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-120645
    BMS-986122
    		Agonist 99.94%
    BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (μ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes.
    BMS-986122
  • 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-P1334
    DPDPE
    		Agonist 99.83%
    DPDPE, an opioid peptide, is a selective δ-opioid receptor?(DOR) agonist?with anticonvulsant effects.
    DPDPE
  • HY-17609
    Difelikefalin
    		Agonist 99.50%
    Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
    Difelikefalin
  • HY-114452
    LY2940094
    		Antagonist 99.91%
    LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models.
    LY2940094
  • HY-P0244
    Dermorphin
    		Agonist 99.96%
    Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.
    Dermorphin
  • HY-101386
    PZM21
    		Agonist 99.46%
    PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
    PZM21
  • HY-15536
    Cebranopadol
    		Agonist 98.46%
    Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.
    Cebranopadol
  • HY-124754
    Navacaprant
    		Inhibitor 99.97%
    Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy.
    Navacaprant
  • HY-P0185
    Endomorphin 1
    		Agonist 99.92%
    Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties.
    Endomorphin 1
  • HY-18618A
    SB-612111 hydrochloride
    		Inhibitor 99.26%
    SB-612111 hydrochloride hydrochloride is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.
    SB-612111 hydrochloride
  • HY-N0923
    Corydaline
    		Agonist 99.70%
    Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioid receptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities.
    Corydaline
  • HY-P1335A
    CTAP TFA
    		Antagonist 99.56%
    CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction.
    CTAP TFA
  • HY-12844
    Ro 64-6198
    		Agonist 99.82%
    Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia.
    Ro 64-6198
  • HY-P1336
    Deltorphin I
    		Agonist
    Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.
    Deltorphin I
  • HY-P1701
    Morphiceptin
    		98.29%
    Morphiceptin is a potent and specific agonist for morphine (μ) receptors. Morphiceptin, as a synthetic peptide, is the amide of a fragment of the milk protein β-casein. Morphiceptin has morphinelike activities and is highly specific for morphine (μ) receptors but not for enkephalin (⸹) receptors.
    Morphiceptin
  • HY-G0021
    N-Desmethylclozapine
    		Agonist 98.99%
    N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
    N-Desmethylclozapine
  • HY-120613
    BMS-986187
    		Activator 98.93%
    BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (∼1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC50=3 μM).
    BMS-986187
  • HY-P1467A
    [Met5]-Enkephalin, amide TFA
    		Agonist 99.58%
    [Met5]-Enkephalin, amide TFA is an agonist for δ opioid receptors as well as putative ζ (zeta) opioid receptors.
    [Met5]-Enkephalin, amide TFA
  • HY-P0186A
    Endomorphin 2 TFA
    		Agonist 99.43%
    Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
    Endomorphin 2 TFA
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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