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 …

Biased ligands at opioid receptors: Current status and future directions

T Che, H Dwivedi-Agnihotri, AK Shukla, BL Roth - Science signaling, 2021 - science.org
The opioid crisis represents a major worldwide public health crisis that has accelerated the
search for safer and more effective opioids. Over the past few years, the identification of …

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 …

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 …

Endogenous opiates and behavior: 2022

RJ Bodnar - Peptides, 2023 - Elsevier
This paper is the forty-fifth consecutive installment of the annual anthological review of
research concerning the endogenous opioid system, summarizing articles published during …

The role of carbon monoxide, heme oxygenase 1, and the Nrf2 transcription factor in the modulation of chronic pain and their interactions with opioids and …

O Pol - Medicinal Research Reviews, 2021 - Wiley Online Library
Chronic pain and its associated comorbidities are difficult to treat, even when the most
potent analgesic compounds are used. Thus, research on new strategies to effectively …

Comprehensive overview of biased pharmacology at the opioid receptors: biased ligands and bias factors

J De Neve, TMA Barlow, D Tourwé, F Bihel… - RSC Medicinal …, 2021 - pubs.rsc.org
One of the main challenges in contemporary medicinal chemistry is the development of safer
analgesics, used in the treatment of pain. Currently, moderate to severe pain is still treated …

Peripherally acting opioid analgesics and peripherally-induced analgesia

V Martínez, R Abalo - Behavioural pharmacology, 2020 - journals.lww.com
The management of pain, particularly chronic pain, is still an area of medical need. In this
context, opioids remain a gold standard for the treatment of pain. However, significant side …

Historical perspectives and recent advances in small molecule ligands of selective/biased/multi-targeted μ/δ/κ opioid receptor (2019–2022)

Y He, Q Su, L Zhao, L Zhang, L Yu, J Shi - Bioorganic Chemistry, 2023 - Elsevier
The opioids have been used for more than a thousand years and are not only the most
widely prescribed drugs for moderate to severe pain and acute pain, but also the preferred …

Progress on the development of Class A GPCR‐biased ligands

P Morales, MM Scharf, M Bermudez… - British Journal of …, 2024 - Wiley Online Library
Class AG protein‐coupled receptors (GPCRs) continue to garner interest for their essential
roles in cell signalling and their importance as drug targets. Although numerous drugs in the …