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-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)
  • HY-15122AR
    Sinomenine hydrochloride (Standard)
    		Activator
    Sinomenine hydrochloride (Standard) is the analytical standard of Sinomenine hydrochloride. This product is intended for research and analytical applications. Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
    Sinomenine hydrochloride (Standard)
  • HY-P1594
    Dynorphin A (1-10)
    		Agonist
    Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
    Dynorphin A (1-10)
  • HY-N7437
    Akuammidine
    		Inhibitor
    Akuammidine, isolated from the seeds of Picralima nitida, shows a preference for μ-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 μM at μ-, σ- and κ-opioid binding sites, respectively. Akuammidine possesses anti-inflammatory and anti-asthmatic properties.
    Akuammidine
  • HY-113929
    Loperamide oxide
    Loperamide oxide (R-58425) is a orally active prodrug of the Loperamide (HY-156131). Loperamide oxide incubation with the contents of the intestinal lumen inhibits fluid secretion under aerobic conditions.
    Loperamide oxide
  • HY-121415
    Herkinorin
    		Agonist
    Herkinorin is a potent and selective agonist of µ opioid receptor with a Ki of 45 nM Herkinorin is widely used for pain research.
    Herkinorin
  • HY-175197
    MP1202
    		Agonist
    MP1202 is a dual-functional agonist of MOR and KOR with EC50s of 0.32 and 0.13  μM for mMOR-1 and mKOR-1, respectively. MP1202 has functional selectivity with reduction of β-arrestin1/2 recruitment but significant activation of G-protein and Gα-subtype at hMOR and hKOR. MP1202 has potent antinociceptive effects without typical opioid side effects, but it shows conditioned place preference and aversion behaviors in subtype-selective opioid KO mice model, promising for analgesia research.
    MP1202
  • HY-144606
    Mu opioid receptor antagonist 1
    		Antagonist
    Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active μ opioid receptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC).
    Mu opioid receptor antagonist 1
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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