Navigation Links
Chemical compound shows promise as alternative to opioid pain relievers
Date:7/15/2013

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.


'/>"/>

Contact: Mount Sinai Press Office
newsmedia@mssm.edu
212-241-9200
The Mount Sinai Hospital / Mount Sinai School of Medicine
Source:Eurekalert

Related medicine news :

1. Metering Pump / Chemical Injection (Metering /Dosing) Pump Market to $4.1 Billion by 2017, With a CAGR of 5.3% From 2012 to 2017 – New Report by MarketsandMarkets
2. Ethanol Leads Renewable Chemicals Market; Polymers Sector 14.3% CAGR Growth Forecasted by 2018 Says New Research Report at ReportsnReports.com
3. Redefining Skincare: Sevique on track to be the Best Natural Alternative to Chemical-Based Products
4. Canadian Linen and Uniform Expands Services with Cleaning Chemicals Management Program
5. Renewable Chemical Market will Grow from an Estimated $57.5 Billion in 2012 to $83.4 Billion by 2018, with a CAGR of 7.7% - New Report by MarketsandMarkets
6. AmeriPride Expands Services with Cleaning Chemicals Management Program
7. American Chemical Society podcast: The first caffeine-addicted bacteria
8. Health Care Without Harm Urges Strengthening of the Chemical Safety Improvement Act of 2013
9. 1-800-GO-VAPOR.com to Target Resort Hotels with Chemical-Free Vapor Steam Cleaner Technology
10. Chemical Safety Improvement Act of 2013: PETA International Science Consortium
11. New American Chemical Society video: Why toothpaste + orange juice = yuk!
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:12/6/2016)... ... 06, 2016 , ... U.S. Security Associates (USA) was named ... their industry leading training methods that engage their associates and link their achievements ... elite in employer-sponsored training and development programs. , “The 2017 Training Top 125 ...
(Date:12/5/2016)... ... ... For many years, Andrew G. Zubinas has accumulated over 130 hardcover ... Lithuanian language and its poetry inspired him in writing “ Forest Lungs ... aspects of a living, breathing forest where nothing ever stays the same. His subjects ...
(Date:12/5/2016)... ... 05, 2016 , ... “Epilepsy Awareness,” which can be found ... a conversation about epilepsy, bearing down on the social stigma and lack of ... with epilepsy within their lifetime. With such a large percentage of people affected, ...
(Date:12/5/2016)... , ... December 05, 2016 , ... BSI and Brenntag ... United States and Canada for distribution of their natural fruits and beverage ... is an exciting addition to our Life Sciences product portfolio,” said Steve Brauer, ...
(Date:12/5/2016)... ... December 05, 2016 , ... ... portfolio company, today announced it has acquired the assets of Frankfurt, Germany ... a subsidiary of Chiltern International and focuses on clinical trial drug packaging, ...
Breaking Medicine News(10 mins):
(Date:12/5/2016)... 5, 2016 Special purpose needles are used in ... fluid and cells from organs or lumps and are available ... The global market for special purpose needles is showing a ... of revenue, the global special purpose needles market is projected ... period (2016–2026) and is expected to be valued at US$ ...
(Date:12/5/2016)... Dec. 5, 2016  Pennsylvania Physician General Dr. ... Programs Gary Tennis today filled prescriptions for ... Pharmacy in York to demonstrate ... Dr. Levine as a prescription to acquire naloxone at ... important to remember that any Pennsylvanian can walk up ...
(Date:12/5/2016)... -- Research and Markets has announced the addition ... (Biomedical & Biochemical Research, Disease Diagnostics), End User (Academic & Research ... report to their offering. ... , The western blotting ... USD 574.8 Million in 2016, growing at a CAGR of 4.9%. ...
Breaking Medicine Technology: