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-14124
    MK-5757
    		Antagonist
    MK-5757 is a Nociceptin/Orphanin FQ Peptide Receptor antagonist. ORL1 antagonist 3 can improve cerebral blood flow disorders and ischemic damage, and alleviate abnormal neurological symptoms. ORL1 antagonist 3can be used for the research of neurological disease, such as traumatic brain injury.
    MK-5757
  • HY-76711R
    Naltrexone (Standard)
    		Antagonist
    Naltrexone (Standard) is the analytical standard of Naltrexone (HY-76711). This product is intended for research and analytical applications. Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
    Naltrexone (Standard)
  • HY-76657AR
    Alvimopan dihydrate (Standard)
    		Antagonist
    Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus.
    Alvimopan dihydrate (Standard)
  • HY-144609
    Mu opioid receptor antagonist 4
    		Antagonist
    Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD).
    Mu opioid receptor antagonist 4
  • HY-P10177
    Acetalin-3
    		Antagonist
    Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors.
    Acetalin-3
  • HY-P5892
    β-Endorphin (1-27) (human)
    		Antagonist
    β-Endorphin (1-27) (human) is an opioid antagonist that binds μ-, δ-, and κ-opioid receptors with Kis of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia.
    β-Endorphin (1-27) (human)
  • 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-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-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-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-122561
    MK-1925
    		Antagonist
    MK-1925 is an orally active, CNS-penetrant ORL1 receptor antagonist with an IC50 of 8.2 nM. MK-1925 selectively inhibits the ORL1 receptor and shows no significant activity against other opioid receptors or the hERG potassium channel.
    MK-1925
  • HY-176505
    NOP antagonist 1
    		Antagonist
    NOP antagonist 1 (Compound (-)-31) is a nociceptin opioid peptide (NOP) antagonist with a Kb of 8.65  nM. NOP antagonist 1 can be used for neuropsychiatric disorders research.
    NOP antagonist 1
  • HY-162669
    Mu opioid receptor antagonist 8
    		Antagonist
    Mu opioid receptor antagonist 8 (368) is a μ-opioid receptor antagonist. Mu opioid receptor antagonist 8 (368) significantly inhibits met-enkephalin-induced µOR activation of Gi.
    Mu opioid receptor antagonist 8
  • HY-118615
    LY2048978
    		Antagonist
    LY2048978 is a non-selective opioid receptor antagonist with Ki of 0.287, 0.471 and 1.05 nM for human mu, kappa and delta opioid receptors in vitro, respectively. LY2048978 can be used in the research of major depressive disorder and alcohol use disorder.
    LY2048978
  • HY-144610
    Mu opioid receptor antagonist 5
    		Antagonist
    Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD).
    Mu opioid receptor antagonist 5
  • HY-158236
    ORL1 antagonist 2
    		Antagonist
    ORL1 antagonist 2 (1B) is an opioid receptor-Like 1 (ORL1) antagonist, usd in P-glycoprotein (P-gp) research.
    ORL1 antagonist 2
  • HY-175661
    SRI-22136
    		Antagonist
    SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC50 of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC50 = 370 nM), KOR (IC50 = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist) (HY-105343) (IC50 = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease.
    SRI-22136
  • HY-P2669
    Boc-YPGFL(O-tBu)
    		Antagonist
    Boc-YPGFL(O-tBu) is a selective δ opioid receptor (DOR) peptide antagonist.
    Boc-YPGFL(O-tBu)
  • HY-158290
    Natrexone/BSA
    		Antagonist
    Natrexone/BSA is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    Natrexone/BSA
  • HY-144608
    Mu opioid receptor antagonist 3
    		Antagonist
    Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD).
    Mu opioid receptor antagonist 3
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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