Corporate Banner
Satellite Banner
Medicinal Chemistry
Scientific Community
Become a Member | Sign in
Home>News>This Article

Scripps' Scientists Develop Promising Drug Candidates for Pain and Addiction

Published: Thursday, January 16, 2014
Last Updated: Thursday, January 16, 2014
Bookmark and Share
Two new drug scaffolds offer researchers novel tools that act on the kappa opioid receptor.

Scientists from the Florida campus of The Scripps Research Institute (TSRI) have described a pair of drug candidates that advance the search for new treatments for pain, addiction and other disorders.

The two new drug scaffolds, described in a recent edition of The Journal of Biological Chemistry, offer researchers novel tools that act on a demonstrated therapeutic target, the kappa opioid receptor (KOR), which is located on nerve cells and plays a role in the release of the neurotransmitter dopamine.

While compounds that activate KOR are associated with positive therapeutic effects, they often also recruit a molecule known as βarrestin2 (beta arrestin), which is associated with depressed mood and severely limits any therapeutic potential.

“Compounds that act at kappa receptors may provide a means for treating addiction and for treating pain; however, there is the potential for the development of depression or dysphoria associated with this receptor target,” said Laura Bohn, a TSRI associate professor who led the study. “There is evidence that the negative feelings caused by kappa receptor drugs may be, in part, due to receptor actions through proteins called beta arrestins. Developing compounds that activate the receptors without recruiting beta arrestin function may serve as a means to improve the therapeutic potential and limit side effects.”

The new compounds are called “biased agonists,” activating the receptor without engaging the beta arrestins.

Research Associate Lei Zhou, first author of the study with Research Associate Kimberly M. Lovell, added, “The importance of these biased agonists is that we can manipulate the activation of one particular signaling cascade that produces analgesia, but not the other one that could lead to dysphoria or depression.”

The researchers note that the avoidance of depression is particularly important in addiction treatment, where depressed mood can play a role in relapse.

The two drug candidates also have a high affinity and selectivity for KOR over other opioid receptors and are able to pass through the blood-brain barrier. Given these promising attributes, the scientists plan to continue developing the compounds.

Further Information
Access to this exclusive content is for Technology Networks Premium members only.

Join Technology Networks Premium for free access to:

  • Exclusive articles
  • Presentations from international conferences
  • Over 2,800+ scientific posters on ePosters
  • More than 4,000+ scientific videos on LabTube
  • 35 community eNewsletters

Sign In

Forgotten your details? Click Here
If you are not a member you can join here

*Please note: By logging into you agree to accept the use of cookies. To find out more about the cookies we use and how to delete them, see our privacy policy.

Related Content

Potential Persistent Tuberculosis Treatment
Researchers have discovered several first-in-class compounds that target hidden TB infections by attacking a critical process the bacteria use to survive in the hostile environment of the lungs.
Monday, November 23, 2015
Scientists Determine How Antibiotic Gains Cancer-Killing Sulfur Atoms
In a discovery with implications for future drug design scientists have shown an unprecedented mechanism for how a natural antibiotic with antitumor properties incorporates sulfur into its molecular structure, an essential ingredient of its antitumor activity.
Friday, August 14, 2015
Chemists Devise Inexpensive, Benchtop Method for Marking and Selecting Cells
Chemists at The Scripps Research Institute have found an easier way to perform one of the most fundamental tasks in molecular biology.
Wednesday, January 16, 2013
Scientists Find Structure of a Protein that Makes Cancer Cells Resistant to Chemotherapy
A research team at the Scripps Research Institute has obtained the first glimpse of a protein that keeps certain substances, including many drugs, out of cells.
Monday, March 30, 2009
Scientific News
Drug May Prevent Life-Threatening Muscle Loss in Advanced Cancers
New data describes how an experimental drug can stop life-threatening muscle wasting (cachexia) associated with advanced cancers and restore muscle health.
Chemical Design Made Easier
Rice University scientists prepare elusive organocatalysts for drug and fine chemical synthesis.
Nanocarriers May Carry New Hope for Brain Cancer Therapy
Berkeley lab researchers develop nanoparticles that can carry therapeutics across the brain blood barrier.
Potential Persistent Tuberculosis Treatment
Researchers have discovered several first-in-class compounds that target hidden TB infections by attacking a critical process the bacteria use to survive in the hostile environment of the lungs.
Shedding Light on “Dark” Cellular Receptors
UNC and UCSF labs create a new research tool to find homes for two orphan cell-surface receptors, a crucial step toward finding better therapeutics and causes of drug side effects.
Giant Molecules Inhibit Ebola Infection
European researchers have designed a "giant" molecule formed by thirteen fullerenes covered by carbohydrates which, by blocking this receptor, are able to inhibit the cell infection by an artificial ebola virus model.
First Therapy Appearing to Reverse Decline in Parkinson’s
An FDA-approved drug for leukemia improved cognition, motor skills and non-motor function in patients with Parkinson’s disease and Lewy body dementia in a small clinical trial, say researchers at Georgetown University Medical Center (GUMC).
Fighting Pain with Ketamine
Researchers at the Texas A&M Health Science Center are using ketamine, a drug that already exists as an anesthetic, to treat pain.
Possible New Treatment for Neurodegenerative Diseases Found
Researchers at the University of Liverpool have found that a well-established anti-epileptic drug could also be used as a treatment for neurodegenerative diseases.
Breast Cancer Drug Beats Superbug
Tamoxifen helps white blood cells clear multidrug-resistant bacteria in lab and mouse studies.
Skyscraper Banner

SELECTBIO Market Reports
Go to LabTube
Go to eposters
Access to the latest scientific news
Exclusive articles
Upload and share your posters on ePosters
Latest presentations and webinars
View a library of 1,800+ scientific and medical posters
2,800+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
4,000+ scientific videos