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More valium please…

valium.jpgScientists have sussed out why people become addicted to diazepam – the drug formerly known as valium – and potentially opened the door to non-addictive versions of the drug.

Benzodiazepines like valium are known to be addictive, but the mechanism underlying this addiction was mysterious.

Now a team led by Christian Lüscher of the University of Geneva found that these types of pharmaceuticals increase levels of dopamine – the gratification brain chemical – just like opioids and cannabinoids. Specifically, benzodiazepine (BDZ) derivatives switch on a neurotransmitter known as GABA, which increases the firing of dopamine neurons, activating the reward pathway. Their results from experiments in mice are published this week in Nature.

By injecting BDZs into mice, the researchers elicited excitement in dopamine cells. Using strategies to block the BDZ binding site on GABA, such as administering BDZ along with a compound that blocks its GABA binding site and using mice genetically engineered so that BDZs were unable to bind, the researchers found that functional GABA receptors were needed for the addictive response.

Diazepam is used both clinically and recreationally to relieve anxiety, soothe acute delirium tremens in alcohol withdrawal, and ease muscle spasms. It grew in popularity among drug addicts as a cheap substitute for heroin and was once one of the world’s most widely prescribed drugs, associated with the acceptable, suburban face of drug-taking, even becoming known as ‘Mother’s Little Helper’.

Drug companies have been trying for some time to develop next-generation benzodiazepines by tweaking their chemical make-up to deliver a more selective effect that avoids unwanted side effects, but it has so far proved an uphill struggle (Reuters).

This new study gives hope for the ease of symptoms without dependence.

“Our work unravels the molecular basis of the defining pharmacological features that BDZs share with addictive drugs, which we believe will be key for designing new BDZs with lower addiction liability,” write the authors in their paper.

A News and Views piece accompanying the work declares the research a “landmark for the field”.

Image: photo by andy54321 via Flickr under creative commons.

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    Uncle Al said:

    Non tamen solam intendit interiorem, immo interior nulla est, nisi foris operetur varias carnis mortificationes.

    The productive are scourged toward ever greater outputs, to be harvested that the unproductive are drugged and caged. Thus recreational pharmaceuticals’ situational ethics.

    When US troops trod through hectares of Afghani opium poppy fields, one wonders… where are the combat botanists winning the War on Drugs?

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