- New research undertaken by American and Chinese researchers may pave the way for safer opioid painkillers, thanks to the use of cryo-electron microscopy (cryo-EM) to examine the detailed structures of opioid receptors.
- By analyzing the connections between these receptors and their natural peptide partners, the researchers hope to inspire the development of peptide-based or peptide-inspired medications with fewer severe side effects.
- This research could revolutionize pain management by mitigating risks such as addiction, numbness, and potentially fatal breathing problems associated with current opioid medications.
Opioids alleviate pain by imitating a natural pain-relief process in our nervous system.
They are the most effective and powerful painkillers available.
However, they also have side effects, some of which can be severe. These include numbness, addiction, and breathing problems, which can result in fatal overdoses.
For many years, researchers have been attempting to address the issue of side effects in different ways, all of which involve one or more of the four opioid receptor subtypes. So far, those efforts have not been successful.
One ongoing approach is the development of peptide-based or peptide-inspired small molecule medications.
Peptides are brief sequences of amino acids, similar to shorter versions of proteins.
Specific naturally occurring peptides, known as endogenous peptides, attach to opioid receptors on cell surfaces to produce a pain-relieving effect, also called an analgesic effect.
Analgesics are different from anesthetics because they don’t “shut down” nerves to numb the body or change one’s state of consciousness.
The goal is to develop a peptide-based drug that provides significant pain relief without causing numbness, altering consciousness, or leading to digestive, respiratory, or addiction problems.
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