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-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-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-144224S
    Tianeptine-d6 hydrochloride
    		Agonist
    Tianeptine-d6 hydrochloride is the deuterium labeled Tianeptine hydrochloride. Tianeptine hydrochloride is an atypical antidepressant. Tianeptine hydrochloride is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine hydrochloride is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine hydrochloride increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine hydrochloride exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine hydrochloride inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine hydrochloride can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
    Tianeptine-d<sub>6</sub> hydrochloride
  • 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-P0192
    [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2
    		Agonist
    [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 is a nociceptin receptor (ORL1) agonist. [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 strongly depresses the nociceptive flexor reflex in rats. [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 can be used for analgesia research.
    [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2
  • 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
  • HY-120456
    SR16835
    		Agonist
    SR16835 has high affinity for both NOPr and MOPr, with full agonist activity for NOPr and partial agonist activity for MOPr. SR16835 has no analgesic effect.
    SR16835
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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