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

Opioid Receptor

Opioid Receptor

Related Products

PDF 2.35 MB

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-76711
    Naltrexone
    		Antagonist 99.94%
    Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system.
    Naltrexone
  • HY-105343
    BW-180C
    		Agonist 99.92%
    BW-180C ([D-Ala2, D-Leu5]-Enkephalin; DADLE) is an δ opioid receptor (DOR) agonist, which belongs to the enkephalin family. Neuroprotective agent. BW-180C reversibly inhibits cellular transcription in neurons without causing cell injury.
    BW-180C
  • HY-15997
    (-)-U-50488 hydrochloride
    		Inhibitor 99.71%
    (-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioid receptor (MOR) (b>Kd=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+)?trans-(1R,2R) U-50488 (HY-15997A)?or the (±)?trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM).
    (-)-U-50488 hydrochloride
  • HY-13716
    Noscapine
    		Agonist 99.98%
    Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier.
    Noscapine
  • HY-P0088
    Porcine dynorphin A(1-13)
    		Agonist 99.85%
    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-G0021
    N-Desmethylclozapine
    		Agonist 98.99%
    N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
    N-Desmethylclozapine
  • HY-120613
    BMS-986187
    		Activator 99.66%
    BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (～1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC50=3 μM).
    BMS-986187
  • HY-P1336
    Deltorphin I
    		Agonist
    Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.
    Deltorphin I
  • HY-A0118A
    Naloxegol oxalate
    		Antagonist 99.91%
    Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
    Naloxegol oxalate
  • HY-P0186A
    Endomorphin 2 TFA
    		Agonist 99.43%
    Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
    Endomorphin 2 TFA
  • 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-P1594A
    Dynorphin A (1-10) (TFA)
    		Agonist
    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-P1701
    Morphiceptin
    Morphiceptin is a potent and specific agonist for morphine (μ) receptors. Morphiceptin, as a synthetic peptide, is the amide of a fragment of the milk protein β-casein. Morphiceptin has morphinelike activities and is highly specific for morphine (μ) receptors but not for Enkephalin receptors.
    Morphiceptin
  • HY-15997B
    (±)-U-50488 hydrochloride
    		Agonist 99.73%
    (±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist.
    (±)-U-50488 hydrochloride
  • HY-13101
    MCOPPB trihydrochloride
    		Agonist 99.98%
    MCOPPB trihydrochloride is a nociceptin receptor agonist with pKi of 10.
    MCOPPB trihydrochloride
  • HY-B0380A
    Trimebutine maleate
    		Agonist 99.91%
    Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine maleate
  • HY-13222
    BAN ORL 24
    		Antagonist 99.68%
    BAN ORL 24 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 can be used for the research of cancer and analgesic.
    BAN ORL 24
  • HY-137279
    Naloxone methiodide
    		Antagonist 99.7%
    Naloxone methiodide is a peripherally restricted, nonselective, and competitive opioid receptor antagonist. Naloxone methiodide does not penetrate the blood-brain barrier.
    Naloxone methiodide
  • HY-P0179
    β-Casomorphin, bovine
    		Agonist 99.89%
    β-Casomorphin, bovine (β-Casomorphin-7 (bovine) ) is a opioid peptide with an IC50 of 14 μM in an Opioid receptors binding assay.
    β-Casomorphin, bovine
  • HY-136208
    TAN-452
    		Antagonist 99.44%
    TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
    TAN-452
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.