Blocking Chilli-Pepper Receptor Can Treat Pain

Biting into a hot spicy chilli-pepper can be irresistible to some people or even intolerable to others. Using their findings on the chilli pepper's effect, scientists are exploring the possibilities to develop a new drug to treat many kinds of pain and problems caused by inflammation. // Lead scientist of these trials, Laykea Tafesse and his colleagues explain that decades ago, scientists had pegged a compound called capsaicin causing that fiery pain. Researchers had been able to sequence the genetic sequence for the protein “receptor” that capsaicin attaches to in the body. The receptor was found to be a protein on cells that acts as a gate, allowing only certain substances into a cell. These new findings brought on a hunt for compounds that can block this gate, cut off the pain trigger and potentially treat pain like no other available drug. Some of the molecules resulting from these tests have been tested on humans but caused unwanted side effects, or they wouldn’t work well as oral medication. Tafesse’s team are currently working on more suitable drug candidate.

More than two dozen similar Transient Receptor Potential Vanilloid (TRPV1) antagonists were produced and evaluated, each with its own unique molecular tweak. The compounds were evaluated for their ability to block capsaicin and acid-induced calcium influx in CHO cells expressing human TRPV1. Tests were done in the lab and in animals for traits like potency, safety, the ability to dissolve in water and whether they can be taken orally. One prospect showed the most promise, and it has advanced into clinical trials.

The progress of these clinic trails are published in ACS’ Journal of Medicinal Chemistry.

Source-Medindia