2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Opioid Receptor

Opioid Receptor

Opioid Receptor

Related Products

PDF 2.35 MB

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-B0418AR
    Loperamide (hydrochloride) (Standard)
    		Agonist 99.89%
    Loperamide (hydrochloride) (Standard) is the analytical standard of Loperamide (hydrochloride). This product is intended for research and analytical applications. Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist. Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect.
    Loperamide (hydrochloride) (Standard)
  • HY-101011
    Naloxonazine dihydrochloride
    		Antagonist 98.1%
    Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity.
    Naloxonazine dihydrochloride
  • HY-P1337A
    Dynorphin B (1-13) TFA
    		Agonist
    Dynorphin B (1-13) TFA acts as an agonist on opioid κ-receptor.
    Dynorphin B (1-13) TFA
  • HY-13243
    Alvimopan
    		Antagonist 98.66%
    Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus.
    Alvimopan
  • HY-120511
    KNT-127
    		Agonist 99.60%
    KNT-127 is a potent δ-opioid receptor agonist that crosses the blood-brain barrier (BBB). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 has analgesic, antidepressant and antianxiety activities.
    KNT-127
  • HY-101205
    ICI 199441
    		Agonist 99.39%
    ICI 199441 is a potent and selective κ-opioid receptor agonist. ICI 199441 can improve heart resistance to ischemia/reperfusion.
    ICI 199441
  • HY-101230
    ICI 174864
    		99.97%
    ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist-tifluadom.
    ICI 174864
  • HY-P1302
    Orphanin FQ(1-11)
    		Agonist 99.52%
    Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice.
    Orphanin FQ(1-11)
  • HY-P0185A
    Endomorphin 1 acetate
    		Agonist 99.92%
    Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties.
    Endomorphin 1 acetate
  • HY-123689
    Samidorphan
    		Antagonist 99.04%
    Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo.
    Samidorphan
  • HY-123689
    Samidorphan
    		Modulator 99.04%
    Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo.
    Samidorphan
  • HY-107744
    Nalmefene
    		Modulator 99.70%
    Nalmefene is a BBB-penatrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders.
    Nalmefene
  • HY-111454
    SR17018
    		Agonist 98.01%
    SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.
    SR17018
  • HY-107722
    SCH 221510
    		Agonist 99.00%
    SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC50 of 12 nM and Ki of 0.3 nM. SCH 221510 shows an anxiolytic-like effect.
    SCH 221510
  • 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-P3609
    CR 665
    		Agonist 99.65%
    CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain.
    CR 665
  • HY-15708
    LY2795050
    		Antagonist 98.68%
    LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction.
    LY2795050
  • HY-101039A
    AR-M 1000390 hydrochloride
    		Agonist 98.20%
    AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
    AR-M 1000390 hydrochloride
  • HY-P0098
    [D-Ala2]leucine-enkephalin
    		Agonist 98.64%
    [D-Ala2]leucine-enkephalin, a delta opioid agonist, is a degradation resistant long-acting Leu-enkephalin.
    [D-Ala2]leucine-enkephalin
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.