Uniform assessment and ranking of opioid Mu receptor binding constants for selected opioid drugs

摘要: The safe disposal of unused opioid drugs is an area regulatory concern. While toilet flushing recommended for some to prevent accidental exposure, there a need data that can support more consistent policy based on assessment relative risk. For acting at the Mu-opioid receptor (MOR), published measurements binding affinity (K(i)) are incomplete and inconsistent due differences in methodology assay system, leading wide range values same drug thus precluding simple meaningful ranking potency. Experiments were conducted obtain K(i)'s 19 approved using single cell membrane preparation expressing recombinant human MOR. K(i) obtained ranged from 0.1380 nM (sufentanil) 12.486 μM (tramadol). separated into three categories upon their values: > 100 (tramadol, codeine, meperidine, propoxyphene pentazocine), K(i)=1-100 (hydrocodone, oxycodone, diphenoxylate, alfentanil, methadone, nalbuphine, fentanyl morphine) < 1 (butorphanol, levorphanol, oxymorphone, hydromorphone, buprenorphine sufentanil). These add understanding pharmacology development labeling policies regarding disposal.