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

Opioid Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P0318
    Hemorphin-7
    Activator
    Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).
    Hemorphin-7
  • HY-P1334A
    DPDPE TFA
    Agonist 99.94%
    DPDPE TFA, an opioid peptide, is a selective δ-opioid receptor (DOR) agonist with anticonvulsant effects.
    DPDPE TFA
  • HY-P1596
    Gluten Exorphin C
    Inhibitor 99.86%
    Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.
    Gluten Exorphin C
  • HY-107384
    Asimadoline
    Agonist 99.36%
    Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).
    Asimadoline
  • HY-107743
    Naloxone benzoylhydrazone
    Modulator ≥99.0%
    Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect.
    Naloxone benzoylhydrazone
  • HY-A0118
    Naloxegol
    Antagonist
    Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
    Naloxegol
  • HY-126941
    Hecogenin acetate
    99.30%
    Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors.
    Hecogenin acetate
  • HY-15536A
    Cebranopadol ((1α,4α)stereoisomer)
    Cebranopadol ((1α,4α)stereoisomer) is a stereoisomer of cebranopadol. Cebranopadol is a potent agonist activity on ORL-1.
    Cebranopadol ((1α,4α)stereoisomer)
  • HY-12698
    NNC 63-0532
    Agonist 99.81%
    NNC63-0532 is a novel non-peptide nociceptin receptor (ORL1) agonist, with EC50s of 305?nM. NNC63-0532 plays important roles in many disorders such as pain, drug addiction.
    NNC 63-0532
  • HY-135230
    LY2444296
    Antagonist 99.59%
    LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects.
    LY2444296
  • HY-P4053
    Dalargin
    Agonist 99.52%
    Dalargin is a potent δ-opioid receptor agonist. Dalargin mitigates Gentamicin (HY-A0276)-induced cell death. Dalargin shows nephroprotective effects on Gentamicin-induced kidney injury. Dalargin shows antiulcer activity.
    Dalargin
  • HY-106147B
    Frakefamide TFA
    Agonist 99.18%
    Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
    Frakefamide TFA
  • HY-13716A
    Noscapine hydrochloride
    Agonist 99.99%
    Noscapine ((S,R)-Noscapine) hydrochloride is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
    Noscapine hydrochloride
  • HY-114072A
    (S,S)-J-113397
    Antagonist 99.87%
    (S,S)-J-113397 is an isomer of J-113397 (HY-114072). J-113397 is an Opioid Receptor antagonist.
    (S,S)-J-113397
  • HY-P1481A
    β-Casomorphin, human TFA
    Agonist 99.67%
    β-Casomorphin, human TFA (Human β-casomorphin 7 TFA) is an opioid peptide, acts as an agonist of opioid receptor.
    β-Casomorphin, human TFA
  • HY-N2304A
    Methyl-6-alpha-Naltrexol
    Antagonist
    Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioid receptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract.
    Methyl-6-alpha-Naltrexol
  • HY-123689S1
    Samidorphan-d5
    Antagonist
    Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo.
    Samidorphan-d<sub>5</sub>
  • HY-132428S
    O-Desmethyl Tramadol-d6
    O-Desmethyl Tramadol-d6 is the deuterium labeled O-Desmethyl Tramadol. O-Desmethyl Tramadol is a primary active metabolite of Tramadol. O-Desmethyl Tramadol is mainly responsible for its µ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme[1].
    O-Desmethyl Tramadol-d<sub>6</sub>
  • HY-76657
    Alvimopan monohydrate
    Antagonist 99.18%
    Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus.
    Alvimopan monohydrate
  • HY-101582
    ZT 52656A hydrochloride
    Agonist 99.98%
    ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye.
    ZT 52656A hydrochloride
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