Poorly controlled postoperative pain: prevalence, consequences, and prevention

TJ Gan - Journal of pain research, 2017 - Taylor & Francis
This review provides an overview of the clinical issue of poorly controlled postoperative pain
and therapeutic approaches that may help to address this common unresolved health-care …

[HTML][HTML] Critical assessment of G protein-biased agonism at the μ-opioid receptor

A Gillis, A Kliewer, E Kelly, G Henderson… - Trends in …, 2020 - cell.com
G protein-biased agonists of the μ-opioid receptor (MOPr) have been proposed as an
improved class of opioid analgesics. Recent studies have been unable to reproduce the …

The physiology, signaling, and pharmacology of dopamine receptors

JM Beaulieu, RR Gainetdinov - Pharmacological reviews, 2011 - ASPET
G protein-coupled dopamine receptors (D1, D2, D3, D4, and D5) mediate all of the
physiological functions of the catecholaminergic neurotransmitter dopamine, ranging from …

Mu opioids and their receptors: evolution of a concept

GW Pasternak, YX Pan - Pharmacological reviews, 2013 - ASPET
Opiates are among the oldest medications available to manage a number of medical
problems. Although pain is the current focus, early use initially focused upon the treatment of …

Biased receptor signaling in drug discovery

T Kenakin - Pharmacological reviews, 2019 - ASPET
A great deal of experimental evidence suggests that ligands can stabilize different receptor
active states that go on to interact with cellular signaling proteins to form a range of different …

Nociceptin/orphanin FQ receptor structure, signaling, ligands, functions, and interactions with opioid systems

L Toll, MR Bruchas, BM Cox, NT Zaveri - Pharmacological reviews, 2016 - ASPET
The NOP receptor (nociceptin/orphanin FQ opioid peptide receptor) is the most recently
discovered member of the opioid receptor family and, together with its endogenous ligand …

Biased agonism: lessons from studies of opioid receptor agonists

E Kelly, A Conibear, G Henderson - Annual review of …, 2023 - annualreviews.org
In ligand bias different agonist drugs are thought to produce distinct signaling outputs when
activating the same receptor. If these signaling outputs mediate therapeutic versus adverse …

Teaching old receptors new tricks: biasing seven-transmembrane receptors

S Rajagopal, K Rajagopal, RJ Lefkowitz - Nature reviews Drug …, 2010 - nature.com
Abstract Seven-transmembrane receptors (7TMRs; also known as G protein-coupled
receptors) are the largest class of receptors in the human genome and are common targets …

Biased agonism: An emerging paradigm in GPCR drug discovery

Z Rankovic, TF Brust, LM Bohn - Bioorganic & medicinal chemistry letters, 2016 - Elsevier
G protein coupled receptors have historically been one of the most druggable classes of
cellular proteins. The members of this large receptor gene family couple to primary effectors …

Therapeutic potential of β-arrestin-and G protein-biased agonists

EJ Whalen, S Rajagopal, RJ Lefkowitz - Trends in molecular medicine, 2011 - cell.com
Members of the seven-transmembrane receptor (7TMR), or G protein-coupled receptor
(GPCR), superfamily represent some of the most successful targets of modern drug therapy …