November 28, 2021

Scientists make non-opioid pain reliever after discovering new compound that regulates biological link to pain

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

This image shows the structure of compound 194 (yellow bars) superimposed on an electrophysiological trace showing reduced sodium currents (yellow lines versus black lines) of cells 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 by Fierce Biotech, the team has designed a non-opioid drug that disrupts the interaction between CRMP2, a mediator protein, and the enzyme Ubc9 which is important in the activity of the NaV1.7 ion channel which plays a role critical when feeling pain. Dubbed 194, the drug has been shown to reverse pain in six different rat models.

The researchers said that NaV1.7 facilitates the transmission of pain signals in the form of electrical currents produced in the brain by neurons. Paralysis of NaV1.7 in animal models has shown that they have become resistant to pain, but previous drugs aimed at inhibiting channel activity failed only when they found out how CRMP2 and Ubc9 were affect.

They tested the efficacy of Drug 194 in managing pain in several animal models and found that the drug did relieve pain in these animals.

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Scientists seeking to optimize 194

The drug is now patented and licensed to start Regulonix LLC through Tech Launch Arizona, Medical Life Sciences News reported. The researchers noted that while 194 shows great promise for pain relief, they are looking to optimize the compound. But this time, they will focus on improving the half-life of 194 and its drug properties.

Optimizing the compound’s potential as a non-opioid pain reliever and taking it to the next level is an important step for researchers who wish to seek approval from the Food and Drug Administration to begin clinical trials.

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