Researchers identified the structure of an opioid receptor in the brain during active engagement with a drug molecule. The discovery could facilitate the creation of safer and more effective opioid analgesics, according to a study published in the journal Cell.
Here are five things to know.
1. Scientists previously identified four opioid receptors in the brain: delta, kappa, mu and nociceptin. Potentially lethal opioids such as fentanyl, heroin, morphine and oxycodone are particularly drawn to the mu receptor, which is problematic because this enables the drugs' painkilling properties and facilitates their lethal and addictive side effects.
2. Unlike mu, the kappa receptor enables the drugs' painkilling qualities without lethal side effects, according to a report published in Wired. A growing body of research suggests this receptor could be key to the development of effective opioid medications that don't carry the same overdose and addiction as currently available opioids.
3. In 2012, researchers identified the structure of an inactive kappa receptor — the first step in designing an opioid that can link to the receptor. To identify the structure of a kappa receptor actively engaged with an opioid molecule, researchers in the most recent study used a synthetic opioid molecule and a single-chain antibody to "prop the [receptor] open in its active state, like poles inside a tent," according to Wired.
4. Experts in the field of kappa receptor study who were not a part of the study say the discovery will provide a substantial boost to research.
"There's probably 100 labs worldwide working on the kappa receptor, not including pharmaceutical companies — it's a big area of research," Michael Bruchas, PhD, a neuroscientist with Washington University in St. Louis who has been studying the kappa receptor for more than 10 years, told Wired.
5. Bruchas said knowledge of the receptor's structure will allow computers to more accurately measure kappa's interactions with different compounds.
"It's not unlike a model of the climate: The more information and data points we have, the stronger the model becomes, and this structure really will accelerate that," he told Wired.
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