Contact Information:

Media Contact

617-954-3971 (Boston Press Center, Aug. 16-19)

Michael Bernstein
202-872-6042 (D.C. Office)
301-275-3221 (Cell)
m_bernstein@acs.org

Katie Cottingham, Ph.D.
301-775-8455 (Cell)
k_cottingham@acs.org




Kredyty mieszkaniowe Kredyty mieszkaniowe

Sprawdź aktualny ranking najlepszych kredytów mieszkaniowych w Polsce - atrakcyjne kredytowanie nieruchomości.

PRESS-NEWS.org - Press Release Distribution
FREE PRESS RELEASES DISTRIBUTION
RSS - Press News Release
Add Press Release

New compounds could reduce alcoholics' impulse to drink


2015-08-19
(Press-News.org) BOSTON, Aug. 19, 2015 -- Alcoholism inflicts a heavy physical, emotional and financial toll on individuals and society. Now new discoveries and promising animal studies are offering a glimmer of hope that a new class of drugs could treat the disease without many of the unwanted side effects caused by current therapies.

Researchers are presenting the results of their work today at the 250th National Meeting & Exposition of the American Chemical Society (ACS), the world's largest scientific society. The meeting features more than 9,000 presentations on a wide range of science topics and is being held here through Thursday.

"Alcoholism is a major problem in the U.S.," V. V. N. Phani Babu Tiruveedhula says. "Alcohol abuse costs almost $220 billion to the U.S. economy every year. That's a shocking number. We need a better treatment right now." Tiruveedhula is a graduate student at the University of Wisconsin, Milwaukee.

The exact causes of alcoholism are not well understood, but the researchers explain that the urge to drink is related to the brain's pleasure centers. Scientists have found that alcohol triggers the brain to release dopamine, the same neurochemical whose levels increase in response to pleasurable behavior like eating, sex or listening to music.

Some drugs currently available to treat alcoholism are aimed at dopamine. "They dampen out the dopamine system a little bit, so you don't get so happy when you have an alcoholic beverage," says James Cook, Ph.D., a chemist at the University of Wisconsin, Milwaukee, who advises Tiruveedhula. But these medications, derived from a class of compounds called opioid antagonists, cause depression in some patients, Cook notes. And they're addictive themselves, which can lead to drug abuse. Valium is an example of another common drug used to treat alcoholism that is also addictive.

Looking for an alternative, Cook focused on molecules known to cause some of the same results as Valium and the opioid antagonists without the unwanted side effects. For almost two decades, Cook collaborated with the late Harry June, Ph.D., a psychopharmacologist at Howard University. They conducted laboratory tests to understand the effects of these new compounds and to discover which ones work best.

Now, Tiruveedhula has made several of these promising beta-carboline compounds that could represent the future of alcoholism treatment. Tiruveedhula simplified their manufacture from eight steps to just two, while increasing the yield tenfold and eliminating unwanted byproducts. Cook says these potential medications could be taken orally.

In tests using rats bred to crave alcohol, the scientists found that administering these compounds drastically diminished the rats' drinking. What's more, they observed very few of the side effects common to alcoholism treatment drugs, such as depression and losing the ability to experience pleasure. The drugs appeared to reduce anxiety in "alcoholic" rats, but not in control rats. Because this is different from what is seen with current drugs, the researchers think the result hints that the new compounds work much differently than opioid antagonists. As such, the beta-carbolines may also be less addictive.

"What excites me is the compounds are orally active, and they don't cause depression like some drugs do," says Cook.

The group is continuing to test the compounds in additional animal studies. Cook has patented several of the most promising compounds, and he is starting to explore possible partnerships with drug makers that could lead to medications.

If everything works out, Cook says, a drug could be ready for the market in five to six years.

INFORMATION:

A press conference on this topic will be held Wednesday, Aug. 19, at 10:30 a.m. Eastern time in the Boston Convention & Exhibition Center. Reporters may check-in at Room 153B in person, or watch live on YouTube http://bit.ly/ACSLiveBoston. To ask questions online, sign in with a Google account.

The researchers acknowledge funding from the National Institute on Alcohol Abuse and Alcoholism.

The American Chemical Society is a nonprofit organization chartered by the U.S. Congress. With more than 158,000 members, ACS is the world's largest scientific society and a global leader in providing access to chemistry-related research through its multiple databases, peer-reviewed journals and scientific conferences. Its main offices are in Washington, D.C., and Columbus, Ohio.

To automatically receive news releases from the American Chemical Society, contact newsroom@acs.org.

Note to journalists: Please report that this research was presented at a meeting of the American Chemical Society.

