Opioids and their Receptors

Abstract

Opioids, derived from Papaver somniferum, have played a significant role in human history since 3400 BC, spanning recreational and medicinal uses. Opioid receptors in the central and peripheral nervous systems mediate their effects, primarily through inhibitory GABAergic interneurons. These are G-protein coupled receptors, with three primary types: μ, κ, and δ, each influencing various physiological and psychological functions. Opioids are classified based on their action on these receptors as full agonists, partial agonists, mixed agonist-antagonists, or antagonists. The endogenous opioid system, comprising opioid receptors and their endogenous ligands, regulates numerous physiological processes, including nociception, emotional behaviour, learning, memory, and reward pathways.

Addiction to opioids, driven by the mesolimbic dopaminergic system, results in significant neurological changes, leading to tolerance, dependency, and severe withdrawal symptoms. Opioid use can cause short-term effects like analgesia and stress reduction, but long-term use leads to tolerance, dependency, and various physiological disorders. The opioid epidemic in the United States shows the urgent need for a deeper understanding of opioid mechanisms to develop effective treatment and prevention strategies, to address this ongoing crisis with comprehensive knowledge and intervention.