Experiments on binding affinity of approved opioid drugs to recombinant human mu opioid receptor..

What is it about?

There is a need for data that can support a more consistent disposal policy based on an assessment of relative risk. For drugs acting at the Mu-opioid receptor (MOR), published measurements of binding affinity (Ki) are incomplete and inconsistent due to differences in methodology and assay system, leading to a wide range of values for the same drug thus precluding a simple and meaningful relative ranking of drug potency.

Featured Image

Why is it important?

The Ki values obtained ranged from 0.1380 (sufentanil) to 12.486 lM (tramadol). The drugs were separated into three categories based upon their Ki values: Ki > 100 nM (tramadol, codeine, meperidine, propoxyphene and pentazocine), Ki =1 100 nM (hydrocodone, oxycodone, diphenoxylate, alfentanil, methadone, nalbuphine, fentanyl and morphine) and Ki < 1 nM (butorphanol, levorphanol, oxymorphone, hydromorphone, buprenorphine and sufentanil). These data add to the understanding of the pharmacology of opioid drugs and support the development of a more consistent labeling policies regarding safe disposal.