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-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-P3555A
    D-Ala-Gly-Phe-Met-NH2 monoacetate
    		Agonist
    D-Ala-Gly-Phe-Met-NH2 monoacetate, an opioid peptide, is a potent opiate δ-receptor agonist.
    D-Ala-Gly-Phe-Met-NH2 monoacetate
  • 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-111011
    CR 665 acetate
    		Agonist
    CR 665 (JNJ 38488502) acetate is a kappa-opioid agonist that may effectively treat visceral pain by activating receptors on afferent nerves within the gut. CR 665 acetate exhibits peripheral selectivity, differentiating its pharmacokinetic profile from that of non-selective opioids like oxycodone. CR 665 acetate has demonstrated a beneficial effect on visceral pain tolerance thresholds without the delayed analgesic response characteristic of opioids that penetrate the brain. CR 665 acetate is proposed for use in managing postoperative pain due to its pain-relieving properties.
    CR 665 acetate
  • 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
  • HY-163065
    σ1 Receptor/μ Opioid receptor modulator 2
    		Agonist
    σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models.
    σ1 Receptor/μ Opioid receptor modulator 2
  • HY-P5826
    Dynorphin B (1-9)
    Dynorphin B (1-9) is a neuropeptide and N-terminal cleavage product of dynorphin B. The formation of dynorphin B (1-9) is blocked by N-ethylmaleimide (NEM), a non-selective inhibitor of cysteine peptidases.
    Dynorphin B (1-9)
  • HY-167946
    CP-866087
    		Antagonist
    CP-866087 is a new, highly effective, and selective antagonist of the mu-opioid receptor designed for exploring female sexual dysfunction.
    CP-866087
  • HY-170310
    AP-238
    		Agonist
    AP-238 is a a new synthetic opioid (NSO), and acts as an agonist for μ-opioid receptor (MOR) with an EC50 of 248 nM. AP-238 exhibits analgesic activity.
    AP-238
  • HY-P1625
    Daeatal
    Daeatal (Dynorphin A ethylamide (1-9)) is an ethylamine-modified dynorphin fragment that can be used in the study of analgesia, addiction, depression, etc. Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease.
    Daeatal
  • HY-P5131
    [Dmt1]DALDA
    		Agonist
    [Dmt1]DALDA is a potent and long-acting analgesic binds to the mu opioid receptor with high affinity and selectivity. [Dmt1]DALDA is a full agonist at hMOR (Kd = 0.199 nM) and hDOR, but only partial agonist against hKOR.
    [Dmt1]DALDA
  • HY-14356
    ADL5859
    		Agonist
    ADL-5859 is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 can be used for the research of pain.
    ADL5859
  • HY-172979
    DH-1-106
    		Agonist
    DH-1-106 is a MOR partial agonist. DH-1-106 can be used in the study of analgesia.
    DH-1-106
  • HY-123492
    Kentsin
    		Control
    Kentsin (Thr-Pro-Arg-Lys), a contraceptive tetrapeptide, is originally extracted from hamster embryos. Kentsin prevents the maturation of Graafian follicles and consequently inhibits ovulation, without binding to opioid receptors. Kentsin has opiate properties on gastrointestinal motility.
    Kentsin
  • HY-105236
    (Rac)-Enadoline
    		Agonist
    (Rac)-Enadoline ((Rac)-CI-977 free base) is a selective K-opioid receptor agonist that stereoselectively antagonizes clonic seizures induced by slow intravenous injection of N-methyl-DL-aspartate in mice.
    (Rac)-Enadoline
  • HY-105604
    Anilopam
    		Agonist
    Anilopam is an opioid analgesic belonging to the benzazepine class and acts as an agonist at opioid receptors.
    Anilopam
  • HY-159088
    KOR agonist 2
    		Agonist
    KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes.
    KOR agonist 2
  • HY-112692A
    AT-121 hydrochloride
    		Agonist
    AT-121 hydrochloride is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 hydrochloride is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects.
    AT-121 hydrochloride
  • HY-W725190A
    Piperidylthiambutene
    		Agonist
    Piperidylthiambutene is a potent µ-opioid receptor (MOR) agonist with a Ki of 2.75 nM. Piperidylthiambutene exhibits analgesic and antitussive properties and can be utilized in relevant research.
    Piperidylthiambutene
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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