Featured Research

from universities, journals, and other organizations

Chemical compound shows promise as alternative to opioid pain relievers

Date:
July 15, 2013
Source:
The Mount Sinai Hospital / Mount Sinai School of Medicine
Summary:
A drug targeting a protein complex containing two different types of opioid receptors may be an effective alternative to morphine and other opioid pain medications, without any of the side effects or risk of dependence, according to new research.

A drug targeting a protein complex containing two different types of opioid receptors may be an effective alternative to morphine and other opioid pain medications, without any of the side effects or risk of dependence, according to research led by the Icahn School of Medicine at Mount Sinai.

The findings are published in July in the journal Proceedings of the National Academy of Sciences.

Morphine is still the most widely-used pain reliever, or analgesic, in people with severe pain, but chronic use can lead to addiction and negative side effects such as respiratory issues, constipation, or diarrhea.

In a previous study published in Science Signaling by Lakshmi Devi, PhD, Professor of Pharmacology and Systems Therapeutics at Mount Sinai, researchers identified a therapeutic target called a GPCR heteromer, which is a protein complex that is made up of two opioid receptors called mu and delta. They also showed that the heteromer is abundant in the area of the brain that processes pain, and is the likely cause of morphine tolerance and side effects.

In the current study, Dr. Devi carried out high throughput screening in collaboration with researchers at the National Institutes of Health (NIH) to identify which small molecules might act on the signaling pathway associated with this protein complex. Researchers found one compound called CYM51010 that was as potent as morphine, but less likely to result in tolerance and negative side effects. Dr. Devi's team is currently developing modified versions of this compound that may have potential as analgesics with reduced side effects.

"GPCR heteromers have been suggested to represent powerful targets for improved, novel therapeutics with reduced adverse effects in people with severe pain," said Dr. Devi. "However, there are presently no chemical tools that allow us to investigate their role in vivo. Our work represents a promising step in this direction, providing results that pave the way towards a new understanding of the function and pharmacology of opioid receptor heteromers."

Dr. Devi and her team are currently working with co-author Marta Filizola, PhD, Associate Professor of Structural and Chemical Biology at Mount Sinai, to learn how CYM51010 binds to the protein complex. Armed with this information, they hope to modify the compound to treat pain without the development of dependency. They also plan to restrict their benefit to the gastrointestinal system and treat diarrhea associated with irritable bowel disease that is unresponsive to existing therapies.

This study was supported by National Institute on Drug Abuse Grants R01-008863 and K05-019521.


Story Source:

The above story is based on materials provided by The Mount Sinai Hospital / Mount Sinai School of Medicine. Note: Materials may be edited for content and length.


Journal Reference:

  1. I. Gomes, W. Fujita, A. Gupta, A. S. Saldanha, A. Negri, C. E. Pinello, E. Roberts, M. Filizola, P. Hodder, L. A. Devi. Identification of a  -  opioid receptor heteromer-biased agonist with antinociceptive activity. Proceedings of the National Academy of Sciences, 2013; DOI: 10.1073/pnas.1222044110

Cite This Page:

The Mount Sinai Hospital / Mount Sinai School of Medicine. "Chemical compound shows promise as alternative to opioid pain relievers." ScienceDaily. ScienceDaily, 15 July 2013. <www.sciencedaily.com/releases/2013/07/130715151156.htm>.
The Mount Sinai Hospital / Mount Sinai School of Medicine. (2013, July 15). Chemical compound shows promise as alternative to opioid pain relievers. ScienceDaily. Retrieved August 21, 2014 from www.sciencedaily.com/releases/2013/07/130715151156.htm
The Mount Sinai Hospital / Mount Sinai School of Medicine. "Chemical compound shows promise as alternative to opioid pain relievers." ScienceDaily. www.sciencedaily.com/releases/2013/07/130715151156.htm (accessed August 21, 2014).

Share This




More Mind & Brain News

Thursday, August 21, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

Do More Wedding Guests Make A Happier Marriage?

Do More Wedding Guests Make A Happier Marriage?

Newsy (Aug. 20, 2014) — A new study found couples who had at least 150 guests at their weddings were more likely to report being happy in their marriages. Video provided by Newsy
Powered by NewsLook.com
Charter Schools Alter Post-Katrina Landscape

Charter Schools Alter Post-Katrina Landscape

AP (Aug. 20, 2014) — Nine years after Hurricane Katrina, charter schools are the new reality of public education in New Orleans. The state of Louisiana took over most of the city's public schools after the killer storm in 2005. (Aug. 20) Video provided by AP
Powered by NewsLook.com
Researcher Testing on-Field Concussion Scanners

Researcher Testing on-Field Concussion Scanners

AP (Aug. 19, 2014) — Four Texas high school football programs are trying out an experimental system designed to diagnose concussions on the field. The technology is in response to growing concern over head trauma in America's most watched sport. (Aug. 19) Video provided by AP
Powered by NewsLook.com
Kids' Drawings At Age 4 Linked To Intelligence At Age 14

Kids' Drawings At Age 4 Linked To Intelligence At Age 14

Newsy (Aug. 19, 2014) — A study by King's College London says there's a link between how well kids draw at age 4 and how intelligent they are later in life. Video provided by Newsy
Powered by NewsLook.com

Search ScienceDaily

Number of stories in archives: 140,361

Find with keyword(s):
 
Enter a keyword or phrase to search ScienceDaily for related topics and research stories.

Save/Print:
Share:  

Breaking News:
from the past week

In Other News

... from NewsDaily.com

Science News

Health News

Environment News

Technology News



Save/Print:
Share:  

Free Subscriptions


Get the latest science news with ScienceDaily's free email newsletters, updated daily and weekly. Or view hourly updated newsfeeds in your RSS reader:

Get Social & Mobile


Keep up to date with the latest news from ScienceDaily via social networks and mobile apps:

Have Feedback?


Tell us what you think of ScienceDaily -- we welcome both positive and negative comments. Have any problems using the site? Questions?
Mobile iPhone Android Web
Follow Facebook Twitter Google+
Subscribe RSS Feeds Email Newsletters
Latest Headlines Health & Medicine Mind & Brain Space & Time Matter & Energy Computers & Math Plants & Animals Earth & Climate Fossils & Ruins