Scientists discover powerful potential pain reliever

August 16, 2017

A team of scientists led by chemists Stephen Martin and James Sahn at The University of Texas at Austin have discovered what they say is a powerful pain reliever that acts on a previously unknown pain pathway. The synthetic compound, known as UKH-1114, is as effective at relieving neuropathic pain in injured mice as a drug widely used for pain relief called gabapentin, but it works at a much lower dose, with longer duration of action.

If the researchers can demonstrate that the drug is safe, effective and nonaddictive in humans -- a process that typically takes years -- the discovery could be instrumental in addressing one of today's biggest public health challenges: the opioid abuse epidemic.

Nearly a third of Americans suffer from chronic pain, yet the most effective pain relievers -- opioids -- are addictive and often require increased dosing to maintain efficacy. According to the National Institute on Drug Abuse, about 2 million people in the U.S. suffer from addiction to prescription opioid pain relievers. Alternatives to opioids have their own drawbacks -- for example, gabapentin (sold as Neurontin) can cause cognitive impairment in certain individuals.

"This opens the door to having a new treatment for neuropathic pain that is not an opioid," said Martin, a professor and the M. June and J. Virgil Waggoner Regents Chair in Chemistry. "And that has huge implications."

The pain drug they found binds to a receptor on cells throughout the central nervous system called the sigma 2 receptor. Although it was discovered 25 years ago, scientists still did not know what sigma 2 did until now.

Theodore Price, associate professor of neuroscience at The University of Texas at Dallas and a leading expert on chronic pain, tested UKH-1114 on mice with nerve damage and found that it alleviated pain as well as gabapentin did, but at a much lower dose (one-sixth as much) and was effective much longer (lasting for a couple of days, compared with 4 to 6 hours). This research is the first to demonstrate that the sigma 2 receptor may be a target for treating neuropathic pain.

Results are published in the Aug. 18 print edition of the journal ACS Chemical Neuroscience. An earlier paper, published online on May 28 in the journal Proceedings of the National Academy of Sciences, described the molecular cloning and identification of the sigma 2 receptor.

The researchers have filed patent applications on the new compound.

Neuropathic pain, or chronic pain, is caused when nerves in the central nervous system are damaged. Among other things, it can result from chemotherapy, diabetes and injuries to the brain or spinal cord.

Much work remains to be done before UKH-1114 can enter the market. More studies are needed to demonstrate safety, efficacy and oral bioavailability. In the meantime, the scientists are working to understand, on a fundamental level, how activating the sigma 2 receptor relieves neuropathic pain.

Still, Martin and Sahn are excited by the compelling results from the mouse model.

"We started out just working on fundamental chemistry in the lab," said Sahn, a research scientist in the Department of Chemistry. "But now we see the possibility that our discoveries could improve the quality of people's lives. That is very satisfying."
-end-


University of Texas at Austin

Related Chronic Pain Articles from Brightsurf:

Researchers are developing potential treatment for chronic pain
Researchers from the University of Copenhagen have developed a new way to treat chronic pain which has been tested in mice.

Molecular link between chronic pain and depression revealed
Researchers at Hokkaido University have identified the brain mechanism linking chronic pain and depression in rats.

How chikungunya virus may cause chronic joint pain
A new method for permanently marking cells infected with chikungunya virus could reveal how the virus continues to cause joint pain for months to years after the initial infection, according to a study published Aug.

Gastroesophageal reflux associated with chronic pain in temporomandibular joint
Gastroesophageal reflux (GERD) is associated with chronic, painful temporomandibular disorder -- pain in the temporomandibular joint -- and anxiety and poor sleep contribute to this association, according to a study in CMAJ.

One step closer to chronic pain relief
While effective drugs against chronic pain are not just around the corner, researchers from Aarhus University, Denmark, have succeeded in identifying a protein as a future potential target for medicinal drugs.

Gut bacteria associated with chronic pain for first time
In a paper published today in the journal Pain, a Montreal-based research team has shown, for the first time, that there are alterations in the bacteria in the gastrointestinal tracts of people with fibromyalgia.

Nearly 5.4 million cancer survivors suffer chronic pain
A new report finds about one in three cancer survivors (34.6%) reported having chronic pain, representing nearly 5.4 million cancer survivors in the United States.

New opioid speeds up recovery without increasing pain sensitivity or risk of chronic pain
A new type of non-addictive opioid developed by researchers at Tulane University and the Southeast Louisiana Veterans Health Care System accelerates recovery time from pain compared to morphine without increasing pain sensitivity, according to a new study published in the Journal of Neuroinflammation.

New target for chronic pain relief confirmed by scientists
A research group at Hiroshima University observed a potential new target for chronic pain treatment.

Menopause symptoms nearly double the risk of chronic pain
In addition to the other health conditions affected by estrogen, it has also been shown to affect pain sensitivity.

Read More: Chronic Pain News and Chronic Pain Current Events
Brightsurf.com is a participant in the Amazon Services LLC Associates Program, an affiliate advertising program designed to provide a means for sites to earn advertising fees by advertising and linking to Amazon.com.