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 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 …

DARK classics in chemical neuroscience: etonitazene and related benzimidazoles

I Ujváry, R Christie, M Evans-Brown… - ACS chemical …, 2021 - ACS Publications
Etonitazene and related 2-benzylbenzimidazoles are potent analgetics invented in the
research laboratories of the Swiss pharmaceutical giant CIBA in the late 1950s. Though the …

The rise and fall of isotonitazene and brorphine: two recent stars in the synthetic opioid firmament

MM Vandeputte, AJ Krotulski… - Journal of Analytical …, 2022 - academic.oup.com
Synthetic opioids constitute one of the fastest-growing groups of new psychoactive
substances (NPS) worldwide. With fentanyl analogues being increasingly controlled via …

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 …

Oxidative metabolism as a modulator of kratom's biological actions

S Chakraborty, R Uprety, ST Slocum, T Irie… - Journal of medicinal …, 2021 - ACS Publications
The leaves of Mitragyna speciosa (kratom), a plant native to Southeast Asia, are increasingly
used as a pain reliever and for attenuation of opioid withdrawal symptoms. Using the tools of …

Comparative neuropharmacology of structurally distinct non-fentanyl opioids that are appearing on recreational drug markets worldwide

MM Vandeputte, MHM Tsai, L Chen… - Drug and alcohol …, 2023 - Elsevier
Background The emergence of novel synthetic opioids (NSOs) is contributing to the opioid
overdose crisis. While fentanyl analogs have historically dominated the NSO market, a shift …

The opioid crisis and the future of addiction and pain therapeutics

NP Coussens, GS Sittampalam, SG Jonson… - Journal of pharmacology …, 2019 - ASPET
Opioid misuse and addiction are a public health crisis resulting in debilitation, deaths, and
significant social and economic impact. Curbing this crisis requires collaboration among …

In vitro functional characterization of a panel of non-fentanyl opioid new psychoactive substances

MM Vandeputte, A Cannaert, CP Stove - Archives of toxicology, 2020 - Springer
The landscape of new psychoactive substances (NPS) is constantly evolving, with new
compounds entering the illicit drug market at a continuous pace. Of these, opioid NPS form a …

Toward directing opioid receptor signaling to refine opioid therapeutics

TW Grim, A Acevedo-Canabal, LM Bohn - Biological psychiatry, 2020 - Elsevier
The mu opioid receptor (MOR) is a diversely regulated target for the alleviation of pain in the
clinical setting. However, untoward side effects such as tolerance, dependence, respiratory …