2. Signalwege
  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
Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • HY-10486
    JDTic
    		Antagonist
    JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (Ki=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal.
    JDTic
  • HY-11051
    JNJ-20788560
    		Agonist 98.05%
    JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia.
    JNJ-20788560
  • 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
  • HY-76711S
    Naltrexone-d4
    		Antagonist 99.82%
    Naltrexone-d4 is deuterium labeled Naltrexone (HY-76711). Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
    Naltrexone-d<sub>4</sub>
  • HY-122489A
    (S)-Laudanosine
    		Control 99.95%
    (S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM).
    (S)-Laudanosine
  • HY-120927
    Alvimopan metabolite
    Alvimopan metabolite is a μ opioid receptor antagonist with activity that selectively interacts with μ peripheral receptors. Alvimopan metabolite can be used as a potential inhibitory drug to alleviate the side effects caused by opioids. Alvimopan metabolite was identified as a highly selective μ opioid receptor antagonist during research and development.
    Alvimopan metabolite
  • HY-15691A
    PF-4455242 hydrochloride
    		Antagonist 99.01%
    PF-4455242 hydrochloride is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-4455242 hydrochloride blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-4455242 hydrochloride promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-4455242 hydrochloride attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-4455242 hydrochloride can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal.
    PF-4455242 hydrochloride
  • HY-15691
    PF-04455242
    		Antagonist
    PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal.
    PF-04455242
  • HY-123534A
    CYT-1010 hydrochloride
    		Agonist
    CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively.
    CYT-1010 hydrochloride
  • HY-19876
    PL37
    		Agonist
    PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities). PL37 exerts its anti-hyperalgesic effects by activating μ-opioid receptors (µ-opioid receptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain.
    PL37
  • HY-113929R
    Loperamide oxide (Standard)
    		Agonist
    Loperamide oxide (Standard) is the analytical standard of Loperamide oxide. This product is intended for research and analytical applications. Loperamide oxide (R-58425) is a orally active prodrug of the Loperamide (HY-156131). Loperamide oxide incubation with the contents of the intestinal lumen inhibits fluid secretion under aerobic conditions.
    Loperamide oxide (Standard)
  • HY-107747A
    GR 89696 free base
    		Agonist
    GR 89696 free base is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus.
    GR 89696 free base
  • HY-115066A
    GSK1521498 free base hydrochloride
    		Antagonist
    GSK1521498 free base (hydrochloride) is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and agents.
    GSK1521498 free base hydrochloride
  • HY-106189
    CCI-1008
    		Agonist
    CCI-1008 is an opioid receptor agonist. CCI-1008 can be used for research on nervous system diseases.
    CCI-1008
  • HY-12392A
    Iprindole hydrochloride
    		Agonist
    Iprindole hydrochloride, an opioid receptor agonist, is a tricyclic antidepressant. Iprindole hydrochloride shortens the immobility time in mice forced swimming test, which can be reversed by the opiate antagonist Naloxone (HY-17417A). Iprindole hydrochloride induces lamellar body formation but devoid of lamellar bodies. Iprindole hydrochloride can be used for the research of depression.
    Iprindole hydrochloride
  • HY-P1338A
    PL-017 TFA
    		Agonist
    PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats.
    PL-017 TFA
  • HY-156614
    Icalcaprant
    		Antagonist
    Icalcaprant is a kappa-opioid receptor antagonist.
    Icalcaprant
  • HY-181103
    ERG-IN-6
    		Activator
    ERG-IN-6 (compound (+)-(S)-5a) is a μ-opioid receptor activator with an EC50 of 0.12 nM. ERG-IN-6 also is a hERG (Kv11.1) potassium channel inhibitor with an IC50 of 0.681 μM. ERG-IN-6 can be used for the research of pain.
    ERG-IN-6
  • HY-106732
    AT-076
    		Antagonist
    AT-076 is an opioid pan antagonist at nociception, kappa, mu, and delta opioid receptors, with Ki values of 1.75 nM (NOP), 1.67 nM (MOP), 1.14 nM (KOP) and 19.6 nM (DOP), respectively.
    AT-076
  • HY-106601A
    Picenadol hydrochloride
    Picenadol (LY-150720) hydrochloride is an opioid mixed agonist-antagonist analgesic. Picenadol hydrochloride is an external racemic mixture, where its d-isomer (LY136596) is a potent μ-opioid receptor agonist, and the l-isomer (LY136595) is a weak μ-receptor competitive antagonist, which can inhibit the agonist effect and reduce the risk of dependence. Picenadol hydrochloride has anticholinergic activity.
    Picenadol hydrochloride
Art. -Nr. Produktname / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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