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-129237
    Azo-enkephalin
    		Activator
    Azo-enkephalin is an endorphin analog with significant analgesic activity. Azo-enkephalin can be used in the development of opioid analgesics.
    Azo-enkephalin
  • HY-161405
    NPFF1-R antagonist 1
    NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively.
    NPFF1-R antagonist 1
  • 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-108229S
    6β-Naltrexol-d3
    		Antagonist
    6β-Naltrexol-d3 (6β-Hydroxynaltrexone-d3) is deuterium labeled 6β-Naltrexol. 6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit.
    6β-Naltrexol-d<sub>3</sub>
  • 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-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-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
  • HY-167842
    22-Thiocyanatosalvinorin A
    		Agonist
    22-Thiocyanatosalvinorin A (RB-64) is a potent and selective kappa-opioid receptor agonist with an EC50 of 0.077 nM.
    22-Thiocyanatosalvinorin A
  • HY-P2199
    SNF 9007
    SNF 9007 is a cholecystokinin analog. SNF 9007 induces analgesia by acting on δ-1, δ-2, and μ opioid receptors in the mouse brain.
    SNF 9007
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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