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-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-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-108229
    6β-Naltrexol
    		Antagonist
    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
  • 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
  • HY-P1599
    Valorphin
    Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM; Valorphin also shows anti-tumor activity.
    Valorphin
  • HY-105525A
    Sameridine hydrochloride
    		Agonist
    Sameridine hydrochloride is a local anesthetic and local analgesic.
    Sameridine hydrochloride
  • 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 fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate 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 fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate 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>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
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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