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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-124754
    Navacaprant
    		Inhibitor 99.97%
    Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy.
    Navacaprant
  • HY-P0088
    Porcine dynorphin A(1-13)
    		Agonist 98.83%
    Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
    Porcine dynorphin A(1-13)
  • HY-P1336
    Deltorphin I
    		Agonist
    Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.
    Deltorphin I
  • HY-P2159
    Dynorphin A (1-8)
    		99.88%
    Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM).
    Dynorphin A (1-8)
  • HY-111454
    SR17018
    		Agonist 98.01%
    SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.
    SR17018
  • HY-P1087
    Adrenorphin
    		Agonist
    Adrenorphin is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM.
    Adrenorphin
  • HY-P1594A
    Dynorphin A (1-10) (TFA)
    		Agonist 98.19%
    Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
    Dynorphin A (1-10) (TFA)
  • HY-19627A
    Naldemedine tosylate
    		Antagonist
    Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine can be used in opioid-induced constipation (OIC) research. Naldemedine tosylate is predicted to bind to 3CLpro encoded by SARS-CoV2 genome.
    Naldemedine tosylate
  • HY-101416
    Vanilpyruvic acid
    		98.28%
    Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid.
    Vanilpyruvic acid
  • HY-12363
    U-69593
    		Agonist ≥99.0%
    U-69593 is a potent and selective κ1-opioid receptor agonist. U-69593 attenuates addictive agent-induced behavioral sensitization in the rat. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum.
    U-69593
  • HY-128865
    BPR1M97
    		Agonist 98.32%
    BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects.
    BPR1M97
  • HY-139690
    CCG258747
    		Inhibitor 99.17%
    CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure.
    CCG258747
  • HY-P1337A
    Dynorphin B (1-13) (TFA)
    		Agonist
    Dynorphin B (1-13) TFA acts as an agonist on opioid κ-receptor.
    Dynorphin B (1-13) (TFA)
  • HY-P1013A
    Deltorphin 2 TFA
    		Agonist 99.88%
    Deltorphin 2 TFA is a selective peptide agonist for the δ opioid receptor.
    Deltorphin 2 TFA
  • HY-13044
    ADL-5859 hydrochloride
    		Agonist 99.77%
    ADL-5859 hydrochloride (compound 20) 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 hydrochloride also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain.
    ADL-5859 hydrochloride
  • HY-120511
    KNT-127
    		Agonist 99.60%
    KNT-127 is a potent and selective δ-opioid receptor agonist effective by systemic administration. KNT-127 shows selectivity for the δ-receptor (Ki 0f 21.3, 0.16, 153 nM for opioid μ-, δ-, and κ-receptors, respectively). KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens and median pre-frontal cortex. Antidepressant-like effects.
    KNT-127
  • HY-107721
    (±)-J-113397
    		Antagonist 98.59%
    (±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a Ki of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ.
    (±)-J-113397
  • HY-101039A
    AR-M 1000390 hydrochloride
    		Agonist 99.05%
    AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
    AR-M 1000390 hydrochloride
  • HY-P1299A
    UFP-101 TFA
    		Antagonist 99.74%
    UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect.
    UFP-101 TFA
  • HY-107747
    GR 89696
    		Agonist 99.88%
    GR 89696 is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus.
    GR 89696
Cat. No. Product Name / Synonyms Application Reactivity