Untangling the complexity of opioid receptor function

RJ Valentino, ND Volkow - Neuropsychopharmacology, 2018 - nature.com
Mu opioid receptor agonists are among the most powerful analgesic medications but also
among the most addictive. The current opioid crisis has energized a quest to develop opioid …

Opioid receptors: drivers to addiction?

E Darcq, BL Kieffer - Nature Reviews Neuroscience, 2018 - nature.com
Drug addiction is a worldwide societal problem and public health burden, and results from
recreational drug use that develops into a complex brain disorder. The opioid system, one of …

Oxycodone in the opioid epidemic: high 'liking','wanting', and abuse liability

C Kibaly, JA Alderete, SH Liu, HS Nasef… - Cellular and molecular …, 2021 - Springer
It is estimated that nearly a third of people who abuse drugs started with prescription opioid
medicines. Approximately, 11.5 million Americans used prescription drugs recreationally in …

New concepts in opioid analgesia

C Stein - Expert opinion on investigational drugs, 2018 - Taylor & Francis
Introduction: Opioids are the oldest and most potent drugs for the treatment of severe pain,
but they are burdened by detrimental side effects such as respiratory depression, addiction …

Endogenous opioid systems alterations in pain and opioid use disorder

JA Higginbotham, T Markovic, N Massaly… - Frontiers in systems …, 2022 - frontiersin.org
Decades of research advances have established a central role for endogenous opioid
systems in regulating reward processing, mood, motivation, learning and memory …

Novel approaches, drug candidates, and targets in pain drug discovery

S Obeng, T Hiranita, F León, LR McMahon… - Journal of medicinal …, 2021 - ACS Publications
Because of the problems associated with opioids, drug discovery efforts have been
employed to develop opioids with reduced side effects using approaches such as biased …

Positive allosteric modulation of the mu-opioid receptor produces analgesia with reduced side effects

R Kandasamy, TM Hillhouse… - Proceedings of the …, 2021 - National Acad Sciences
Positive allosteric modulators (PAMs) of the mu-opioid receptor (MOR) have been
hypothesized as potentially safer analgesics than traditional opioid drugs. This is based on …

Biased versus partial agonism in the search for safer opioid analgesics

J Azevedo Neto, A Costanzini, R De Giorgio… - Molecules, 2020 - mdpi.com
Opioids such as morphine—acting at the mu opioid receptor—are the mainstay for treatment
of moderate to severe pain and have good efficacy in these indications. However, these …

New binding sites, new opportunities for GPCR drug discovery

HCS Chan, Y Li, T Dahoun, H Vogel, S Yuan - Trends in biochemical …, 2019 - cell.com
Many central biological events rely on protein–ligand interactions. The identification and
characterization of protein-binding sites for ligands are crucial for the understanding of …

Natural products for the treatment of pain: chemistry and pharmacology of salvinorin A, mitragynine, and collybolide

S Chakraborty, S Majumdar - Biochemistry, 2020 - ACS Publications
Pain remains a very pervasive problem throughout medicine. Classical pain management is
achieved through the use of opiates belonging to the mu opioid receptor (MOR) class, which …