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

Opioid Receptor Ligand

Opioid Receptor Isoform Comparison

Opioid Receptor Ligands (8):

Cat. No. Product Name Effect Purity
  • HY-P11642A
    Sialorphin TFA
    		Ligand
    Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.
  • HY-168351
    Fluorphine
    		Ligand 99.1%
    Fluorphine is an analogue of Brorphine and can bind to μ-opioid receptor (MOR) (Ki: 12.5 nM). Fluorphine has GTPγS binding (EC50: 75 nM) and βarrestin 2 recruitment (EC50: 377 nM) activity. Fluorphine induces respiratory depressant effects.
  • HY-168352
    Orphine
    		Ligand 98.2%
    Orphine is an opioid compound. Orphine can enhance the antinociceptive effects in mice that are mitigated by Naloxone (HY-17417).
  • HY-137056
    LY164929
    		Ligand
    LY164929 is a highly selective ligand for the lower affinity [3H]D-Ala2-D-Leu-5-enkephalin binding site, exhibiting 1,986-fold selectivity compared to other ligands.
  • HY-182563
    Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide
    		Ligand
    Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide is a μ/δ opioid receptor ligand with high μ opioid receptor selectivity and agonist activity. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide has an IC50 of 237 nM for μ receptors and 1050 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide shows Ki values of 17 nM for μ receptors and 480 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide inhibits electrically evoked contractions of guinea pig ileum and mouse vas deferens. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide serves as a starting compound for structure-activity relationship investigations of μ receptor recognition.
  • HY-P11642
    Sialorphin
    		Ligand
    Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.
  • HY-169469
    N-Phenethylnoroxymorphone
    		Ligand
    N-Phenethylnoroxymorphone is an opioid compound. N-Phenethylnoroxymorphone enhances morphine-induced analgesia in rats. N-Phenethylnoroxymorphone can be used for research on neurological diseases.
  • HY-W714505
    AH 7563
    		Ligand
    AH 7563 structurally belongs to the opioid compounds and exhibits analgesic activity. In the phenylquinone test and hot plate test, the ED50 of AH 7563 for analgesia in mice were 15.3 mg/kg (orally) and 15.5 mg/kg (subcutaneous injection), respectively.