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 …

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 …

Dynorphin/kappa opioid receptor signaling in preclinical models of alcohol, drug, and food addiction

A Karkhanis, KM Holleran, SR Jones - International review of neurobiology, 2017 - Elsevier
The dynorphin/kappa opioid receptor (KOR) system is implicated in the “dark side” of
addiction, in which stress exacerbates maladaptive responses to drug and alcohol …

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 …

Synthesis and κ-opioid receptor activity of furan-substituted salvinorin A analogues

AP Riley, CE Groer, D Young, AW Ewald… - Journal of medicinal …, 2014 - ACS Publications
The neoclerodane diterpene salvinorin A, found in the leaves of Salvia divinorum, is a potent
κ-opioid receptor agonist, making it an attractive scaffold for development into a treatment for …

From plant to chemistry: Sources of active opioid antinociceptive principles for medicinal chemistry and drug design

R Turnaturi, S Piana, S Spoto, G Costanzo, L Reina… - Molecules, 2023 - mdpi.com
Pain continues to be an enormous global health challenge, with millions of new untreated or
inadequately treated patients reported annually. With respect to current clinical applications …

A review of salvinorin analogs and their kappa-opioid receptor activity

JJ Roach, RA Shenvi - Bioorganic & medicinal chemistry letters, 2018 - Elsevier
The plant metabolite salvinorin A potently and selectively agonizes the human kappa-opioid
receptor, an emerging target for next-generation analgesics. Here we review analogs of the …

Salvinorin A, a kappa-opioid receptor agonist hallucinogen: pharmacology and potential template for novel pharmacotherapeutic agents in neuropsychiatric disorders

ER Butelman, MJ Kreek - Frontiers in Pharmacology, 2015 - frontiersin.org
Salvinorin A is a potent hallucinogen, isolated from the ethnomedical plant Salvia divinorum.
Salvinorin A is a selective high efficacy kappa-opioid receptor (KOPr) agonist, and thus …

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 …