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-101039
    AR-M 1000390
    		Agonist
    AR-M 1000390 is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
    AR-M 1000390
  • HY-13716S
    Noscapine-13C,d3
    		Agonist
    Noscapine-13C,d3 is a 13C- labeled and deuterated labeled Noscapine. 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.
    Noscapine-<sup>13</sup>C,d<sub>3</sub>
  • HY-130696A
    (±)-U-50488
    		Agonist
    (±)-U-50488 ((±)-trans-(1R,2R)-U-50488) is a selective kappa opioid receptor agonist. (±)-U-50488 can improve symptoms related to status epilepticus, but has no significant effect on spontaneous seizure episodes. (±)-U-50488 can be used for research of epilepsy.
    (±)-U-50488
  • HY-181515
    KOR agonist 8
    		Agonist
    KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a Ki value of 5.3 nM for human KOR, and EC50 values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research.
    KOR agonist 8
  • HY-10886
    MCOPPB
    		Agonist
    MCOPPB is an orally active and selective agonist of Nociceptin/Orphanin FQ–Receptor. MCOPPB inhibits signaling through the NOP receptor in the mouse brain. MCOPPB is used in anxiety disorders research.
    MCOPPB
  • HY-P1819
    N-Acetyl-α-Endorphin
    N-Acetyl-α-Endorphin is an acetylated α-Endorphin at N-terminal. α-Endorphin is an endogenous opioid peptide.
    N-Acetyl-α-Endorphin
  • HY-136623
    BW443C
    		Agonist
    BW443C is a selective opioid receptor agonist. BW443C has antinociceptive effect.
    BW443C
  • HY-N0398R
    Sec-O-Glucosylhamaudol (Standard)
    		Inhibitor
    Sec-O-Glucosylhamaudol (Standard) is the analytical standard of Sec-O-Glucosylhamaudol. This product is intended for research and analytical applications. Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect.
    Sec-O-Glucosylhamaudol (Standard)
  • HY-P1299
    UFP-101
    		Antagonist
    UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect.
    UFP-101
  • HY-135238
    (rel)-RSD 921
    		Agonist
    (rel)-RSD 921 (PD-117302) is a κ-opioid receptor agonist. (rel)-RSD 921 did not have a greater food-inducing effect in obese than in lean Zucker rats; in both obese and lean Zucker rats, lean rats were more sensitive to its initial food-inducing effect but ultimately ate less.
    (rel)-RSD 921
  • HY-P1320
    [Nphe1]Nociceptin(1-13)NH2
    		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
  • HY-14157A
    ADL-5747 hydrochloride
    		Agonist
    ADL-5747 hydrochloride is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 hydrochloride activates these receptors, thereby playing a role in pain management pathways. ADL-5747 hydrochloride can be used for research into pain management mechanisms.
    ADL-5747 hydrochloride
  • HY-W013353
    (RS)-Salsolinol hydrobromide
    		Agonist
    (RS)-Salsolinol hydrobromide is the hydrobromide form of (±)-Salsolinol (HY-113316). (RS)-Salsolinol hydrobromide is a Dopamine (HY-B0451)-derived endogenous metabolite. (RS)-Salsolinol hydrobromide activates μ-opioid receptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA).
    (RS)-Salsolinol hydrobromide
  • HY-169867
    BNTX
    		Antagonist
    BNTX (7-Benzylidenenaltrexone) is a highly selective δ1 opioid receptor antagonist. BNTX selectively antagonizes the antinociceptive activity mediated by spinal δ1 opioid receptors, and does not alter the antinociceptive effects mediated by δ2, μ or κ opioid receptors at selective doses.
    BNTX
  • HY-129853A
    Doxpicomine
    		Inhibitor
    Doxpicomine is an analgesic with potent activity, effective in treating severe postoperative pain.
    Doxpicomine
  • HY-16979
    TRK-851
    		Antagonist
    RK-851 is a highly selective and orally active δ-opioid receptor antagonist, with a negative logarithm of the antagonist concentration (pA2) of 8.84. TRK-851 exhibits the selectivity for the δ receptor of more than 100 times higher than that for the μ or κ receptors. TRK-851 exhibits a potent antitussive effect in a rat model of capsaicin-induced cough. TRK-851 can be used for research on antitussive effects.
    TRK-851
  • HY-178945
    KOR agonist 7
    		Agonist
    KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (Ki = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation.
    KOR agonist 7
  • HY-106756
    Spiradoline
    		Agonist
    Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier.
    Spiradoline
  • HY-P3087
    Tyr-W-MIF-1
    		Modulator
    Tyr-W-MIF-1 is an opioid tetrapeptide with opiate and antiopiate activity. Tyr-W-MIF-1 can induce analgesia.
    Tyr-W-MIF-1
  • HY-170023
    Samidorphan isoquinoline dioxolane
    Samidorphan isoquinoline dioxolane (Compound 16) is a cyclazocine analogue with opioid receptor binding properties.
    Samidorphan isoquinoline dioxolane
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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