Opioid Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S5507 Trimebutine maleate Trimebutine maleate is the maleate salt form of trimebutine, which is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu opioid agonist effects.
E2868 Naloxegol Oxalate Naloxegol oxalate (NKTR-118 oxalate) is a μ-opioid-receptor antagonist with a Ki of 33.8 nM. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
S4588 Docusate Sodium Docusate Sodium (Aerosol OT, Bis(2-ethylhexyl) sulfosuccinate sodium salt, Constonate) is a laxative used to treat constipation, for constipation due to the use of opiates it maybe used with a stimulant laxative, can be taken by mouth or rectally.
E2880 methylnaltrexone bromide Methylnaltrexone bromide is an antagonist of µ-opioid receptor that reduces the viability of lung cancer cells by inhibiting Src activation.
E7162 CTAP CTAP is a potent, highly selective, and blood–brain barrier penetrant antagonist of μ opioid receptor with an IC50 of 3.5 nM. It displays over 1200-fold selectivity over δ opioid and somatostatin receptors. It exhibits anti-dyskinetic potential and can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction.
E7164 β-Endorphin, human β‑Endorphin, human is a prominent endogenous peptide of the hypothalamus and hypophysis cerebri that acts as an agonist of opioid receptors, with preferred affinity for μ‑opioid receptors and δ‑opioid receptors, and exhibits antinociceptive activity.