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-162728
    RO-76
    		Agonist
    RO-76 is a mu opioid receptor (μOR) selective partial agonist. RO-76 binds to μOR-G-protein complex with an EC50 value of 454 nM. RO-76 reduces β-Arrestin-1/2 recruitment. RO-76 shows antinociception activity.
    RO-76
  • HY-155706
    MOR agonist-2
    		Agonist
    MOR agonist-2 (compound 46) is a antagonist of D3R and agonist of MOR (Ki: 7.26 nM and 564 nM, respectively). MOR agonist-2 has the potential to produce analgesic effects through MOR partial agonism. MOR agonist-2 reduces opioid-misuse liability via D3R antagonism.
    MOR agonist-2
  • HY-P1253
    α-Endorphin (human)
    		Modulator
    α-Endorphin (human) is a neuropeptide, that acts on the central nervous system (CNS) and peripheral nervous system (PNS). α-Endorphin (human) binds μ-opioid receptor, and exhibits analgesic efficacy. α-Endorphin (human) regulates sexual behaviors and pleasure felling.
    α-Endorphin (human)
  • HY-P3517
    β-Endorphin (6-31), human
    		Agonist
    β-Endorphin, an endogenous opioid neuropeptide, is an opioid receptor agonist. β-Endorphin binds preferentially to μ-opioid receptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation.
    β-Endorphin (6-31), human
  • HY-120277
    TIPP
    		Antagonist
    TIPP is a potent and selective δ-opioid antagonist with a Ki value of 1.22 nM.
    TIPP
  • HY-P1577
    Dermorphin Analog
    		Agonist
    Dermorphin Analog is an analog of Dermorphin. Dermorphin is a natural heptapeptide μ-opioid receptor agonist found in amphibian skin.
    Dermorphin Analog
  • HY-B0380S1
    Trimebutine-d5 fumarate
    		Agonist
    Trimebutine-d5 (fumarate) is deuterium labeled Trimebutine.
    Trimebutine-d<sub>5</sub> fumarate
  • HY-P3550
    β-Lipotropin (60-65)
    		Agonist
    β-Lipotropin (60-65) (β-LPH (60-65)), an opioid peptide, is a potent opioid agonist.
    β-Lipotropin (60-65)
  • HY-P0179A
    β-Casomorphin, bovine TFA
    		Agonist
    β-Casomorphin, bovine TFA (β-Casomorphin-7 (bovine) TFA) is a opioid peptide with an IC50 of 14 μM in an Opioid receptors binding assay.
    β-Casomorphin, bovine TFA
  • HY-P5061
    Dynorphin A (1-13) amide
    		Antagonist
    Dynorphin A (1-13) amide is an endogenous opioid peptide that antagonizes morphine-induced analgesia.
    Dynorphin A (1-13) amide
  • HY-P1332
    DSLET
    		Agonist
    DSLET ([D-Ser2, Leu5, Thr6]-enkephalin) is a highly specific agonist of the δ-receptor. DSLET is an enkephalin-related peptide selectively bound to the δ opioid receptor.
    DSLET
  • HY-P1481
    β-Casomorphin, human
    		Agonist
    is an opioid peptide, acts as an agonist of opioid receptor.
    β-Casomorphin, human
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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