2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Opioid Receptor

Opioid Receptor

Opioid Receptor

Related Products

PDF 2.35 MB

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-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-P4196
    Met-Enkephalin-Arg-Phe
    Met-Enkephalin-Arg-Phe is a naturally occurring heptapeptide with analgesic activity.
    Met-Enkephalin-Arg-Phe
  • 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
  • HY-19231
    DPI-3290
    		Agonist
    DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively. DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity.
    DPI-3290
  • HY-101199
    N-Benzylnaltrindole hydrochloride
    		Antagonist
    N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function.
    N-Benzylnaltrindole hydrochloride
  • HY-168351
    Fluorphine
    		Ligand
    Fluorphine is an analogue of Brorphine and can bind to μ-opioid receptor (MOR) (Ki: 12.5 nM). Fluorphine has GTPγS binding (EC50: 75 nM) and βarrestin 2 recruitment (EC50: 377 nM) activity. Fluorphine induces respiratory depressant effects.
    Fluorphine
  • HY-101317A
    TAN-67
    		Agonist
    TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
    TAN-67
  • HY-107750A
    Cyprodime hydrochloride
    		Antagonist
    Cyprodime hydrochloride is a highly selective μ-opioid receptor antagonist with Ki values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioid receptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect.
    Cyprodime hydrochloride
  • HY-126910
    Mesyl Salvinorin B
    		Agonist
    Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice.
    Mesyl Salvinorin B
  • HY-P3515
    β-Lipotropin (61-69)
    		Agonist
    β-Lipotropin (61-69) is a potent opioid agonist.
    β-Lipotropin (61-69)
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.