3D atomic-level snapshots reveal ketamine binds to human opioid receptors
Ketamine, a drug approved for medical use in 1970 as a short-acting anesthetic, including during the Vietnam War for battlefield surgery, is still a pharmacological mystery. For a long time, scientists knew that ketamine, which is highly valued for treating severe pain and treatment-resistant depression, primarily works by blocking NMDARs, major receptors in the brain. However, this didn't fully…
Ketamine, a pain-relief and depression treatment approved since 1970, remains a mystery to scientists. While it is known to block NMDARs, the exact reason for its rapid effectiveness over drugs with similar actions has been unclear. In a study published in Nature Structural & Molecular Biology, researchers used 3D atomic-level snapshots to reveal that ketamine directly binds and activates human opioid receptors, specifically the mu and kappa receptors.
These receptors are the same ones that natural pain-relieving endorphins activate. The study also found that ketamine's pain-relieving effect in mice disappeared when opioid receptors were blocked with naloxone or the kappa receptor was blocked with aticaprant. The discovery of ketamine's direct activation of opioid receptors could potentially help develop treatments with rapid effects on pain and depression without the high or addictive potential.
To achieve this, a deeper understanding of the atomic-level details of how ketamine acts is required.
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