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Breathing rhythm and pattern and their influence on emotion
Breathing is a vital rhythmic motor behavior with a surprisingly broad influence on the brain
and body. The apparent simplicity of breathing belies a complex neural control system, the …
and body. The apparent simplicity of breathing belies a complex neural control system, the …
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 …
[HTML][HTML] Molecular recognition of morphine and fentanyl by the human μ-opioid receptor
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 …
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …
Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists
Biased agonism at G protein–coupled receptors describes the phenomenon whereby some
drugs can activate some downstream signaling activities to the relative exclusion of others …
drugs can activate some downstream signaling activities to the relative exclusion of others …
Structure-based discovery of opioid analgesics with reduced side effects
Morphine is an alkaloid from the opium poppy used to treat pain. The potentially lethal side
effects of morphine and related opioids—which include fatal respiratory depression—are …
effects of morphine and related opioids—which include fatal respiratory depression—are …
Morphine‐induced respiratory depression is independent of β‐arrestin2 signalling
Background and Purpose GPCRs can signal through both G proteins and β‐arrestin2. For
the μ‐opioid receptor, early experimental evidence from a single study suggested that G …
the μ‐opioid receptor, early experimental evidence from a single study suggested that G …
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 …
improved class of opioid analgesics. Recent studies have been unable to reproduce the …
Advances in achieving opioid analgesia without side effects
Opioids are the most effective drugs for the treatment of severe pain, but they also cause
addiction and overdose deaths, which have led to a worldwide opioid crisis. Therefore, the …
addiction and overdose deaths, which have led to a worldwide opioid crisis. Therefore, 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 …
to induce minimal arrestin recruitment and be devoid of the respiratory depressant effects …
Recent progress in assays for GPCR drug discovery
S Guo, T Zhao, Y Yun, X **e - American Journal of …, 2022 - journals.physiology.org
G-protein-coupled receptors (GPCRs), also known as seven transmembrane receptors, are
the largest family of cell surface receptors in eukaryotes. There are∼ 800 GPCRs in human …
the largest family of cell surface receptors in eukaryotes. There are∼ 800 GPCRs in human …