Follow us: Twitter | Facebook

Title Design and regiospecific synthesis of 3-substituted β-carbolines as a GABAA subtype selective agents for the treatment of alcohol abuse

Abstract Alcohol abuse is known to mediated, in part, by GABAA receptors. GABAA receptors are the major inhibitory chloride ion channels while γ-aminobutyric acid (GABA) is the endogenous ligand for this system in the central nervous system. Alcoholism plays a significant role in public health concerns impacting physical and mental well-being, family structure and occupational stability. β-Carboline-3-carboxylate-t-butyl ester [βCCt] and 3-propoxy-β-carboline hydrochloride [3PBC·HCl] function as mixed benzodiazepine receptor agonist-antagonists, and they preferentially bind at the benzodiazepine GABAA α-1 receptor. Results have shown that systemic and direct infusion of βCCt or 3-PBC·HCl into the ventral pallidum produces remarkably selective reduction in alcohol responding in alcohol preferring (P) and high alcohol drinking (HAD) rats. The ligands were also weakly anxiolytic in these genetic rat lines but not anxiolytic in normal rats. This indicates that these types of β-carbolines may represent a non-addicting treatment for human alcoholics. Initially βCCt and 3-PBC were synthesized via a 5 step (35 % yield) and 8 step (8 % yield) protocol, respectively. In an attempt to replace these time consuming syntheses, a new route involving 2 steps was developed. This new route involved a palladium catalyzed Buchwald-Hartwig coupling, and an intramolecular Heck reaction as key steps. The later reaction led to two regioisomeric β- and d- carbolines. Regioselective synthesis of β-carbolines was achieved by simply changing the chlorine position from the benzene ring to the pyridine ring. This 2-step protocol decreased the number of steps, eliminated the unwanted regioisomer and improved the overall yields. Using this protocol a number of 3-substituted β-carbolines analogs were synthesized. Among these analogs, 3-ISOPBC·HCl appeared to be a potential lead anti-alcohol (self-administration) agent active against binge drinking in maternally deprived (MD) rats. The development, application of this synthetic route and in vivo studies will be presented.


ELSE PRESS RELEASES FROM THIS DATE:

Helium anomaly preceded Mount Ontake eruption

Helium anomaly preceded Mount Ontake eruption
2015-08-19
University of Tokyo researchers discovered an increase in a helium isotope during a ten-year period before the 2014 Mount Ontake eruption in central Japan. The finding suggests that this helium isotope anomaly is related to activation of the volcano's magma system and could be a valuable marker for long-term risk mitigation concerning volcanic eruption. Small quantities of the isotope helium-3 are present in the mantle, while helium-4 is produced in the crust and mantle by radioactive decay. A higher ratio of helium-3 to helium-4 therefore indicates that a sample of helium ...

The global cost of unsafe abortion

2015-08-19
Seven million women a year in the developing world are treated in healthcare facilities for complications following unsafe abortion, finds a study published today (19 August) in BJOG: An International Journal of Obstetrics & Gynaecology (BJOG). Every day, approximately 800 women die from preventable causes related to pregnancy and childbirth. Unsafe abortion accounts for 8 - 15% of maternal deaths and remains one of the leading causes of maternal mortality worldwide.[1] However, these figures do not take into account the number of women who are surviving but need hospital ...

How UEA research could help build computers from DNA

How UEA research could help build computers from DNA
2015-08-19
New research from the University of East Anglia could one day help build computers from DNA. Scientists have found a way to 'switch' the structure of DNA using copper salts and EDTA (Ethylenediaminetetraacetic acid) - an agent commonly found in shampoo and other household products. It was previously known that the structure of a piece of DNA could be changed using acid, which causes it to fold up into what is known as an 'i-motif'. But new research published today in the journal Chemical Communications reveals that the structure can be switched a second time into ...

Nine-gene MPI can provide accurate survival stratification in patients with NSCLC

2015-08-18
A nine-gene molecular prognostic index (MPI) for patients with early-stage non-small cell lung cancer (NSCLC) was able to provide accurate survival stratification and could potentially inform the use of adjuvant therapy in patients struggling with the disease, according to a study published August 18 in the JNCI: Journal of the National Cancer Institute. Non-small cell lung cancer (NSCLC) accounts for roughly 85% of all lung cancers, additionally; lung cancer is the leading cause of cancer death through out the world. While gene expression profiles have been shown to ...

Reports on US geoscience education published by AGI's Center for Geoscience & Society

2015-08-18
Alexandria, VA - The American Geosciences Institute's Center for Geoscience and Society is pleased to release two reports concerning geosciences education in the United States. The reports were developed in response to the need for comprehensive monitoring of the U.S. educational system in terms of the instruction of geoscience content and participation in geoscience-related learning experiences. The reports are based on data pertaining to science education collected from all 50 states and the District of Columbia. The "Report on the Status of K-5 Geosciences Education ...

