New painkillers: effects instead of side effects

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MunichSome painkillers and drugs for the treatment of addictions have an unpleasant side effect: They put you in a bad mood. American researchers have now found a way to eliminate this effect.

A protein that makes you sad

Kappa Opioid Receptor (KOR) is the name of the key through which the drugs work. The small molecule sits on the surface of nerve cells in the brain and spinal cord. If you activate KOR, the perception of pain decreases, or the desire for an addictive substance decreases. That is why there are many drugs that target this receptor.

The problem: When docking, these substances activate a molecule called beta-arrestin. This substance triggers depression, irritability, and a bad mood. Such states of mind should be avoided, especially when treating addicts, because they increase the risk of relapse, write the authors of a study group led by Lei Zhou from the Scripps Research Institute in Florida.

Custom-fit active ingredients

He and his team have developed two new compounds that bind very specifically to KOR and do not lead to the formation of beta-arrestin. The active ingredients can cross the blood-brain barrier and therefore reach the binding sites in the central nervous system as well as the currently used drugs. So far, the researchers have successfully tested the active ingredients on mice. Now they want to develop the substances further so that they are also suitable for humans. (away)

Source: Zhou et al .: Development of functionally selective, small molecule agonists at kappa opioid receptors, The Journal of Biological Chemistry, 2013, doi: 10.1074 / jbc.M113.504381

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