Strategies towards safer opioid analgesics—A review of old and upcoming targets

BR Varga, JM Streicher… - British journal of …, 2023 - Wiley Online Library
Opioids continue to be of use for the treatment of pain. Most clinically used analgesics target
the μ opioid receptor whose activation results in adverse effects like respiratory depression …

Morphine alkaloids: History, biology, and synthesis

C Wicks, T Hudlicky, U Rinner - The Alkaloids: Chemistry and Biology, 2021 - Elsevier
This chapter provides a short overview of the history of morphine since it's isolation by
Sertürner in 1805. The biosynthesis of the title alkaloid as well as all total and formal …

Structure-based design of bitopic ligands for the µ-opioid receptor

A Faouzi, H Wang, SA Zaidi, JF DiBerto, T Che, Q Qu… - Nature, 2023 - nature.com
Mu-opioid receptor (µOR) agonists such as fentanyl have long been used for pain
management, but are considered a major public health concern owing to their adverse side …

Peptide-derived ligands for the discovery of safer opioid analgesics

A Eliasof, LY Liu-Chen, Y Li - Drug discovery today, 2024 - Elsevier
Drugs targeting the μ-opioid receptor (MOR) remain the most efficacious analgesics for the
treatment of pain, but activation of MOR with current opioid analgesics also produces …

Current and future therapeutic options in pain management: Multi-mechanistic opioids involving both MOR and NOP receptor activation

F Coluzzi, L Rullo, MS Scerpa, LM Losapio, M Rocco… - CNS drugs, 2022 - Springer
Opioids are widely used in chronic pain management, despite major concerns about their
risk of adverse events, particularly abuse, misuse, and respiratory depression from …

Therapeutic potentials of NOP and MOP receptor coactivation for the treatment of pain and opioid abuse

N Kiguchi, H Ding, MC Ko - Journal of neuroscience research, 2022 - Wiley Online Library
Following the identification of the nociceptin/orphanin FQ (N/OFQ) peptide (NOP) as an
endogenous ligand for the NOP receptor, ample evidence has revealed unique functional …

Signaling Modulation Mediated by Ligand Water Interactions with the Sodium Site at μOR

RS Ople, N Ramos-Gonzalez, Q Li… - ACS Central …, 2024 - ACS Publications
The mu opioid receptor (μOR) is a target for clinically used analgesics. However, adverse
effects, such as respiratory depression and physical dependence, necessitate the …

Spotlight on nociceptin/orphanin FQ receptor in the treatment of pain

A El Daibani, T Che - Molecules, 2022 - mdpi.com
In our society today, pain has become a main source of strain on most individuals. It is
crucial to develop novel treatments against pain while focusing on decreasing their adverse …

Multitargeted opioid ligand discovery as a strategy to retain analgesia and reduce opioid-related adverse effects

MT Smith, D Kong, A Kuo, MZ Imam… - Journal of Medicinal …, 2023 - ACS Publications
The global “opioid crisis” has placed enormous pressure on the opioid ligand discovery
community to produce novel opioid analgesics with superior opioid-related adverse-effect …

[HTML][HTML] IUPHAR THEMED ISSUE–Emerging Targets for the Treatment of Pain Bivalent and Bifunctional Opioid Receptor Ligands as Novel Analgesics

KJ Rehrauer, CW Cunningham - Pharmacological Research, 2023 - Elsevier
Though efficacious in managing chronic, severe pain, opioid analgesics are accompanied
by significant adverse effects including constipation, tolerance, dependence, and respiratory …