Discovery: a painkiller without side effects

Published by Adrien,
Source: Cell
Other Languages: FR, DE, ES, PT

A team of researchers has made a major breakthrough in the field of painkillers. The compound SBI-810 could be a game-changer for millions of patients.

This new drug, developed at Duke University, specifically targets the neurotensin 1 receptor (NTSR1) found on sensory neurons and in the spinal cord. Unlike opioids, it acts selectively to relieve pain without causing unwanted side effects.


Illustration image Pixabay

Preclinical tests on mice have shown remarkable efficacy of SBI-810. It not only significantly reduced pain but also allowed for decreased opioid use when combined with low doses. These results pave the way for safer alternatives in pain management.

Ru-Rong Ji, lead researcher of the study, highlights the importance of this discovery. SBI-810 avoids the issues of addiction and tolerance associated with opioids while providing effective relief. This advancement could benefit patients suffering from acute or chronic pain.

The mechanism of action of SBI-810 relies on biased agonism, specifically activating the β-arrestin-2 pathway linked to pain relief. This targeted approach minimizes the risks of side effects and addiction, a major concern with current treatments.

Researchers are now planning human clinical trials. SBI-810 represents hope for patients requiring strong painkillers without the drawbacks of opioids. Its development is supported by patents and public funding.

This study, published in Cell, marks an important milestone in pain research. SBI-810 could become a valuable tool in the therapeutic arsenal against pain, offering a safe and effective alternative to opioids.

How does biased agonism work in drugs?


Biased agonism is a pharmacological approach that allows a drug to selectively activate certain signaling pathways of a receptor while ignoring others. This specificity reduces side effects.

In the case of SBI-810, biased agonism targets the β-arrestin-2 pathway, associated with pain relief, without activating the pathways responsible for adverse effects. This method represents a significant advancement in drug design.

Unlike traditional agonists that activate all signaling pathways of a receptor, biased agonists offer unprecedented precision. This technology could be applied to other receptors to treat various diseases with fewer side effects.

Why are opioids so problematic?


Opioids, while effective for pain relief, carry high risks of addiction and overdose. They act on multiple receptors in the brain, causing not only pain relief but also euphoria that can lead to abuse.

Tolerance to opioids develops quickly, requiring increasingly higher doses to achieve the same effect. This increases the risk of overdose, a major cause of death, particularly in the United States.

Additionally, opioids cause side effects such as constipation, respiratory depression, and sedation. These issues limit their long-term use and make the search for alternatives urgent.

SBI-810, by specifically targeting the NTSR1 receptor without activating the pathways responsible for addiction and side effects, represents a potential solution to these problems. Its development could mark a turning point in pain management.
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