Opiates such as morphine are effective in relieving pain. Their big disadvantage: they make you dazed, dependent and can slow down breathing threateningly. An international group led by Peter Gmeiner from the Friedrich-Alexander-Universität Erlangen-Nürnberg has now developed active ingredients that activate the adrenaline instead of the opioid receptors in the brain. The new compounds have similar pain-relieving properties, but not the unpleasant side effects of opioids.
For their analyzes, the experts caught the eye of the A2 adrenozeptor, to which some approved pain relievers are already targeting. This includes, for example, dexmedetomidine, but this has a strongly sedative effect, so it makes very tired. In a virtual library with more than 300 million different molecules, Gmeiner and his colleagues search for alternatives that could fit the receptor from construction. After a number of complex virtual simulations, they selected about 50 molecules for synthesis, two of which then met the desired criteria (such as good binding properties). The researchers optimized these molecules with regard to physical properties and finally synthesized two substances, the effectiveness and tolerance of which they demonstrated in the animal model. The results published in the specialist magazine »Science« could be a milestone in the development of non -opioid pain relievers, especially since the fabrics are comparatively easy to produce. However, Gmeiner has to dampen hopes for a quick application in human medicine: »We are currently still talking about basic research. The development of medication is subject to strict controls and, in addition to considerable financial means, needs a lot of time. Nevertheless, these results make us very optimistic. "
