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Designer opioids to target pain

Morphine and other alkaloids from the opium poppy are μ-opioid receptor agonists that have been used to treat pain for many centuries. These authors used a computational approach to dock over three million small molecules to the μ-opioid receptor. Structure-based optimization of the most promising structures led to the identification of a potent agonist, PZM21, with exceptional subtype selectivity for the μ-opioid receptor. In mice, PZM21 generates substantial analgesia, which is fully ablated in μ-opioid receptor knockout animals. This small molecule seems to reduce the affective component of pain, without detectably altering reflexive behaviours, and has little effect on respiration.

Nature 537, 7619 table of contents

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