Endogenous and exogenous opioids in pain

G Corder, DC Castro, MR Bruchas… - Annual review of …, 2018 - annualreviews.org
Opioids are the most commonly used and effective analgesic treatments for severe pain, but
they have recently come under scrutiny owing to epidemic levels of abuse and overdose …

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 …

Molecular recognition of morphine and fentanyl by the human μ-opioid receptor

Y Zhuang, Y Wang, B He, X He, XE Zhou, S Guo… - Cell, 2022 - cell.com
Morphine and fentanyl are among the most used opioid drugs that confer analgesia and
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …

Structures of the entire human opioid receptor family

Y Wang, Y Zhuang, JF DiBerto, XE Zhou, GP Schmitz… - Cell, 2023 - cell.com
Opioids are effective analgesics, but their use is beset by serious side effects, including
addiction and respiratory depression, which contribute to the ongoing opioid crisis. The …

The novel μ‐opioid receptor agonist PZM21 depresses respiration and induces tolerance to antinociception

R Hill, A Disney, A Conibear, K Sutcliffe… - British journal of …, 2018 - Wiley Online Library
Background and Purpose PZM21 is a novel μ‐opioid receptor ligand that has been reported
to induce minimal arrestin recruitment and be devoid of the respiratory depressant effects …

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 …

The G-protein biased mu-opioid agonist, TRV130, produces reinforcing and antinociceptive effects that are comparable to oxycodone in rats

CA Zamarripa, SR Edwards, HN Qureshi… - Drug and Alcohol …, 2018 - Elsevier
Mu-opioid agonists (eg, oxycodone) are highly effective therapeutics for pain. However, they
also produce reinforcing effects that increase their likelihood of abuse. Recent strategies in …

Insight into pain modulation: nociceptors sensitization and therapeutic targets

A Khan, S Khan, YS Kim - Current drug targets, 2019 - ingentaconnect.com
Pain is a complex multidimensional concept that facilitates the initiation of the signaling
cascade in response to any noxious stimuli. Action potential generation in the peripheral …

The emerging role of adhesion GPCRs in cancer

AA Gad, N Balenga - ACS pharmacology & translational science, 2020 - ACS Publications
Aberrant expression, function, and mutation of G protein-coupled receptors (GPCRs) and
their signaling partners, G proteins, have been well documented in many forms of cancer …

Current strategies toward safer mu opioid receptor drugs for pain management

AT Ehrlich, BL Kieffer, E Darcq - Expert opinion on therapeutic …, 2019 - Taylor & Francis
Introduction: Pain relief remains a major public health challenge. The most efficient available
painkillers are opioids targeting the mu opioid receptor (MOR). MORs are expressed in the …