The kappa opioid receptor: a promising therapeutic target for multiple pathologies

ML Dalefield, B Scouller, R Bibi… - Frontiers in Pharmacology, 2022 - frontiersin.org
Kappa-opioid receptors (KOR) are widely expressed throughout the central nervous system,
where they modulate a range of physiological processes depending on their location …

Biased opioid ligands

A Faouzi, BR Varga, S Majumdar - Molecules, 2020 - mdpi.com
Achieving effective pain management is one of the major challenges associated with
modern day medicine. Opioids, such as morphine, have been the reference treatment for …

Terpenoids, Cannabimimetic Ligands, beyond the Cannabis Plant

ECD Gonçalves, GM Baldasso, MA Bicca, RS Paes… - Molecules, 2020 - mdpi.com
Medicinal use of Cannabis sativa L. has an extensive history and it was essential in the
discovery of phytocannabinoids, including the Cannabis major psychoactive compound—Δ9 …

A review of the therapeutic potential of recently developed G protein-biased kappa agonists

KL Mores, BR Cummins, RJ Cassell… - Frontiers in …, 2019 - frontiersin.org
Between 2000 and 2005 several studies revealed that morphine is more potent and exhibits
fewer side effects in beta-arrestin 2 knockout mice. These findings spurred efforts to develop …

Natural products for the treatment of pain: chemistry and pharmacology of salvinorin A, mitragynine, and collybolide

S Chakraborty, S Majumdar - Biochemistry, 2020 - ACS Publications
Pain remains a very pervasive problem throughout medicine. Classical pain management is
achieved through the use of opiates belonging to the mu opioid receptor (MOR) class, which …

[HTML][HTML] Classic and non‐classic psychedelics for substance use disorder: A review of their historic, past and current research

FR Mendes, C dos Santos Costa, VD Wiltenburg… - Addiction …, 2022 - Elsevier
Substance use disorder (SUD) is a global public health concern that affects millions of
people worldwide. Considering current research, addiction has been noted as the last stage …

Design of κ-opioid receptor agonists for the development of potential treatments of pain with reduced side effects

F Santino, L Gentilucci - Molecules, 2023 - mdpi.com
The κ-opioid receptor (KOR) has recently emerged as an alternative therapeutic target for
the development of pain medications, without deleterious side effects associated with the μ …

Kappa opioid receptor antagonists as potential therapeutics for stress-related disorders

ML Jacobson, CA Browne, I Lucki - Annual review of …, 2020 - annualreviews.org
Exposure to stressful stimuli activates kappa opioid receptor (KOR) signaling, a process
known to produce aversion and dysphoria in humans and other species. This endogenous …

Comprehensive overview of biased pharmacology at the opioid receptors: biased ligands and bias factors

J De Neve, TMA Barlow, D Tourwé, F Bihel… - RSC Medicinal …, 2021 - pubs.rsc.org
One of the main challenges in contemporary medicinal chemistry is the development of safer
analgesics, used in the treatment of pain. Currently, moderate to severe pain is still treated …

Signaling properties of structurally diverse kappa opioid receptor ligands: toward in vitro models of in vivo responses

AD Dunn, B Reed, J Erazo, A Ben-Ezra… - ACS chemical …, 2019 - ACS Publications
Biased ligands preferentially activate certain signaling pathways downstream of their target
receptor, leading to differential physiological or behavioral responses downstream. The …