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Scientists are Making Non-Opioid Pain Reliever After Discovering New Compound That Regulates Biological Link to Pain

University of Arizona Health Sciences researchers are planning to develop a safe and effective non-opioid pain reliever after creating a new compound that reduces the pain sensation by regulating a biological channel associated with pain.


compound 194

This image shows the structure of compound 194 (yellow sticks) overlaid on an electrophysiology trace showing reduced sodium currents (yellow vs. black lines) from cells that are treated with compound 194. The structure illustrates the predicted interaction of CRMP2 (pink, PDB 2GSE) with the Nav1.7 channel (cyan, PDB 6J8G). (PHOTO: University of Arizona Health Sciences)

Drug 194 Reverses Pain in Rat Models

According to an article in Fierce Biotech, the team has designed a non-opioid drug that disrupts the interaction between CRMP2, a mediator protein, and the enzyme Ubc9 that is important in the activity of the NaV1.7 ion channel that plays a critical role in sensing pain. Dubbed as 194, the drug was proven to have reversed pain in six different rat models.

Researchers said that NaV1.7 facilitates the transmission of pain signals in the form of electrical currents produced in the brain by the neurons. Crippling NaV1.7 in animal models showed that they have become resistant to pain, but previous drugs aimed at inhibiting the channel’s activity failed not until they discovered how CRMP2 and Ubc9 affect it.

They tested drug 194’s efficacy in pain management in several animal models and found that the drug indeed relieved the pain in those animals.

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Scientists Looking Into Optimizing 194

The drug is now patented and licensed to startup Regulonix LLC through Tech Launch Arizona, News Medical Life Sciences reported. Researchers noted that although 194 shows great promise for pain relief, they are looking into optimizing the compound. But this time, they will focus on improving 194’s half-life and its drug-like properties.

Optimizing the potential of the compound as a non-opioid pain-reliever and advancing it to the next stage is an important step for researchers to file for approval from the Food and Drug Administration to begin clinical trials.


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