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-159924
    DBPR116
    		Modulator
    DBPR116 is a prodrug of BPRMU191 (HY-159923) with blood-brain barrier penetration capability. DBPR116 significantly improves the delivery of centrally targeted drugs. In combination with the antagonist Naltrexone (HY-76711), DBPR116 demonstrated superior safety and analgesic efficacy compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a prodrug strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing potential as a safer opioid analgesic.
    DBPR116
  • HY-P6053
    KK-103
    		Agonist
    KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect.
    KK-103
  • HY-130176
    UFP-512
    		Agonist
    UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser363 with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders.
    UFP-512
  • HY-106147
    Frakefamide
    		Agonist
    Frakefamide 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
  • HY-P1618
    LY-281217
    		Agonist
    LY-281217 is a potent mu-opioid agonist with analgesic effects.
    LY-281217
  • HY-A0118AS
    Naloxegol-d5 oxalate
    		Antagonist
    Naloxegol-d5 (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
    Naloxegol-d<sub>5</sub> oxalate
  • HY-P1319A
    Nociceptin(1-7) TFA
    		Agonist
    Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo.
    Nociceptin(1-7) TFA
  • HY-105235
    Enadoline
    		Agonist
    Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects.
    Enadoline
  • HY-P1318A
    Ac-RYYRIK-NH2 TFA
    		Agonist
    Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
    Ac-RYYRIK-NH2 TFA
  • HY-156131
    Loperamide
    		Agonist
    Loperamide (ADL 2-1294) is a selective μ opioid receptor agonist with Kis of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide can be used as an antidiarrheal agent.
    Loperamide
  • HY-170437
    MOR modulator-1
    		Modulator
    MOR modulator-1 (compound 6) is a potent and selective μ opioid receptor (MOR) modulator. MOR modulator-1 exhibits improved opioid receptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with Kis of 0.25, 41.1, 1.30 nM, respectively[1]
    MOR modulator-1
  • HY-163667
    Atoxifent
    		Agonist
    Atoxifent is a potent μ-opioid receptor agonist (EC50=0.39 nM). These receptors are found in brain regions that control pain, emotions, habitual learning, and cognition. Atoxifent exhibits strong analgesic effects and a lower risk of respiratory depression. Atoxifent can be used for research in opioid pharmacology and signal transduction.
    Atoxifent
  • HY-P3634
    [DAla2] Dynorphin A (1-13), amide (porcine)
    [DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system.
    [DAla2] Dynorphin A (1-13), amide (porcine)
  • HY-101039
    AR-M 1000390
    		Agonist
    AR-M 1000390 is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
    AR-M 1000390
  • HY-13716S
    Noscapine-13C,d3
    		Agonist
    Noscapine-13C,d3 is a 13C- labeled and deuterated labeled Noscapine. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier.
    Noscapine-<sup>13</sup>C,d<sub>3</sub>
  • HY-10886
    MCOPPB
    		Agonist
    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 is used in anxiety disorders research.
    MCOPPB
  • HY-P1819
    N-Acetyl-α-Endorphin
    N-Acetyl-α-Endorphin is an acetylated α-Endorphin at N-terminal. α-Endorphin is an endogenous opioid peptide.
    N-Acetyl-α-Endorphin
  • HY-136623
    BW443C
    		Agonist
    BW443C is a selective opioid receptor agonist. BW443C has antinociceptive effect.
    BW443C
  • HY-N0398R
    Sec-O-Glucosylhamaudol (Standard)
    		Inhibitor
    Sec-O-Glucosylhamaudol (Standard) is the analytical standard of Sec-O-Glucosylhamaudol. This product is intended for research and analytical applications. Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect.
    Sec-O-Glucosylhamaudol (Standard)
  • HY-P1299
    UFP-101
    		Antagonist
    UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect.
    UFP-101
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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