In a recent study, researchers have developed two new medications that can effectively reduce pain.
In addition, the two new drugs could prevent brain- and gut-related side effects typically linked to opioid use.
Opioids are a class of drugs with powerful pain-relieving features. They are often used to treat the pain linked to body tissue damage and inflammation.
Patients after surgery or cancer treatment often need to use opioids.
However, previous studies have shown that opioid use can bring many harmful side effects, including drowsiness, nausea, constipation, dependency and respiratory symptoms.
Therefore, it is important to develop a new opioid drug that can reduce pain effectively with few side effects.
In the current study, the team used computer simulations to develop new opioids that will only work at brain regions affected by injury or inflammation.
They developed two new opioids. In both cases, the researchers used fentanyl as the starting molecule.
They supposed that damaged or inflamed body tissues show stronger interaction between ‘opioid agonists’ and the opioid receptors they bind to.
Opioid agonists are the substances that could elicit the pain-relieving effect.
The computer simulations showed that this is due to an increased concentration of protons in inflamed tissues. It leads to lower pH values than in healthy tissues and results in acidic conditions.
The team also found that opioid molecules need to undergo protonation before they can bind to and activate opioid receptors.
Based on the information, they designed two drugs that would only exist in their protonated state in inflammation.
The new drugs only work on body tissue damage or inflammation, rather than affecting the brain or the gut.
Then they tested the two new drugs in preclinical experiments and found they could strongly reduce pain while avoiding the dangerous side effects.
These findings enhance scientists’ understanding of the molecular processes underlying the complex interactions seen in inflamed tissues.
The researchers hope their new results could help scientists fight the opioid crisis, a problem that is particularly serious in the United States.
The future work will focus on making these newly-designed drugs available to patients.
The team also suggest that their new findings may help develop other new drugs to treat chronic health conditions.
The study findings are published in Pain and Scientific Reports.
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