2. シグナル伝達
  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
製品番号 製品名 製品効果 純度 構造式
  • HY-101205A
    ICI-199441 Agonist
    ICI-199441 is a potent and selective κ-opioid receptor agonist with analgesic effects. ICI 199441 can improve heart resistance to ischemia/reperfusion.
    ICI-199441
  • HY-175486
    KOR agonist 6 Agonist
    KOR agonist 6 is a KOR agonist (Ki = 0.25 pM). KOR agonist 6 shows agonistic activity at MOR and DOR in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation. KOR agonist 6 stimulates KOR-mediated [35S]GTPγS binding and inhibits cAMP accumulation in KOR-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects.
    KOR agonist 6
  • HY-P3647A
    [DPro10] Dynorphin A (1-11), porcine hydrochloride Agonist
    [DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property.
    [DPro10] Dynorphin A (1-11), porcine hydrochloride
  • HY-112263
    ORL1 antagonist 1 Antagonist
    ORL1 antagonist 1 is an opioid receptor-like 1 (ORL1) antagonist with an IC50 of 61 nM.
    ORL1 antagonist 1
  • HY-153471
    MOR agonist-1 Agonist
    MOR agonist-1 is a MOR (μ-opioid receptor) agonist. MOR agonist-1 has good analgesic effect. MOR agonist-1 can be used for the research of pain and pain-related disorders.
    MOR agonist-1
  • HY-W725197
    3,4-Difluoro-N,N-didesmethyl U-47700 TFA
    3,4-Difluoro-N,N-didesmethyl U-47700 TFA is an opioid.
    3,4-Difluoro-N,N-didesmethyl U-47700 TFA
  • HY-171236
    FEKAP Agonist
    FEKAP is a brain-penetrant and selective kappa opioid receptor (KOR) agonist (Ki = 0.43 nM) which isotope labeled form exhibits excellent imaging properties. 11C-FEKAP can be utilized as a radiotracer for imaging KOR.
    FEKAP
  • HY-W725208
    2-(Di-sec-butylamino)-1-(1-(2-fluorobenzyl)-1H-pyrrol-2-yl)ethan-1-ol
    2-(Di-sec-butylamino)-1-(1-(2-fluorobenzyl)-1H-pyrrol-2-yl)ethan-1-ol is structurally similar to known opioids.
    2-(Di-sec-butylamino)-1-(1-(2-fluorobenzyl)-1H-pyrrol-2-yl)ethan-1-ol
  • HY-W046349
    N,N-didesmethyl AH 7921
    N,N-didesmethyl AH 7921 is structurally categorized as an opioid metabolite and is a metabolite of AH 7921.
    N,N-didesmethyl AH 7921
  • HY-105343R
    BW-180C (Standard) Agonist
    BW-180C (Standard) is the analytical standard of BW-180C (HY-105343). This product is intended for research and analytical applications. 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 (Standard)
  • HY-126063
    ICI-204448 free acid
    ICI-204448 free acid is a κ-opioid agonist with limited access to the CNS, ICI-204448 free acid can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes.
    ICI-204448 free acid
  • HY-B0380AR
    Trimebutine maleate (Standard) Agonist
    Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. 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 (Standard)
  • HY-90003S
    Tianeptine-d12 Agonist
    Tianeptine-d12 is a deuterated analog of Tianeptine (HY-90003).Tianeptine is an atypical antidepressant. Tianeptine is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
    Tianeptine-d<sub>12</sub>
  • HY-U00420
    Opioid receptor modulator 1 Modulator
    Opioid receptor modulator 1 is a opioid receptor modulator extracted from patent WO2014072809A2, Compound RA11 in EXAMPLE 7.
    Opioid receptor modulator 1
  • HY-N13293
    Isopaynantheine Control
    Isopaynantheine (3-Isopaynantheine), an alkaloid, is an opioid. Isopaynantheine has antinociceptive activity in mice.
    Isopaynantheine
  • HY-114861
    Nor-6α-Oxycodol
    Nor-6α-Oxycodol is structurally similar to known opioids and is a metabolite of Oxycodone.
    Nor-6α-Oxycodol
  • HY-17609S
    Difelikefalin-d5 Agonist
    Difelikefalin-d5 (CR-845-d5) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
    Difelikefalin-d<sub>5</sub>
  • HY-120045
    DuP 747 Agonist
    DuP 747 is a select opioid kappa agonist analgesic amine.
    DuP 747
  • HY-12392R
    Iprindole (Standard) Agonist
    Iprindole (Standard) is the analytical standard of Iprindole. This product is intended for research and analytical applications. Iprindole, an opioid receptor agonist, is a tricyclic antidepressant. Iprindole shortens the immobility time in mice forced swimming test, which can be reversed by the opiate antagonist Naloxone (HY-17417A). Iprindole induces lamellar body formation but devoid of lamellar bodies. Iprindole hydrochloride can be used for the research of depression.
    Iprindole (Standard)
  • HY-19467
    SCH 486757 Agonist
    SCH 486757 is an orally effective pain peptide receptor (NOP) agonist. SCH 486757 can be used for the study of cough.
    SCH 486757
製品番号 製品名 / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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