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-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 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
  • HY-135238
    (rel)-RSD 921
    		Agonist
    (rel)-RSD 921 (PD-117302) is a κ-opioid receptor agonist. (rel)-RSD 921 did not have a greater food-inducing effect in obese than in lean Zucker rats; in both obese and lean Zucker rats, lean rats were more sensitive to its initial food-inducing effect but ultimately ate less.
    (rel)-RSD 921
  • HY-P1320
    [Nphe1]Nociceptin(1-13)NH2
    		Antagonist
    [Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
    [Nphe1]Nociceptin(1-13)NH2
  • HY-14157A
    ADL-5747 hydrochloride
    		Agonist
    ADL-5747 hydrochloride is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 hydrochloride activates these receptors, thereby playing a role in pain management pathways. ADL-5747 hydrochloride can be used for research into pain management mechanisms.
    ADL-5747 hydrochloride
  • HY-W013353
    (RS)-Salsolinol hydrobromide
    		Agonist
    (RS)-Salsolinol hydrobromide is the hydrobromide form of (±)-Salsolinol (HY-113316). (RS)-Salsolinol hydrobromide is a Dopamine (HY-B0451)-derived endogenous metabolite. (RS)-Salsolinol hydrobromide activates μ-opioid receptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA).
    (RS)-Salsolinol hydrobromide
  • HY-106756
    Spiradoline
    		Agonist
    Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier.
    Spiradoline
  • HY-P3087
    Tyr-W-MIF-1
    		Modulator
    Tyr-W-MIF-1 is an opioid tetrapeptide with opiate and antiopiate activity. Tyr-W-MIF-1 can induce analgesia.
    Tyr-W-MIF-1
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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