Featured Research

from universities, journals, and other organizations

New technology for screening potential analgesic drugs

Date:
February 24, 2014
Source:
Universidad de Barcelona
Summary:
Researchers have developed technology that enables them to a determine drugs’ analgesic potential before being tested in animal models. The finding saves time and money on researching new effective pain treatments.

Researchers of the Neuropharmacology and Pain Research Group of the Bellvitge Biomedical Research Institute (IDIBELL), the University of Barcelona (UB) and ESTEVE, have developed  technology that enables them to a determine drugs' analgesic potential before being tested in animal models. The finding saves time and money on researching new effective pain treatments.

Traditionally in the development of analgesic drugs, the effectiveness of these molecules has been determined by using pain animal models, a hard, expensive and unclear process from a pharmacological point of view. Therefore, the great challenge is to develop more effective methodologies. Francisco Ciruela, senior lecturer of the Department of Pathology and Experimental Therapy at UB and researcher of the Neuropharmacology and Pain Research Group, explains: "We are talking about thousands of drugs; so, before testing them in preclinical pain models, that is, animal models, it will be useful to do a screening of the activity of these molecules in order to separate those that have greater antinociceptive potential."

The study led by Ciruela describes a new technology to determine the analgesic activity of drugs before being tested in animal models. "We have developed a Receptor Fluorescence Resonance Energy Transfer (FRET) based biosensor that allow us to classify in a simple system (cells in culture) ligands in sigma-1 receptor into agonists and antagonists," details the researcher.

The experiments carried out by ESTEVE and the research group led by Dr Ciruela (IDEBELL-UB) with known drugs established a direct correlation between the biosensor FRET signal in response to these drugs and their analgesic effect in a pain animal model. Results show that, whereas sigma-1 agonists reduce FRET signal and have low analgesic effects, sigma-1 antagonists increase FRET signal and have high analgesic effects in pain animal models.

"Thanks to this well-defined pattern -- explains Dr Ciruela -- , we can predict the analgesic behaviour of a molecule." Therefore, if FRET signal is reduced -- that is, if it is an agonist -- , it won't have analgesic effects on the pain animal model; however, if FRET signal is increased -- in other words, if it is an antagonist -- , it will have maximum analgesic effects and, therefore, it will be a suitable candidate to be tested in vivo.

The researcher points out that the new technology has already been patented, and "although is too early to get the most of it -- because FRET measures are now done one drug by one -- , it is expected that it will be soon applied in an extensive way to the development of analgesic antagonists sigma-1 receptor," highlights Ciruela. Therefore, the system will be robotized in order to develop a tool technically known as 'high-throughput screening' (HTS), in other words, a method to test many medicines in a quick and effective manner.

Analgesia: a subject area with many medical needs

There are two main groups of medicines in pain pharmacology: non-steroidal anti-inflammatory drugs (NSAIDs) and opioids. Each type has different action mechanisms with an 'analgesic ceiling' and different side effects. Whereas NSAIDs (for instance, ibuprofen) have a low-moderate analgesic potential and non-serious side effects, opioids (for instance, morphine) have high analgesic potential and serious side effects. So, there is an important analgesic gap, not only to present a risk-benefit favourable to treat moderate and severe pain, but also in the approach to pain treatment, a field in which medicines are not usually effective (for instance, in neuropathic pain).

ESTEVE focuses part of its R&D on active molecules for the treatment of neuropathic pain in patients receiving opioids. The main goal is to improve effectiveness, tolerance and safety and reduce side effects' frequency of this group of drugs. In this sense, to block sigma-1 receptor with specific antagonists constitutes a new mechanism of action for pain in a field that needs new treatments. Therefore, besides the selective sigma-1 receptor antagonist, E-52862, which is now in a phase II clinical trial, ESTEVE has a number of molecules with potential activity on this receptor.


Story Source:

The above story is based on materials provided by Universidad de Barcelona. Note: Materials may be edited for content and length.


Journal Reference:

  1. Maricel Gómez-Soler, Víctor Fernández-Dueñas, Enrique Portillo-Salido, Pilar Pérez, Daniel Zamanillo, José Miguel Vela, Javier Burgueño, Francisco Ciruela. Predicting the Antinociceptive Efficacy of σ1Receptor Ligands by a Novel Receptor Fluorescence Resonance Energy Transfer (FRET) Based Biosensor. Journal of Medicinal Chemistry, 2014; 57 (1): 238 DOI: 10.1021/jm401529t

Cite This Page:

Universidad de Barcelona. "New technology for screening potential analgesic drugs." ScienceDaily. ScienceDaily, 24 February 2014. <www.sciencedaily.com/releases/2014/02/140224092052.htm>.
Universidad de Barcelona. (2014, February 24). New technology for screening potential analgesic drugs. ScienceDaily. Retrieved October 23, 2014 from www.sciencedaily.com/releases/2014/02/140224092052.htm
Universidad de Barcelona. "New technology for screening potential analgesic drugs." ScienceDaily. www.sciencedaily.com/releases/2014/02/140224092052.htm (accessed October 23, 2014).

Share This



More Health & Medicine News

Thursday, October 23, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

Orthodontist Mom Jennifer Salzer on the Best Time for Braces

Orthodontist Mom Jennifer Salzer on the Best Time for Braces

Working Mother (Oct. 22, 2014) — Is your child ready? Video provided by Working Mother
Powered by NewsLook.com
U.S. Issues Ebola Travel Restrictions, Are Visa Bans Next?

U.S. Issues Ebola Travel Restrictions, Are Visa Bans Next?

Newsy (Oct. 22, 2014) — Now that the U.S. is restricting travel from West Africa, some are dropping questions about a travel ban and instead asking about visa bans. Video provided by Newsy
Powered by NewsLook.com
US to Track Everyone Coming from Ebola Nations

US to Track Everyone Coming from Ebola Nations

AP (Oct. 22, 2014) — Stepping up their vigilance against Ebola, federal authorities said Wednesday that everyone traveling into the US from Ebola-stricken nations will be monitored for symptoms for 21 days. (Oct. 22) Video provided by AP
Powered by NewsLook.com
Doctors Help Paralysed Man Walk Again, Patient in Disbelief

Doctors Help Paralysed Man Walk Again, Patient in Disbelief

AFP (Oct. 22, 2014) — Polish doctors describe how they helped a paralysed man walk again, with the patient in disbelief at the return of sensation to his legs. Duration: 1:04 Video provided by AFP
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:

Strange & Offbeat Stories

 

Health & Medicine

Mind & Brain

Living & Well

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