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-P1335
    CTAP
    		Antagonist 99.30%
    CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction.
    CTAP
  • HY-76657A
    Alvimopan dihydrate
    		Antagonist 98.66%
    Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus.
    Alvimopan dihydrate
  • 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 can improve the behavior of depressed animals.
    Samidorphan
  • HY-114072
    J-113397
    		Antagonist 99.00%
    J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors.
    J-113397
  • HY-115066
    GSK1521498 free base
    		Antagonist 99.79%
    GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base has the potential for disorders of compulsive consumption of food, alcohol, and agents.
    GSK1521498 free base
  • HY-101376
    (+)-N-Allylnormetazocine hydrochloride
    		Antagonist 99.6%
    (+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease.
    (+)-N-Allylnormetazocine hydrochloride
  • HY-P1299A
    UFP-101 TFA
    		Antagonist 99.36%
    UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect.
    UFP-101 TFA
  • HY-17417R
    Naloxone hydrochloride (Standard)
    		Antagonist
    Naloxone (hydrochloride) (Standard) is the analytical standard of Naloxone (hydrochloride). This product is intended for research and analytical applications. Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias.
    Naloxone 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-107748
    5'-Guanidinonaltrindole hydrochloride
    		Antagonist 98.65%
    5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor.
    5'-Guanidinonaltrindole hydrochloride
  • HY-15708
    LY2795050
    		Antagonist 98.12%
    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-100122
    Bevenopran
    		Antagonist 99.09%
    Bevenopran is a peripheral μ-opioid receptor antagonist.
    Bevenopran
  • HY-114452A
    LY2940094 tartrate
    		Antagonist 99.66%
    LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.
    LY2940094 tartrate
  • HY-168366
    R-6890
    		Antagonist 99.59%
    R-6890 is a Brorphine-related opioid receptor antagonist that exhibits differential binding activities toward rat opioid receptors (IC50=4.6 nM (0.05 M Tris; pH 7.4) and 170 nM (0.05 M Tris+0.1 M NaCl)). R-6890 displaces bound labeled opioids from receptors, and its binding affinity is affected by environmental factors, decreasing in the presence of NaCl. R-6890 crosses the blood-brain barrier (BBB) and exerts analgesic effects in the warm water-induced tail-flick reflex model of male Wistar rats.
    R-6890
  • HY-16765A
    Axelopran sulfate
    		Antagonist 99.14%
    Axelopran sulfate is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
    Axelopran sulfate
  • HY-118949
    LY255582
    		Antagonist 98.0%
    LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity.
    LY255582
  • 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-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-118416
    BMS-986124
    		Antagonist 99.00%
    BMS-986124 is a μ-opioid receptor silent allosteric modulator (μ-SAMs). BMS-986124 antagonizes positive allosteric modulator effect of BMS-986122 (µ-OR PAM).
    BMS-986124
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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