S Fritzwanker, S Schulz, A Kliewer - Molecules, 2021 - mdpi.com
Opioid-associated overdoses and deaths due to respiratory depression are a major public health problem in the US and other Western countries. In the past decade, much research …
A Kliewer, A Gillis, R Hill, F Schmiedel… - British journal of …, 2020 - Wiley Online Library
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 …
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 …
SM DeWire, DS Yamashita, DH Rominger, G Liu… - … of Pharmacology and …, 2013 - ASPET
The concept of ligand bias at G protein-coupled receptors broadens the possibilities for agonist activities and provides the opportunity to develop safer, more selective therapeutics …
Drugs targeting the G protein-coupled μ-opioid receptor (μOR) are the most effective analgesics available but are also associated with fatal respiratory depression. While some …
I Bachmutsky, XP Wei, A Durand, K Yackle - elife, 2021 - elifesciences.org
Opioids are perhaps the most effective analgesics in medicine. However, between 1999 and 2018, over 400,000 people in the United States died from opioid overdose. Excessive …
L Webster, RL Rauck - Journal of Opioid Management, 2021 - europepmc.org
Opioids are an important tool in the treatment of pain, but opioid overdose has become a serious health issue. Most opioid-related deaths are caused by respiratory depression, and …
V Le Rouzic, A Narayan, A Hunkle… - Anesthesia & …, 2019 - journals.lww.com
BACKGROUND: Levorphanol is a potent analgesic that has been used for decades. Most commonly used for acute and cancer pain, it also is effective against neuropathic pain. The …
The search for safer opioid analgesics that have reduced liability for tolerance, addiction, and lethal overdose due to respiratory depression has met with little success for well over a …