ADL-5859, also known as compound 20, is an opioid drug that is selective for the

δ-opioid receptor The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi alpha subunit, Gi/G0 and has enkephalins as it ...

, it is being investigated as an alternative to traditional opioids in pain management.

Mechanism of action

Like all opioid drugs, ADL-5859 activates opioid receptors, but where as traditional opioids (such as

oxycodone Oxycodone, sold under the brand name Roxicodone and OxyContin (which is the extended-release form) among others, is a semi-synthetic opioid used medically for the treatment of moderate to severe pain. It is highly addictive and is a commonly ...

) activate the three main receptors ( mu,

delta Delta commonly refers to: * Delta (letter) (Δ or δ), the fourth letter of the Greek alphabet * D (NATO phonetic alphabet: "Delta"), the fourth letter in the Latin alphabet * River delta, at a river mouth * Delta Air Lines, a major US carrier ...

, and

kappa Kappa (; uppercase Κ, lowercase κ or cursive ; , ''káppa'') is the tenth letter of the Greek alphabet, representing the voiceless velar plosive sound in Ancient and Modern Greek. In the system of Greek numerals, has a value of 20. It was d ...

), ADL-5859 appears to be selective and only activates the delta receptor. with a K_i of 20 nM

Therapeutic potential

Like other opioids, it has potential in pain management; however, by being selective for the delta receptor, multiple undesirable side effects of traditional opioids are not present, such as respiratory depression, sedation, and euphoria. ADL-5859 was also found to be orally active, which makes it easier to administer. Multiple tests have shown its efficacy as an analgesic. It also did not seem to be a convulsant, unlike some other delta agonist opioids.

References

{{Opioid receptor modulators Synthetic opioids Delta-opioid receptor agonists Analgesics Chromanes Piperidines Spiro compounds Benzamides Diethylamino compounds