In a new study from the Luxembourg Institute of Health, researchers found that conolidine, a natural painkiller derived from the pinwheel flower and traditionally used in Chinese medicine, may help improve the treatment of chronic pain.
The painkiller interacts with the newly identified opioid receptor that regulates opioid peptides naturally produced in the brain.
The researchers also developed a synthetic analog of conolidine, which displays an even greater activity on the receptor.
These findings further advance the understanding of pain regulation and open alternative therapeutic avenues for the treatment of chronic pain.
Opioid peptides are small proteins that mediate pain relief and emotions, including euphoria, anxiety, stress and depression, by interacting with four classical receptors (“molecular switches”) in the brain.
In the study, the researchers confirmed that conolidine binds to the newly identified opioid receptor ACKR3.
They screened over 240 receptors for their ability to be activated or inhibited by this molecule.
By doing so, conolidine blocks ACKR3 and prevents it from trapping the naturally secreted opioids, which in turn increases their availability for interacting with classical receptors.
The researchers believe that this molecular mechanism is at the basis of the beneficial effects of this traditionally used medicine on pain relief.
The scientists then developed a modified variant of conolidine, which exclusively binds to ACKR3 with an even higher affinity.
The new drug is postulated to increase the levels of opioid peptides that bind to classical opioid receptors in the brain, resulting in a heightened painkilling activity.
The team says the discovery of ACKR3 as a target of conolidine further emphasizes the role of this newly discovered receptor in modulating the opioid system and, consequently, in regulating our perception of pain.
The findings could also mean that conolidine, and potentially also its synthetic analogs, could carry new hope for the treatment of chronic pain and depression.
This is because conolidine was reported to trigger fewer of the detrimental side-effects—namely addiction, tolerance and respiratory problems—associated with commonly used opioid drugs like morphine and fentanyl.
If you care about pain management, please read studies about common opioid painkillers may increase pancreatic cancer risk and findings of can depression drugs help reduce chronic back pain and osteoarthritis?
For more information about pain and your health, please see recent studies about a new way to treat chronic pain without opioids and results showing that this diet may increase your risk of low back pain.
The study is published in Signal Transduction and Targeted Therapy. One author of the study is Dr. Andy Chevigné.
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