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-106234
    ZP 120C
    		Agonist
    ZP 120C is a potent and partial ORL1 receptor agonist. ZP 120C inhibits electrically induced contraction. ZP 120C can be used in the research of hyponatremia/hypokalemia.
    ZP 120C
  • HY-115844
    LY-99335
    		Antagonist
    LY-99335 is an anesthetic antagonist with behavioral inhibitory activity. LY-99335 exhibits large dose separation at specific doses, indicating its potential in anesthetic antagonism.
    LY-99335
  • HY-N0164R
    Matrine (Standard)
    		Agonist
    Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-170033
    3-Carboxamidonaltrexone
    3-Carboxamidonaltrexone (example 32) is a opioid receptor binding compound with Ki values of 1.9 nM, 110 nM, and 22 nM for μ-opioid receptor, δ-opioid receptor, and K-opioid receptor, respectively.
    3-Carboxamidonaltrexone
  • HY-163669
    ITI-333
    		Agonist
    ITI-333 is a tetracyclic compound with oral bioavailability and analgesic activity, targeting multiple receptors. ITI-333 can be used for research on various forms of pain.
    ITI-333
  • HY-P3632
    [DAla2, DArg6] Dynorphin A, (1-13) (porcine)
    [DAla2, DArg6] Dynorphin A, (1-13) (porcine) (DADAD) is an opioid peptide (dynorphinl-13, DYN) derivative found in porcine pituitary extracts. DYN is highly potent at the peripheral opioid receptors GPI and MVD, but is readily and rapidly degraded in vivo. [DAla2, DArg6] Dynorphin A, (1-13) (porcine) has some resistance to enzymatic cleavage and prevents peptide cleavage by enzymes.
    [DAla2, DArg6] Dynorphin A, (1-13) (porcine)
  • HY-17417AR
    Naloxone (Standard)
    		Antagonist
    Naloxone (Standard) is the analytical standard of Naloxone. This product is intended for research and analytical applications. Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias.
    Naloxone (Standard)
  • HY-173016
    HINT1-IN-1
    		Modulator
    HINT1-IN-1 (Compound 8) is the inhibitor for histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. HINT1-IN-1 affects the cross-regulation between μ-opioid receptor (MOR) and NMDA receptor (NMDAR). HINT1-IN-1 enhances the analgesic effect of morphine without causing opioid tolerance and has independent analgesic effects in mouse model.
    HINT1-IN-1
  • HY-161539
    KOR agonist 1
    		Agonist
    KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg).
    KOR agonist 1
  • HY-P1467
    [Met5]-Enkephalin, amide
    		Agonist
    [Met5]-Enkephalin, amide is an agonist for δ opioid receptors as well as putative ζ (zeta) opioid receptors.
    [Met5]-Enkephalin, amide
  • HY-122681
    SR-16435
    		Agonist
    SR-16435 is a nociceptin/orphanin FQ (NOP)/μ-opioid receptor partial agonist, with high binding affinity (NOP receptor Ki=7.49; μ-Opioid receptor Ki=2.70). SR-16435 can relieve pain.
    SR-16435
  • HY-W654256
    Matrine-d3
    Matrine-d3 (Matridin-d3) is a deuterium labeled Matrine (HY-N0164). 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-d<sub>3</sub>
  • HY-P4196
    Met-Enkephalin-Arg-Phe
    Met-Enkephalin-Arg-Phe is a naturally occurring heptapeptide with analgesic activity.
    Met-Enkephalin-Arg-Phe
  • HY-176063
    TRPV1 antagonist 11
    		Agonist
    TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC50 of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice.
    TRPV1 antagonist 11
  • HY-P1301A
    [Arg14,Lys15]Nociceptin TFA
    		Agonist
    [Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.
    [Arg14,Lys15]Nociceptin TFA
  • HY-P10555
    (D-Arg2, Sar 4)-Dermorphin (1-4)
    		Agonist
    (D-Arg2, Sar 4)-Dermorphin (1-4) is a tetrapeptide derivative of the peptide Dermorphin (HY-P0244) found in amphibian skin. (D-Arg2, Sar 4)-Dermorphin (1-4) has significant analgesic effects by binding to the μ-opioid receptor (MOR) in the body. (D-Arg2, Sar 4)-Dermorphin (1-4) can be used in the development of analgesic drugs.
    (D-Arg2, Sar 4)-Dermorphin (1-4)
  • HY-149386
    D3R/MOR antagonist 1
    		Antagonist
    D3R/MOR antagonist 1 (Compound 114) is a D3R/MOR antagonist (Ki: 46.5 nM and 691 nM respectively). D3R/MOR antagonist 1 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism.
    D3R/MOR antagonist 1
  • HY-P10498
    [Des-Tyr1]-gamma-Endorphin
    [Des-Tyr1]-gamma-Endorphin is a neuropeptide, which can be found in human cerebrospinal fluid. [Des-Tyr1]-gamma-Endorphin exhibits antidepressant efficacy, facilitates the extinction of active avoidance and attenuates the passive avoidance behavior in rats.
    [Des-Tyr1]-gamma-Endorphin
  • HY-155320
    Mu opioid receptor antagonist 7
    		Antagonist
    Mu opioid receptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioid receptor), with an IC50 of 29 ± 3.0 nM. Mu opioid receptor antagonist 7 can be used for the research of pain and opioid use disorder.
    Mu opioid receptor antagonist 7
  • HY-15691A
    PF-4455242 hydrochloride
    		Antagonist
    PF-4455242 hydrochloride is a selective, short-acting antagonist of the κ-opioid receptor, exhibiting potential analgesic effects. PF-4455242 hydrochloride has been identified through a strategy utilizing parallel chemistry and physicochemical property design. PF-4455242 hydrochloride demonstrated confirmed potency and selectivity in the tail-flick analgesia model.
    PF-4455242 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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