Dualism, allosteric modulation, and biased signaling of opioid receptors: Future therapeutic potential

Abstract

Opioids are still the drugs of choice for the treatment of acute post-surgical pain and chronic cancer pain. Overprescribing of these drugs has given rise to an “opioid crisis” in some countries. In this context, attention has been drawn to the therapeutic potential of various ligands that act as allosteric modulators of orthosteric binding sites and modulate the drug’s activity, affinity, potency, and even efficacy.