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

Opioid Receptor Antagonist

Opioid Receptor Antagonists (60):

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-101718
    Aticaprant
    		Antagonist 99.87%
    Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 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-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-10487
    JDTic dihydrochloride
    		Antagonist 98.01%
    JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
  • HY-76711
    Naltrexone
    		Antagonist 99.94%
    Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system.
  • HY-136208
    TAN-452
    		Antagonist 99.44%
    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-101376
    (+)-N-Allylnormetazocine hydrochloride
    		Antagonist ≥99.0%
    (+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease.
  • HY-A0118A
    Naloxegol oxalate
    		Antagonist 99.91%
    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.
  • HY-107744
    Nalmefene
    		Antagonist 99.70%
    Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence.
  • HY-15708
    LY2795050
    		Antagonist 98.68%
    LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction.
  • HY-117040
    nor-Binaltorphimine
    		Antagonist 98.70%
    nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo.
  • HY-13243
    Alvimopan
    		Antagonist 98.66%
    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-123689
    Samidorphan
    		Antagonist 99.04%
    Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo.
  • HY-17417A
    Naloxone
    		Antagonist
    Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias.
  • HY-19627
    Naldemedine
    		Antagonist
    Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine 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 is predicted to bind to 3CLpro encoded by SARS-CoV2 genome.
  • HY-A0118
    Naloxegol
    		Antagonist
    Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
  • HY-135230
    LY2444296
    		Antagonist 99.59%
    LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects.
  • 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.
  • 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.