What Does ACKR3 And Conolidine Have To Do With Pain Relief?

ScienceDaily is a treasure trove of goodies when it comes to information on the current trends of pain relief and management.  It can get a bit nerdy with some of the scientific words and jargon, however, it does provide a lot of valuable content.  Did you know that the human body has the capability of generating a natural and safe form of opioids in response to pain?  ACKR3 and conolidine appears to play a significant role in this.

 

Tabernaemontana divaricata at Aanakkulam

 

New study further advances the treatment of chronic pain

“Scientists have demonstrated that conolidine, a natural painkiller derived from the pinwheel flower and traditionally used in Chinese medicine, interacts with the newly identified opioid receptor ACKR3/CXCR7 that regulates opioid peptides naturally produced in the brain. The researchers also developed a synthetic analogue of conolidine, RTI-5152-12, which displays an even greater activity on the receptor.”

Click on this link to continue reading the article ===> New study further advances the treatment of chronic pain

 

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Did you get to read the article on the site ScienceDaily?  If you haven’t, I recommend that you do.  It has some interesting content on a new form of pain relief that does not have the addictive nature of prescription opioids like morphine and fentanyl.  The article discussed how the researchers discovered another opioid receptor called ACKR3.  According to a MedLinePlus article, “[o]pioid receptors are found in the nervous system, where they are embedded in the outer membrane of nerve cells (neurons)”. Unlike the normal opioid receptors that promote pain relief within our body, ACKR3 actually dampens pain relief by binding to the naturally generated opioids, and thus, preventing it from binding with the normal opioid receptors that generate pain relief.

So, what did the researchers do next?  Well, like all good researchers, they went about looking for some chemical (hopefully natural) that would block that scavenger of an opioid receptor, the ACKR3, from taking away the naturally generated opioids from the normal opioid receptors.  And they discovered something called conolidine, which is attracted to and binds with ACKR3, allowing the naturally generated opioids to bind with normal opioid receptors, and thus, promoting pain relief.  It is interesting that the researchers took a deep dive into traditional Chinese medicine and found the effectiveness of conolidine in blocking the function of ACKR3.

It is promising that the researchers did not stop there.  They went one step further, and designed a synthetic version of conolidine, called “RTI-5152-12”, which has the same effect as conolidine, however, much more effective.  And moreover, offers promise “… for the development of a new class of drugs with alternative mechanism of action, thereby contributing to tackling the public health crisis linked to the increasing misuse of and addiction to opioid drugs …”.

To Your Success & Freedom,

Glenn Shimabukuro
 
 

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