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-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-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-168366
    R-6890
    R-6890 is an opiate compound with analgesic potencies.
    R-6890
  • HY-101392A
    Harmane hydrochloride
    		Inhibitor 99.35%
    Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harmane hydrochloride
  • 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-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-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 99.32%
    Naltrexone-d4 is deuterium labeled Naltrexone.
    Naltrexone-d<sub>4</sub>
  • HY-122489A
    (S)-Laudanosine
    		Control 99.95%
    (S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM).
    (S)-Laudanosine
  • 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-10486
    JDTic
    		Antagonist
    JDTic is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.
    JDTic
  • HY-139583
    Sunobinop
    		Modulator
    Sunobinop (S 117957) is a modulator of the opioid receptor-like orphan receptor (ORL1).
    Sunobinop
  • HY-123534A
    CYT-1010 hydrochloride
    		Agonist
    CYT-1010 hydrochloride 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 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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