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:1/20/2017)... ... January 20, 2017 , ... Vitamin Well has launched two ... drinks have been produced in collaboration with Zlatan Ibrahimovic and have been developed ... After a successful launch in Sweden last year, the next generation sports drinks ...
(Date:1/20/2017)... ... ... Angel”: a heartwarming and earnest tale of faith and believing in the path ... the creation of published author, Marjorie Lund-Fontaine, a former professional violinist, alumnus of The ... of her new book, Marjorie says, “‘The Angel’ was written as a fairytale, but ...
(Date:1/20/2017)... ... 2017 , ... “I Forgive You”: a fine examination of how God handles sin, including ... of published author, Stephen Miller, who, for over ten long years has been waiting to ... in Trinidad and Tobago, he has been serving the Lord for over twenty years, and ...
(Date:1/20/2017)... (PRWEB) , ... January 20, 2017 , ... “Christmas in ... creation of published author, Sara Seymour, who lives in Lafayette, Indiana where she works ... sips on iced coffees and writes. , Published by Christian Faith Publishing, Sara Seymour’s ...
(Date:1/20/2017)... ... January 20, 2017 , ... “Knowledge is God’s Lighthouse”: a moving and ... God’s Lighthouse” is the creation of published author, Gene Gaapf, a retired truck driver, ... , “I have been writing since high school and have many different titles,” Gaapf ...
Breaking Medicine News(10 mins):
(Date:1/20/2017)... 2017 Research and Markets has announced ... Opportunities, and Future" report to their offering. ... This research service on the ... technologies, and provides a snapshot of the key participants in the ... are provided from 2016 to 2020. The market is expected to ...
(Date:1/20/2017)... -- Avillion LLP, a co-developer and financier of late-stage ... MD MBA as Chief Medical Officer. Dr Weinberg will be based ... ... spent more than 17 years as a pharmaceutical and biotech executive ... Over the course of his career, he has interfaced with the ...
(Date:1/19/2017)... , Jan. 19, 2017 The Global Therapy ... and access to partnering deals and agreements entered into ... in partnering deals - Top deals by value - ... development, technology type The report provides understanding and ... by the world,s leading healthcare companies. The report ...
Breaking Medicine Technology: