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-P3625
    Dynorphin (2-17), amide (porcine)
    Dynorphin (2-17), amide (porcine) is a dynorphin derivative with some analgesic effects. Dynorphin is a class of opioid peptides produced by the precursor protein dynorphinogen and is involved in pain, addiction and mood regulation.
    Dynorphin (2-17), amide (porcine)
  • HY-129271
    Deltorphin
    		Agonist
    Deltorphin (Deltorphin A; Dermenkephalin) is a biological active peptide. (Deltorphin A peptide was isolated from skin extracts of the South American frog, Phyllomedusa sauvagei. Deltorphin A is a potent and selective agonist for the delta-opioid receptor.)
    Deltorphin
  • HY-P5907
    Helianorphin-19
    		Activator
    Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain.
    Helianorphin-19
  • HY-170342
    KOR agonist 3
    		Agonist
    KOR agonist 3 (Compound 5) is a κ opioid receptor (κOR) agonist with an EC50 of 0.88 nM. KOR agonist 3 also has a certain activation effect on μOR with an EC50 of 720 nM. KOR agonist 3 shows no agonist activity for δOR at concentrations less than 1 μM. KOR agonist 3 has a lower ability to induce the recruitment of β-Arrestin-2 than U50488 (HY-15997B).
    KOR agonist 3
  • HY-145369
    DS34942424
    		Modulator
    DS34942424 is an orally potent analgesic without mu opioid receptor agonist activity.
    DS34942424
  • HY-P1626
    Acetyl tetrapeptide-15
    		Agonist 99.49%
    Acetyl tetrapeptide-15 is a synthetic peptide. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway. Acetyl tetrapeptide-15 is used in the cosmetics for sensitive skin.
    Acetyl tetrapeptide-15
  • HY-P2046
    β-Endorphin (rat)
    		Modulator
    β-Endorphin (rat) is an endogenous opioid neuropeptide and peptide hormone. β-Endorphin (rat) has analgesic activity and also contributes to food intake in satiated rats. β-Endorphin (rat) can be used in the research of neurological diseases such as analgesia and drug addiction.
    β-Endorphin (rat)
  • HY-121974
    SR14150
    SR14150 is a partial agonist of the NOP receptor with high affinity. The biological activity of SR14150 makes it potentially useful for the development of a new generation of multi-target opioids designed to simultaneously improve analgesia and reduce side effects. The activity of SR14150 and its interaction with other opioid receptors may provide new inhibitory options for the management of chronic pain.
    SR14150
  • HY-100963
    U-54494A
    U-54494A is a benzamide derivative related to κ-opioid receptor agonists, U-54494A has an anticonvulsant activity.
    U-54494A
  • HY-P1316
    Ac-RYYRWK-NH2
    		Antagonist
    Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors.
    Ac-RYYRWK-NH2
  • HY-163017
    NP-5497-KA
    		Agonist
    NP-5497-KA is a κ-opioid receptor agonist. NP-5497-KA has orally activity[1].
    NP-5497-KA
  • HY-149387
    D3R/MOR antagonist 2
    		Antagonist
    D3R/MOR antagonist 2 (Compound 121) is a D3R/MOR antagonist (Ki: 361 nM and 85.2 nM respectively). D3R/MOR antagonist 2 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism.
    D3R/MOR antagonist 2
  • HY-P1302A
    Orphanin FQ(1-11) TFA
    		Agonist
    Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1 mice.
    Orphanin FQ(1-11) TFA
  • HY-131930
    AH-8533
    		Control
    AH-8533 is a opioid agent.
    AH-8533
  • HY-P2429
    N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu
    		Antagonist
    N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu is a compound that can antagonize the δ-opioid receptor and the action of [D-Pen2,D-Pen?] enkephalin in vivo. Its antagonistic effect can be verified by specific behavioral experiments.
    N,N-Diallyl-Tyr-Aib-Aib-Phe-Leu
  • HY-P3874
    Peptide E
    		Agonist
    Peptide E is a potent kappa opiate receptor agonist. Peptide E has opiate receptor binding activity with IC50 value of 0.39 μM. Peptide E can be used for the research of central nervous system.
    Peptide E
  • HY-172407
    KOR agonist 5
    		Modulator
    KOR agonist 5 (Compound 10a) is a KOR/MOR modulator with agonistic activity towards KOR and antagonistic activity towards MOR. KOR agonist 5 can effectively block morphine-induced antinociception and inhibition of intestinal motility. KOR agonist 5 can be used in the research of Substance Use Disorder (SUD).
    KOR agonist 5
  • HY-P1320A
    [Nphe1]Nociceptin(1-13)NH2 TFA
    		Antagonist
    [Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
    [Nphe1]Nociceptin(1-13)NH2 TFA
  • HY-107751
    BW373U86
    		Agonist
    BW373U86 (SNC86) is a δ-opioid receptor agonist with an IC50 of 1.49 nM. BW373U86 shows antidepressant-like effects.
    BW373U86
  • HY-138839
    Allyphenyline oxalate
    		Agonist
    Allyphenyline oxalate (compound 9) can enhance the analgesic effect of Morphine. The pKi values ​​of Allyphenyline for α2A, α2B and α2C are 7.24, 6.47 and 7.07, respectively.
    Allyphenyline oxalate
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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