The Pharmacological Characterization Of Some New Opioid Ligands

Opiate and opioid drugs have been widely used as analgesics. They also produce some side effects such as respiratory depression, decreased gastrointestinal motility, sedation, dependence and tolerance. Many structurally diverse opiates and opioid compounds have been synthesized aiming to minimize the side effects and to understand the structure-function relationship. To expedite this process, a full understanding of the action of opioid agonists at the cellular level is essential. In this report, some new synthesized opioid ligands have been performed drug assay. Cellular and molecular mechanisms of new opioid ligands were explored by cellular biological techniques and molecular pharmacological methods. First, the binding characteristics of the opioid ligand was studied in cloned δ and μ opioid receptors stably expressed in Chinese hamster ovary cells by saturation binding experiments and by competition bindingexperiments. Then ,the bioassay of the new opioid receptor ligands was performed on isolated organs,such as GP1 and MVD. In addition, the regulation of the new ligands on the δ or μ opioid receptor-coupled AC-cAMP signal transdaction pathway was further explored.1. The binding of new opioid receptor ligands to cloned opioid receptor stably expressed in...