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-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-13716A
    Noscapine hydrochloride
    		Agonist 99.87%
    Noscapine ((S,R)-Noscapine) hydrochloride is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
    Noscapine hydrochloride
  • 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-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-B0505
    Moguisteine
    		Control 99.92%
    Moguisteine???(BBR-2173) is an antitussive compound but has no significant affinity for opiate receptors.
    Moguisteine
  • 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[1].
    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 98.00%
    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-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-107749
    ML 190
    		Antagonist 98.2%
    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-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
  • HY-19876
    PL37
    		Agonist
    PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities). PL37 exerts its anti-hyperalgesic effects by activating μ-opioid receptors (µ-opioid receptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain.
    PL37
  • HY-100845
    Salvinorin A
    		Inhibitor ≥98.0%
    Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with Ki value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum.
    Salvinorin A
  • HY-113929R
    Loperamide oxide (Standard)
    		Agonist
    Loperamide oxide (Standard) is the analytical standard of Loperamide oxide. This product is intended for research and analytical applications. Loperamide oxide (R-58425) is a orally active prodrug of the Loperamide (HY-156131). Loperamide oxide incubation with the contents of the intestinal lumen inhibits fluid secretion under aerobic conditions.
    Loperamide oxide (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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