Endogenous and exogenous opioids in pain
Opioids are the most commonly used and effective analgesic treatments for severe pain, but
they have recently come under scrutiny owing to epidemic levels of abuse and overdose …
they have recently come under scrutiny owing to epidemic levels of abuse and overdose …
New concepts in opioid analgesia
C Stein - Expert opinion on investigational drugs, 2018 - Taylor & Francis
Introduction: Opioids are the oldest and most potent drugs for the treatment of severe pain,
but they are burdened by detrimental side effects such as respiratory depression, addiction …
but they are burdened by detrimental side effects such as respiratory depression, addiction …
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 …
Structures of the entire human opioid receptor family
Opioids are effective analgesics, but their use is beset by serious side effects, including
addiction and respiratory depression, which contribute to the ongoing opioid crisis. The …
addiction and respiratory depression, which contribute to the ongoing opioid crisis. 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 …
New binding sites, new opportunities for GPCR drug discovery
Many central biological events rely on protein–ligand interactions. The identification and
characterization of protein-binding sites for ligands are crucial for the understanding of …
characterization of protein-binding sites for ligands are crucial for the understanding of …
The G-protein biased mu-opioid agonist, TRV130, produces reinforcing and antinociceptive effects that are comparable to oxycodone in rats
CA Zamarripa, SR Edwards, HN Qureshi… - Drug and Alcohol …, 2018 - Elsevier
Mu-opioid agonists (eg, oxycodone) are highly effective therapeutics for pain. However, they
also produce reinforcing effects that increase their likelihood of abuse. Recent strategies in …
also produce reinforcing effects that increase their likelihood of abuse. Recent strategies in …
Insight into pain modulation: nociceptors sensitization and therapeutic targets
Pain is a complex multidimensional concept that facilitates the initiation of the signaling
cascade in response to any noxious stimuli. Action potential generation in the peripheral …
cascade in response to any noxious stimuli. Action potential generation in the peripheral …
The emerging role of adhesion GPCRs in cancer
AA Gad, N Balenga - ACS pharmacology & translational science, 2020 - ACS Publications
Aberrant expression, function, and mutation of G protein-coupled receptors (GPCRs) and
their signaling partners, G proteins, have been well documented in many forms of cancer …
their signaling partners, G proteins, have been well documented in many forms of cancer …
Current strategies toward safer mu opioid receptor drugs for pain management
Introduction: Pain relief remains a major public health challenge. The most efficient available
painkillers are opioids targeting the mu opioid receptor (MOR). MORs are expressed in the …
painkillers are opioids targeting the mu opioid receptor (MOR). MORs are expressed in the …