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-106147B
    Frakefamide TFA
    		Agonist 99.18%
    Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
    Frakefamide TFA
  • HY-W000665
    2,6-Dimethyl-L-tyrosine
    		99.94%
    2,6-Dimethyl-L-tyrosine (Dmt) is a tyrosine derivative that enhances receptor affinity, functional bioactivity and in vivo analgesia of opioid peptides.
    2,6-Dimethyl-L-tyrosine
  • HY-B0188S
    Mianserin-d3
    		Activator
    Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy.
    Mianserin-d<sub>3</sub>
  • HY-114072A
    (S,S)-J-113397
    		Antagonist 99.87%
    (S,S)-J-113397 is an isomer of J-113397 (HY-114072). J-113397 is an Opioid Receptor antagonist.
    (S,S)-J-113397
  • HY-13101B
    (S)-MCOPPB
    		Agonist 98.97%
    (S)-MCOPPB is the S-form of MCOPPB (HY-13101). MCOPPB is an orally active and selective agonist of Nociceptin/Orphanin FQ-Receptor. MCOPPB inhibits signaling through the NOP receptor in the mouse brain. MCOPPB can be used for anxiety disorders study.
    (S)-MCOPPB
  • HY-108229
    6β-Naltrexol
    		Antagonist 99.03%
    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-P1481A
    β-Casomorphin, human TFA
    		Agonist 99.67%
    β-Casomorphin, human TFA (Human β-casomorphin 7 TFA) is an opioid peptide, acts as an agonist of opioid receptor.
    β-Casomorphin, human TFA
  • HY-123689S
    Samidorphan-d4
    		Antagonist
    Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).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-d<sub>4</sub>
  • HY-B0505
    Moguisteine
    		Control 99.92%
    Moguisteine???(BBR-2173) is an antitussive compound but has no significant affinity for opiate receptors.
    Moguisteine
  • HY-101307
    BNTX maleate
    		Antagonist 98.2%
    BNTX (7-Benzylidenenaltrexone) maleate is a δ1-opioid receptor antagonist with the Kis of 0.1, 10.8, 13.3, and 58.6 nM for δ1, δ2-, μ-, and κ-opioid receptor, respectively. BNTX maleate shows antinociceptive activity.
    BNTX maleate
  • HY-B0188AR
    Mianserin hydrochloride (Standard)
    		Activator
    Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy.
    Mianserin hydrochloride (Standard)
  • HY-N2304A
    Methyl-6-alpha-Naltrexol
    		Antagonist
    Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioid receptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract.
    Methyl-6-alpha-Naltrexol
  • HY-123689S1
    Samidorphan-d5
    		Antagonist
    Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo.
    Samidorphan-d<sub>5</sub>
  • HY-132428S
    O-Desmethyl Tramadol-d6
    O-Desmethyl Tramadol-d6 is the deuterium labeled O-Desmethyl Tramadol. O-Desmethyl Tramadol is a primary active metabolite of Tramadol. O-Desmethyl Tramadol is mainly responsible for its μ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme.
    O-Desmethyl Tramadol-d<sub>6</sub>
  • HY-168352
    Orphine
    		Ligand 98.2%
    Orphine is an opioid compound. Orphine can enhance the antinociceptive effects in mice that are mitigated by Naloxone (HY-17417).
    Orphine
  • HY-76657
    Alvimopan monohydrate
    		Antagonist 99.18%
    Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus.
    Alvimopan monohydrate
  • HY-11051
    JNJ-20788560
    		Agonist 98.05%
    JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia.
    JNJ-20788560
  • HY-15122R
    Sinomenine (Standard)
    		Activator
    Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
    Sinomenine (Standard)
  • HY-101582
    ZT 52656A hydrochloride
    		Agonist 99.98%
    ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye.
    ZT 52656A hydrochloride
  • HY-76711S
    Naltrexone-d4
    		Antagonist 99.82%
    Naltrexone-d4 is deuterium labeled Naltrexone (HY-76711). Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
    Naltrexone-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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