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-120927A
    Alvimopan metabolite hydrochloride
    		Antagonist 99.93%
    Alvimopan metabolite hydrochloride is a peripherally restricted Opioid Receptor antagonist that inhibits the amplitude of electrically evoked contractions and spontaneous mechanical activity in guinea pig ileum.
    Alvimopan metabolite hydrochloride
  • HY-150332
    N-Propionitrile Chlorphine hydrochloride
    		98.2%
    N-Propionitrile Chlorphine hydrochloride is structurally similar to known opioids.
    N-Propionitrile Chlorphine hydrochloride
  • HY-107749
    ML 190
    		Antagonist 99.60%
    ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively.
    ML 190
  • HY-108229S
    6β-Naltrexol-d3
    		Antagonist 99.72%
    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-P1013
    Deltorphin 2
    		Agonist
    Deltorphin 2 is a selective peptide agonist for the δ opioid receptor.
    Deltorphin 2
  • HY-17609S1
    Difelikefalin-d5 hydrochloride
    		Agonist
    Difelikefalin-d5 (CR-845-d5) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) 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> hydrochloride
  • HY-123534
    CYT-1010
    		Agonist 99.28%
    CYT-1010 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
  • HY-128038
    N-Desmethyl-loperamide
    		Activator 98.36%
    N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein.
    N-Desmethyl-loperamide
  • HY-124959
    Spiradoline mesylate
    		Agonist 99.95%
    Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier.
    Spiradoline mesylate
  • HY-107094
    MT-7716 hydrochloride
    		Agonist 99.06%
    MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.
    MT-7716 hydrochloride
  • HY-145128
    GR103545 fumarate
    		Agonist
    GR103545 is a potent and selective agonist of the κ-opioid receptor (κ-OR). 11GR103545 is a radiotracer for imaging κ-OR in vivo[1]
    GR103545 fumarate
  • HY-169450
    (-)-9-Hydroxycorynantheidine
    		Agonist 99.2%
    (-)-9-Hydroxycorynantheidine (9-O-Desmethyl mitragynine), the 9-demethyl analogue of Mitragynine, is a selective and partial agonist of μ-opioid receptor. (-)-9-Hydroxycorynantheidine inhibits electrically stimulated twitch contraction in guinea-pig ileum.
    (-)-9-Hydroxycorynantheidine
  • HY-P1171
    N-terminally acetylated Endomorphin-1
    		Control 99.20%
    N-terminally acetylated Endomorphin-1 is a modified Endomorphin-1.
    N-terminally acetylated Endomorphin-1
  • HY-120949
    (1R,2R)-U-50488 hydrochloride
    		Agonist 99.14%
    (1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist.
    (1R,2R)-U-50488 hydrochloride
  • HY-15997C
    (±)-U-50488 hydrate hydrochloride
    		Agonist 99.76%
    (±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist.
    (±)-U-50488 hydrate hydrochloride
  • HY-110302
    6'-GNTI dihydrochloride
    		Agonist 99.54%
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
    6'-GNTI dihydrochloride
  • HY-112692
    AT-121
    		Agonist 98.01%
    AT-121 is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects.
    AT-121
  • HY-101317
    TAN-67 dihydrobromide
    		Agonist 99.20%
    TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a Ki value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke.
    TAN-67 dihydrobromide
  • HY-P1626
    Acetyl tetrapeptide-15
    		Agonist 99.64%
    Acetyl tetrapeptide-15 is a synthetic peptide. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway. Acetyl tetrapeptide-15 is used in the cosmetics for sensitive skin.
    Acetyl tetrapeptide-15
  • HY-P2046
    β-Endorphin (rat)
    		Modulator
    β-Endorphin (rat) is an endogenous opioid neuropeptide and peptide hormone. β-Endorphin (rat) has analgesic activity and also contributes to food intake in satiated rats. β-Endorphin (rat) can be used in the research of neurological diseases such as analgesia and drug addiction.
    β-Endorphin (rat)
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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