Experimental Class of Drugs Could Treat Pain

Researchers in a recent study discovered a class of small-molecule drugs that can inhibit the ion channels TRPV4 and TRPA1, 2 targets for the treatment of pain.

According to the study, published in Scientific Reports, this drug could potentially treat skin irritation and itching, headaches, jaw pain, and abdominal pain from the pancreas and colon.

"We are very pleased with what is a first chapter in a highly promising story," said researcher Wolfgang Liedtke, MD, PhD. "We hope to be able to develop these compounds for clinical use in humans or animals."

The molecule TRPV4 is able to transmit skin irritation from sunburn, as well as pain from the head and face. The researchers hoped to develop an even more potent inhibitor of this molecule.

Compared with the prototype inhibitor, researchers found that the drug candidate 16-8 was 10 times as effective in cells with active TRPV4, which is needed for the development of osteoarthritis.

The drug 16-8 also worked in a cell type that was involved with nerve cell injury, stroke, and epilepsy, according to the study. It also showed the ability to block TRPA1, a target for pain and itch treatments.

"As a physician, I soon realized the enormous potential that these compounds might have, given how beneficial dual-target molecules can be in clinical medicine," Dr Liedtke said.

Researchers found that the drug 16-8 could also stop pain from abdominal aches in mice with inflamed pancreases, according to the study. The drug could potentially be used to treat osteoarthritis, joint, head, face, and jaw pain. It could also potentially be used to treat pain from nerve cell injury.

The researchers’ preclinical work will have a focus on the drug’s possible uses while learning more about how it works and hope to explore topical applications as well, the study concluded.