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-171758
    BU72
    		Agonist
    BU72 is a highly potent and long-acting agonist of μ and κ opioid receptors, and also has a partial agonist effect on δ opioid receptors (EC50 values are 0.054, 0.033, and 0.58 nM, respectively). BU72 has a strong and long-lasting analgesic effect, which is mainly mediated by μ opioid receptors. BU72 has a long-lasting activity and can partially reverse the analgesic effect of morphine. BU72 can be used in the study of opioid dependence.
    BU72
  • HY-130696
    (+)-U-50488
    		Agonist
    (+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997).
    (+)-U-50488
  • HY-P10175
    Acetalin-1
    		Antagonist
    Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors.
    Acetalin-1
  • HY-15997A
    (+)-U-50488 hydrochloride
    		Agonist
    (+)-U-50488 (hydrochloride) (+)-Trans-(1R,2R)-U-50488 hydrochloride) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997).
    (+)-U-50488 hydrochloride
  • HY-P1866
    β-Endorphin, equine
    		Agonist
    β-Endorphin, equine is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors. Analgesic properties.
    β-Endorphin, equine
  • HY-P1329
    CTOP
    		Agonist
    CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity.
    CTOP
  • HY-P1336A
    Deltorphin I TFA
    		Agonist
    Deltorphin I TFA (Deltorphin 1 TFA; Deltorphin C TFA; [D-Ala2] Deltorphin I TFA) is a high-affinity, selective δ-opioid receptor agonist that targets the δ1 and δ2 opioid receptor subtypes. Deltorphin I TFA produces analgesic effects in the rat spinal cord. Deltorphin I TFA increases the pain threshold in rats. Deltorphin I TFA can be used in studies related to nociception (acute pain).
    Deltorphin I TFA
  • HY-P10394
    DP32
    		Agonist
    DP32 is a bifunctional compound that contains an opioid receptor (MOP) agonist and a neuropeptide FF receptor (NPFFR) antagonist. DP32 can be used in analgesia-related research.
    DP32
  • HY-134189
    EST73502
    		Agonist
    EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.
    EST73502
  • HY-16765
    Axelopran
    		Antagonist
    Axelopran (TD-1211) is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
    Axelopran
  • HY-170654
    Opioid receptor antagonist 1
    		Antagonist
    Opioid receptor antagonist 1 (Compound 10) is an Orvinol (HY-D0168)-based opioid receptor antagonist. Opioid receptor antagonist 1 has antagonistic activity to the analgesic properties of Morphine.
    Opioid receptor antagonist 1
  • HY-133717
    Naltriben
    		Antagonist
    Naltriben is a selective δ2-opioid receptor antagonist and TRPM7 activator. Naltriben enhances glioblastoma cell migration and invasion. Naltriben can be used in research into neurological diseases and cancer.
    Naltriben
  • HY-P3870B
    DALDA TFA
    		Agonist
    DALDA TFA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA TFA shows antinociceptive and respiratory effects.
    DALDA TFA
  • HY-B0380S2
    Trimebutine-d3 hydrochloride
    		Agonist
    Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride 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 hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine-d<sub>3</sub> hydrochloride
  • HY-163895
    δ opioid receptor antagonist 1
    		Antagonist
    δ opioid receptor antagonist 1 (compound 6-Cy3) is a fluorescent antagonist probe with high selectivity for δ opioid receptor (DOR) (Ki=1.7 nM). δ opioid receptor antagonist 1 can be used to study the mechanism of pain perception.
    δ opioid receptor antagonist 1
  • HY-107121
    Ondelopran
    		Antagonist
    Ondelopran (LY 2196044) is a non-selective opioid receptor antagonist. Ondelopran inhibits the release of dopamine in the nucleus accumbens induced by alcohol, reduces the rewarding effect of alcohol consumption, and lowers the craving. Ondelopran can be used for alcohol use disorder (AUD).
    Ondelopran
  • HY-101202A
    (Rac)-SNC80
    		Agonist
    (Rac)-SNC80 is a racemate of SNC80 (HY-101202). SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.
    (Rac)-SNC80
  • HY-17417AS
    Naloxone-d5
    Naloxone D5 is deuterium labeled Naloxone. Naloxone is a a potent opioid receptor antagonist.
    Naloxone-d<sub>5</sub>
  • HY-141468
    β-Chlornaltrexamine dihydrochloride
    		Inhibitor
    β-Chlornaltrexamine dihydrochloride (β-CNA dihydrochloride) is a potent long-term opioid receptor blocker. β-Chlornaltrexamine dihydrochloride can effectively block the inhibitory effect of κ opioid receptor agonists on dopamine release. β-Chlornaltrexamine dihydrochloride can be used to study the mechanism of pain perception.
    β-Chlornaltrexamine dihydrochloride
  • HY-173030
    Opioid receptor agonist 1
    		Agonist
    Opioid receptor agonist 1 (Compound 2638-28) is the orally active agonist for opioid receptor that exhibits good affinity to MOR, DOR and KOR with Ki of 5, 24 and 212 nM, respectively. Opioid receptor agonist 1 exhibits analgesic activity in mouse warm water tail flick models and acetic acid writhing models.
    Opioid receptor agonist 1
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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