Opioid Receptor 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.

Fluorphine is an analogue of Brorphine and can bind to μ-opioid receptor (MOR) (K_i: 12.5 nM). Fluorphine has GTPγS binding (EC₅₀: 75 nM) and βarrestin 2 recruitment (EC₅₀: 377 nM) activity. Fluorphine induces respiratory depressant effects.

Orphine is an opioid compound. Orphine can enhance the antinociceptive effects in mice that are mitigated by Naloxone (HY-17417).

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.

Gluten Exorphin A5 is an orally active δ-opioid receptor ligand. Gluten Exorphin A5 exhibits opioid agonist biological activity, analgesic activity, stress-induced analgesia regulatory effects, memory-promoting effects, and non-cytotoxicity. Gluten Exorphin A5 modulates intestinal permeability, can cross in vitro human intestinal epithelial cells via paracellular transport, and resists brush border peptidase hydrolysis. Gluten Exorphin A5 can be used in the research of stress-related processes and cognitive processes.

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 K_i 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.

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.

N-Phenethylnoroxymorphone is an opioid compound. N-Phenethylnoroxymorphone enhances morphine-induced analgesia in rats. N-Phenethylnoroxymorphone can be used for research on neurological diseases.

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.