Designing safer analgesics via μ-opioid receptor pathways

HCS Chan, D McCarthy, J Li, K Palczewski… - Trends in …, 2017 - cell.com
Pain is both a major clinical and economic problem, affecting more people than diabetes,
heart disease, and cancer combined. While a variety of prescribed or over-the-counter …

Designing safer analgesics: a focus on μ-opioid receptor pathways

JV Pergolizzi Jr, JA LeQuang, R Taylor Jr… - Expert Opinion on …, 2018 - Taylor & Francis
Introduction: The recent dramatic increase in intentional and unintentional deaths attributed
to opioids has refocused attention on the therapeutic ratio (risk–benefit ratio) of opioid …

Strategies towards safer opioid analgesics—A review of old and upcoming targets

BR Varga, JM Streicher… - British journal of …, 2023 - Wiley Online Library
Opioids continue to be of use for the treatment of pain. Most clinically used analgesics target
the μ opioid receptor whose activation results in adverse effects like respiratory depression …

Biased opioid ligands

A Faouzi, BR Varga, S Majumdar - Molecules, 2020 - mdpi.com
Achieving effective pain management is one of the major challenges associated with
modern day medicine. Opioids, such as morphine, have been the reference treatment for …

New vistas in opioid control of pain

H Mizoguchi, C Watanabe, T Sakurada… - Current opinion in …, 2012 - Elsevier
The μ-opioid receptors mainly contribute to the control of pain transmission, while a number
of splice variants may have different physiological roles. In fact, some μ-opioid receptor …

[HTML][HTML] IUPHAR THEMED ISSUE–Emerging Targets for the Treatment of Pain Bivalent and Bifunctional Opioid Receptor Ligands as Novel Analgesics

KJ Rehrauer, CW Cunningham - Pharmacological Research, 2023 - Elsevier
Though efficacious in managing chronic, severe pain, opioid analgesics are accompanied
by significant adverse effects including constipation, tolerance, dependence, and respiratory …

Targeting multiple opioid receptors–improved analgesics with reduced side effects?

T Günther, P Dasgupta, A Mann, E Miess… - British journal of …, 2018 - Wiley Online Library
Classical opioid analgesics, including morphine, mediate all of their desired and undesired
effects by specific activation of the μ‐opioid receptor (μ receptor). The use of morphine for …

Replacement of current opioid drugs focusing on MOR-related strategies

J Busserolles, S Lolignier, N Kerckhove, C Bertin… - Pharmacology & …, 2020 - Elsevier
The scarcity and limited risk/benefit ratio of painkillers available on the market, in addition to
the opioid crisis, warrant reflection on new innovation strategies. The pharmacopoeia of …

Comprehensive molecular pharmacology screening reveals potential new receptor interactions for clinically relevant opioids

KM Olson, DI Duron, D Womer, R Fell, JM Streicher - PloS one, 2019 - journals.plos.org
Most clinically used opioids are thought to induce analgesia through activation of the mu
opioid receptor (MOR). However, disparities have been observed between the efficacy of …

Potential for kappa-opioid receptor agonists to engineer nonaddictive analgesics: a narrative review

SW Kaski, AN White, JD Gross… - Anesthesia & …, 2021 - journals.lww.com
A serious adverse effect of prescription opioid analgesics is addiction, both to these
analgesics and to illicit drugs like heroin that also activate the µ-opioid receptor (MOR) …