Researchers from Charité – Universitätsmedizin Berlin have discovered a new way of developing painkillers.
The team of researchers used computational simulation to analyze interactions at opioid receptors – the cell’s docking sites for painkillers. When used in an animal model, their prototype of a morphine-like molecule was able to produce substantial pain relief in inflamed tissues. However, healthy tissues remained unaffected, suggesting that the severe side effects currently associated with these types of painkillers might be avoided. This research has been published in the current issue of the journal Science*.
Opioids are a class of strong pain killers. They are mainly used to treat pain associated with tissue damage and inflammation, such as that caused by surgery, nerve damage, arthritis or cancer. Common side effects associated with their use include drowsiness, nausea, constipation and dependency and, in some cases, respiratory arrest. “By analyzing drug-opioid receptor interactions in damaged tissues, as opposed to healthy tissues, we were hoping to provide useful information for the design of new painkillers without harmful side effects,” explains Prof. Dr. Christoph Stein, Head of the Department of Anesthesiology and Surgical Critical Care Medicine on Campus Benjamin Franklin. In cooperation with PD Dr. Marcus Weber from the Zuse Institute Berlin, and with the help of innovative computational simulations, the researchers were able to analyze morphine-like molecules and their interactions with opioid receptors. They were able to successfully identify a new mechanism of action, which is capable of producing pain relief only in the desired target tissues – those affected by inflammation.
Treating postoperative and chronic inflammatory pain should now be possible without causing side effects. Doing so would substantially improve patient quality of life. The study’s first authors, Dr. Viola Spahn and Dr. Giovanna Del Vecchio, explain: “In contrast to conventional opioids, our NFEPP-prototype appears to only bind to, and activate, opioid receptors in an acidic environment. This means it produces pain relief only in injured tissues, and without causing respiratory depression, drowsiness, the risk of dependency, or constipation.” After designing and synthesizing the drug prototype, the researchers subjected it to experimental testing. Using computer modeling, the researchers simulated an increased concentration of protons, thereby mimicking the acidic conditions found in inflamed tissues. “We were able to show that the protonation of drugs is a key requirement for the activation of opioid receptors,” conclude the authors. Their findings, which may also apply to other types of pain, may even find application in other areas of receptor research. Thereby, the benefits of improved drug efficacy and tolerability are not limited to painkillers, but may include other drugs as well.
Learn more: Breakthrough: Charité-based researchers discover new mechanism of action
[osd_subscribe categories=’pain’ placeholder=’Email Address’ button_text=’Subscribe Now for any new posts on the topic “PAIN”‘]
Receive an email update when we add a new PAIN article.
The Latest on: Painkillers
[google_news title=”” keyword=”painkillers” num_posts=”10″ blurb_length=”0″ show_thumb=”left”]
via Google News
The Latest on: Painkillers
- Former Iowa nurse charged with stealing painkillers from patientson April 26, 2024 at 7:17 am
Court documents say Amanda Manatt kept the drugs for herself instead of giving them to a patient to help with pain.
- McKinsey Faces Criminal Probe for its Role in Opioid Crisison April 25, 2024 at 11:19 am
The Justice Department is investigating the consulting firm over its role in advising drug makers how to market prescription painkillers and contributed to a national addiction disaster.
- Onawa woman pleads not guilty of stealing painkillerson April 25, 2024 at 6:00 am
According to court documents, Haptonstall broke into former customers' homes after she no longer worked for the pharmacy and stole drugs.
- Can I take antibiotics and painkillers together? See the NHS adviceon April 25, 2024 at 3:24 am
Here is the health expert's advice regarding taking them with painkillers and the other key things you should avoid when taking antibiotics. The NHS has advised that is safe to take paracetamol with ...
- McKinsey Under Criminal Investigation Over Alleged Role In Fueling Opioid Epidemicon April 25, 2024 at 1:42 am
McKinsey & Company is facing a criminal investigation by U.S. attorneys' offices in Massachusetts and the Western District of Virginia for its alleged role in fueling the opioid epidemic.
- UW-Madison scientists develop green method for producing painkillers from poplar treeson April 25, 2024 at 1:00 am
Researchers at the University of Wisconsin-Madison Energy Institute made a groundbreaking discovery to produce Tylenol through a more sustainable process.
- Explainer: Why is the use of highly potent synthetic painkillers nitazenes and xylazine spiking?on April 22, 2024 at 6:30 am
At the same time, an increasing quantity of synthetic drugs such as nitazenes and xylazine have been detected in the illicit drug market both internationally and in the UK and it is feared that a ...
- She got addicted to painkillers after her miscarriage – Dr Grace Boadu’s boyfriendon April 21, 2024 at 1:52 am
Pastor Kingsley Gyamfi, the boyfriend of the late Dr. Grace Boadu, has disclosed that his partner became addicted to painkillers to relieve her of the pain she was going through.
- Cannabis holds promise for pain management, reducing the need for opioid painkillers – a neuropharmacology expert explains howon April 19, 2024 at 10:02 am
Opioid receptors are dynamically regulated, meaning that as they get exposed to more and more opioids, the body adapts quickly by deactivating the receptor. In other words, the bo ...
via Bing News