2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Opioid Receptor
  5. Opioid Receptor Antagonist

Opioid Receptor Antagonist

Opioid Receptor Isoform Comparison

Opioid Receptor Antagonists (133):

Cat. No. Product Name Effect Purity
  • HY-17417
    Naloxone hydrochloride
    		Antagonist 99.96%
    Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias.
  • HY-100903
    Norbinaltorphimine dihydrochloride
    		Antagonist 98.91%
    Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain.
  • HY-17417A
    Naloxone
    		Antagonist 99.71%
    Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias.
  • HY-101718
    Aticaprant
    		Antagonist 99.59%
    Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
  • HY-76711
    Naltrexone
    		Antagonist 99.94%
    Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
  • HY-10487
    JDTic dihydrochloride
    		Antagonist 98.03%
    JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
  • HY-13274
    JTC-801
    		Antagonist 98.67%
    JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM.
  • HY-101302
    Naltriben mesylate
    		Antagonist 99.65%
    Naltriben mesylate is a potent δ2-opioid receptor antagonist and a TRPM7 activator. Naltriben mesylate shows Ki values of 0.013 nM, 19 nM and 152 nM for δ, μ and κ receptors, respectively. Naltriben mesylate enhances glioblastoma cell migration and invasion. Naltriben mesylate can be used in research into neurological diseases and cancer.
  • HY-A0118A
    Naloxegol oxalate
    		Antagonist 99.91%
    Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is an orally active peripherally acting μ-opioid receptor antagonist with a target Ki of 7.42 nM. Naloxegol oxalate inhibits the binding of opioids to μ-opioid receptors in the gastrointestinal tract, and alleviates opioid-induced gastrointestinal hypomotility, delayed transit, hypertonicity, and increased fluid reabsorption. Naloxegol oxalate is applicable to research related to opioid-induced constipation.
  • HY-19627A
    Naldemedine tosylate
    		Antagonist
    Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine can be used in opioid-induced constipation (OIC) research. Naldemedine tosylate is predicted to bind to 3CLpro encoded by SARS-CoV2 genome.
  • HY-117040
    nor-Binaltorphimine
    		Antagonist 98.70%
    nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain.
  • HY-P1335A
    CTAP TFA
    		Antagonist 99.60%
    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.
  • HY-13243
    Alvimopan
    		Antagonist 98.42%
    Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus.
  • HY-114452
    LY2940094
    		Antagonist 99.17%
    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.
  • HY-137279
    Naloxone methiodide
    		Antagonist 99.7%
    Naloxone methiodide is a peripherally restricted, nonselective, and competitive opioid receptor antagonist. Naloxone methiodide does not penetrate the blood-brain barrier.
  • HY-101318
    β-Funaltrexamine hydrochloride
    		Antagonist 99.07%
    β-Funaltrexamine (β-FNA) hydrochloride is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine hydrochloride inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine hydrochloride inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine hydrochloride is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases.
  • HY-P1329A
    CTOP TFA
    		Antagonist 99.84%
    CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity.
  • HY-107721
    (±)-J-113397
    		Antagonist 99.82%
    (±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a Ki of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ.
  • HY-136208
    TAN-452
    		Antagonist 99.16%
    TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
  • HY-13222
    BAN ORL 24
    		Antagonist 99.68%
    BAN ORL 24 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 can be used for the research of cancer and analgesic.