Scientist: Most complete human brain model to date is a 'brain changer'

2015-08-18
COLUMBUS, Ohio - Scientists at The Ohio State University have developed a nearly complete human brain in a dish that equals the brain maturity of a five-week-old fetus. The brain organoid, engineered from adult human skin cells, is the most complete human brain model yet developed, said Rene Anand, professor of biological chemistry and pharmacology at Ohio State. The lab-grown brain, about the size of a pencil eraser, has an identifiable structure and contains 99 percent of the genes present in the human fetal brain. Such a system will enable ethical and more rapid ...

Use of contact precautions should be customized based on local needs and resources

2015-08-18
Baltimore, August 18, 2015--Contact precautions are recommended by the Centers for Disease Control and Prevention (CDC) for all patients known to be infected with or carrying multidrug-resistant organisms (MDROs) such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). Yet, the use of contact precautions--which require a patient to be isolated in a single hospital room and health care providers to wear a gown and gloves when caring for patients--is widely debated in the medical community. To help inform best practices, a ...

Harnessing the butterfly effect

2015-08-18
This news release is available in French. The atmosphere is so unstable that a butterfly flapping its wings can, famously, change the course of weather patterns. The celebrated "butterfly effect" also means that the reliability of weather forecasts drops sharply beyond 10 days. Beyond this, there are strong fluctuations in temperature, with increases tending to be followed by decreases, and vice-versa. The same pattern holds true over months, years and decades. "This natural tendency to return to a basic state is an expression of the atmosphere's memory that is so ...

Is nature mostly a tinkerer or an inventor?

2015-08-18
CORAL GABLES, Fla. (August 18, 2015) - The Krüppel-like factor and specificity protein (KLF/SP) genes are found across many species, ranging from single cell organisms to humans. This gene family has been conserved during evolution, because it plays a vital role in regulating the expression of other genes. Understanding the evolutionary history of the KLF/SP gene family may shed light on major events in animal evolution and perhaps help discern some of the molecular mechanisms associated with certain human diseases, including many cancers. By closely examining the ...

Following maternal transmission, group B strep mutates to sicken infants

2015-08-18
Washington, DC - August 18, 2015 - Group B streptococcus, a mostly benign inhabitant of healthy adults, is one of the world's leading causes of neonatal sepsis and meningitis. A team of French investigators has now shown that such cases might occur when the microbe mutates within the infant following transmission from the mother. The research appeared August 17 in the Journal of Bacteriology, a publication of the American Society for Microbiology. In the study, the investigators compared for the first time samples of group B streptococcus (GBS) from pairs of infected ...

LAST 30 PRESS RELEASES:

How your brain decides blame and punishment -- and how it can be changed

Uniquely human brain region enables punishment decisions

Pinpointing punishment

Chapman University publishes research on attractiveness and mating

E-cigarettes: Special issue from Nicotine & Tobacco Research

Placental problems in early pregnancy associated with 5-fold increased risk of OB & fetal disorders

UT study: Invasive brood parasites a threat to native bird species

Criminals acquire guns through social connections

Restoring ocean health

Report: Cancer remains leading cause of death in US Hispanics

Twin study suggests genetic factors contribute to insomnia in adults

To be fragrant or not: Why do some male hairstreak butterflies lack scent organs?

International team discovers natural defense against HIV

Bolivian biodiversity observatory takes its first steps

Choice of college major influences lifetime earnings more than simply getting a degree

Dominant strain of drug-resistant MRSA decreases in hospitals, but persists in community

Synthetic biology needs robust safety mechanisms before real world application

US defense agencies increase investment in federal synthetic biology research

Robots help to map England's only deep-water Marine Conservation Zone

Mayo researchers identify protein -- may predict who will respond to PD-1 immunotherapy for melanoma

How much water do US fracking operations really use?

New approach to mammograms could improve reliability

The influence of citizen science grows despite some resistance

Unlocking secrets of how fossils form

What happens on the molecular level when smog gets into the lungs?

Using ultrasound to clean medical instruments

Platinum and iron oxide working together get the job done

Tiny silica particles could be used to repair damaged teeth, research shows

A quantum lab for everyone

No way? Charity's logo may influence perception of food in package

[Press-News.org] New compounds could reduce alcoholics' impulse to drink
Press-News.org is a service of DragonFly Company. All Rights Reserved.
Issuers of news releases are solely responsible for the accuracy of their content.