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-W714509
    AH 8507
    AH 8507 structurally belongs to the opioid compounds and is an analog of AH 7563 (HY-W714505). However, AH 8507 does not exhibit significant analgesic effects in mice in both the phenylquinone test and the hot plate test, with ED50 values greater than 100 mg/kg.
    AH 8507
  • HY-165021
    3,4-Difluoro propyl U-47700
    3,4-Difluoro propyl U-47700 is a utopioid.
    3,4-Difluoro propyl U-47700
  • HY-135032
    Norcarfentanil hydrochloride
    Norcarfentanil hydrochloride is an opioid and is a metabolite of Carfentanil.
    Norcarfentanil hydrochloride
  • HY-B0380R
    Trimebutine (Standard)
    		Agonist
    Trimebutine (Standard) is the analytical standard of Trimebutine (HY-B0380). This product is intended for research and analytical applications. Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine 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 also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine (Standard)
  • HY-156988
    DPI-287
    		Agonist
    DPI-287 is a selective delta-opioid receptor (DOP) agonist with a Ki value of 0.39 nM and can be used for pain research.
    DPI-287
  • HY-169867
    BNTX
    		Antagonist
    BNTX (7-Benzylidenenaltrexone) is a selective δ1-opioid receptor antagonist. BNTX antagonizes the antisecretory actions of DPDPE (HY-P1334), Deltorphin 2 (HY-P1013), and DAMGO (HY-P0210) competitively. BNTX can be used for research of antinociception.
    BNTX
  • HY-123689A
    Samidorphan hydrochloride
    		Modulator
    Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan hydrochloride primarily acts as an opioid receptor antagonist in vivo.
    Samidorphan hydrochloride
  • HY-123689A
    Samidorphan hydrochloride
    		Antagonist
    Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan hydrochloride primarily acts as an opioid receptor antagonist in vivo.
    Samidorphan hydrochloride
  • HY-165000
    3,4-Difluoro isopropyl U-47700
    3,4-Difluoro isopropyl U-47700 is a utopioid.
    3,4-Difluoro isopropyl U-47700
  • HY-170055
    Meta-fluoro 4-ANBP
    Meta-fluoro 4-ANBP (m-Fluoro 4-ANBP) is structurally similar to known opioids.
    Meta-fluoro 4-ANBP
  • HY-17609C
    Difelikefalin acetate
    		Agonist
    Difelikefalin (CR-845; FE-202845) acetate is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin acetate produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
    Difelikefalin acetate
  • HY-135521
    U-49900
    U-49900 is a utopioid.
    U-49900
  • HY-76711S
    Naltrexone-d4
    		Antagonist
    Naltrexone-d4 is deuterium labeled Naltrexone.
    Naltrexone-d<sub>4</sub>
  • HY-119733
    BU09059
    		Antagonist
    BU09059 is a potent and selective Kappa-opioid receptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception.
    BU09059
  • HY-120927
    Alvimopan metabolite
    Alvimopan metabolite is a μ opioid receptor antagonist with activity that selectively interacts with μ peripheral receptors. Alvimopan metabolite can be used as a potential inhibitory drug to alleviate the side effects caused by opioids. Alvimopan metabolite was identified as a highly selective μ opioid receptor antagonist during research and development.
    Alvimopan metabolite
  • HY-156972
    NOP agonist-1
    		Agonist
    NOP agonist-1(compound 4) is a nociceptin opioid receptor (NOP) partial agonist. NOP agonist-1attenuate parkinsonian disabilities in 6-OHDA hemilesioned rats.
    NOP agonist-1
  • HY-130482
    Salvinorin A carbamate
    		Agonist
    Salvinorin A carbamate is an agonist for κ-opioid receptor with an EC50 of 6.2 nM and a Ki of 3.2 nM.
    Salvinorin A carbamate
  • HY-W028263
    6-Hydroxyflavanone
    		Inhibitor
    6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-A receptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes.
    6-Hydroxyflavanone
  • HY-N15180
    Corynantheidine
    Corynantheidine ((-)-Corynantheidine) is a mu-opioid receptor (MOR) partial agonist that shows MOR-dependent analgesic effects in mice.
    Corynantheidine
  • HY-139239
    Bipiperidinyl 4-ANPP
    Bipiperidinyl 4-ANPP is structurally similar to known opioids.
    Bipiperidinyl 4-ANPP
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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