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 …
activating the same receptor. If these signaling outputs mediate therapeutic versus adverse …
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 …
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 …
substances (NPS) worldwide. With fentanyl analogues being increasingly controlled via …
Novel approaches, drug candidates, and targets in pain drug discovery
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 …
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 …
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 …
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 …
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
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 …
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 …
clinical setting. However, untoward side effects such as tolerance, dependence, respiratory …