Better than opiates: Researchers use adrenaline receptors for highly-effective pain relief. Scientists have identified new substances that have a similar pain-relieving effect to opiates, but without the negative aspects such as respiratory depression and addiction. Instead of activating opioid r
Research has uncovered new substances that have a similar pain-relieving effect to opiates, but without the negative aspects such as respiratory depression and addiction.Scientists have identified new substances that have a similar pain-relieving effect to opiates, but without the negative aspects such as respiratory depression and addiction. Instead of activating opioid receptors, they work by stimulating adrenalin receptors.
“We are focusing particularly on the molecular structures of the receptors that dock onto the pharmaceutical substances,” says Gmeiner. “It is only when we understand these on the atomic level that we can develop effective and safe active substances.” Gmeiner and a team of researchers from Erlangen, China, Canada, and the USA have now turned their attention to a new receptor that is responsible for binding adrenaline – the alpha 2A adrenergic receptor. There are already some analgesics that target this receptor such as brimonidine, clonidine, and dexmedetomidine.
After a series of complex virtual docking simulations, around 50 molecules were selected for synthesis and testing and two of these fulfilled the desired criteria. They had good bonding characteristics, activated only certain protein sub-types, and thus a very selective set of cellular signal pathways, whereas dexmedetomidine responds to a significantly wider range of proteins.
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