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-P1331
    BAM-22P
    		Agonist
    BAM-22P, a highly potent opioid peptide, is a potent opioid agonist.
    BAM-22P
  • HY-P3555
    D-Ala-Gly-Phe-Met-NH2
    		Agonist
    D-Ala-Gly-Phe-Met-NH2, an opioid peptide, is a potent opiate δ-receptor agonist.
    D-Ala-Gly-Phe-Met-NH2
  • HY-P4679
    (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8)
    		Agonist
    (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist.
    (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8)
  • HY-117091
    DDD-028
    DDD-028 is a potent non-opioid, non-cannabinoid analgesic which attenuates neuropathic and inflammatory pain without the possible side effects or abuse potential associated with opioid or cannabinoid activities. DDD-028 can be utilized in analgesic research.
    DDD-028
  • 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-P1793
    α-Casein (90-95)
    		Agonist 99.51%
    α-Casein (90-95) is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) can be used in the study of the mechanisms of allergic diseases and prostate cancer.
    α-Casein (90-95)
  • 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-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-101233
    ICI 154129
    ICI 154 129 is a delta-opioid receptor antagonist and can be used for seizure research.
    ICI 154129
  • HY-105604
    Anilopam
    		Agonist
    Anilopam is an opioid analgesic belonging to the benzazepine class and acts as an agonist at opioid receptors.
    Anilopam
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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