This product is intended for research and analytical applications. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier[4].
    Noscapine (Standard)
  • HY-183773
    KOR agonist-9
    		Agonist
    KOR agonist-9 is a selective kappa opioid receptor (KOR) agonist with an EC50 of 1.41 nM. KOR agonist-9 exhibits >125-fold selectivity over μ/δ-opioid receptors. KOR agonist-9 antinociceptive and antipruritic effects in mice. KOR agonist-9 can be used for the research of pain, pruritus.
    KOR agonist-9
  • HY-14124
    MK-5757
    		Antagonist
    MK-5757 is a Nociceptin/Orphanin FQ Peptide Receptor antagonist. ORL1 antagonist 3 can improve cerebral blood flow disorders and ischemic damage, and alleviate abnormal neurological symptoms. ORL1 antagonist 3can be used for the research of neurological disease, such as traumatic brain injury.
    MK-5757
  • HY-76711R
    Naltrexone (Standard)
    		Antagonist
    Naltrexone (Standard) is the analytical standard of Naltrexone (HY-76711). This product is intended for research and analytical applications. Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
    Naltrexone (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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