An updated assessment of the translational promise of G-protein-biased kappa opioid receptor agonists to treat pain and other indications without debilitating adverse …

AR French, RM van Rijn - Pharmacological research, 2022 - Elsevier
Kappa opioid receptor (κOR) agonists lack the abuse liability and respiratory depression
effects of clinically used mu opioid receptor (μOR) analgesics and are hypothesized to be …

[HTML][HTML] Diels–Alder Adducts of Morphinan-6, 8-Dienes and Their Transformations

J Marton, A Fekete, P Cumming, S Hosztafi, P Mikecz… - Molecules, 2022 - mdpi.com
6, 14-ethenomorphinans are semisynthetic opiate derivatives containing an ethylene bridge
between positions 6 and 14 in ring-C of the morphine skeleton that imparts a rigid molecular …

SLL-627 is a highly selective and potent κ opioid receptor (KOR) agonist with an unexpected nonreduction in locomotor activity

L Kong, X Shu, S Tang, R Ye, H Sun… - Journal of Medicinal …, 2022 - ACS Publications
Undue central nervous system (CNS) side effects including dysphoria and sedation remain
to be a challenge for the development of κ opioid receptor (KOR) agonists as effective and …

Discovery of an M-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaine as a Selective, Potent, and Orally Active κ-Opioid Receptor …

Q He, Y Wei, X Liu, R Ye, L Kong, Z Li… - Journal of Medicinal …, 2021 - ACS Publications
The search for selective kappa opioid receptor (κOR) agonists with an improved safety
profile is an area of interest in opioid research. In this work, a series of m-substituted analogs …

Discovery of an Ortho-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid …

Z Li, R Ye, Q He, J Lu, Y Sun, X Sun… - Journal of Medicinal …, 2024 - ACS Publications
Research into kappa opioid receptor (KOR) agonists with attenuated central-nervous-system
side effects is a critical focus for developing productive and safe analgesics. Herein, a series …

Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone

L Kong, K Ning, X Liu, J Lu, B Chen, R Ye, Z Li… - European Journal of …, 2023 - Elsevier
The discovery and development of novel μ-opioid receptor (MOR) antagonists is a
significant area to combat Opioid Use Disorder (OUD). In this work, a series of para …

Exploration of the SAR connection between morphinan-and arylacetamide-based κ opioid receptor (κOR) agonists using the strategy of bridging

X Liu, S Jiang, L Kong, R Ye, L Xiao, X Xu… - ACS Chemical …, 2021 - ACS Publications
κ opioid receptor (κOR) is a subtype of opioid receptors, and there are two major κOR
agonists currently available, morphinans and arylacetamides, which are structurally distinct …

Historical perspectives and recent advances in small molecule ligands of selective/biased/multi-targeted μ/δ/κ opioid receptor (2019–2022)

Y He, Q Su, L Zhao, L Zhang, L Yu, J Shi - Bioorganic Chemistry, 2023 - Elsevier
The opioids have been used for more than a thousand years and are not only the most
widely prescribed drugs for moderate to severe pain and acute pain, but also the preferred …

Morphinan Evolution: The Impact of Advances in Biochemistry and Molecular Biology

K Kajino, A Tokuda, T Saitoh - The Journal of Biochemistry, 2024 - academic.oup.com
Morphinan-based opioids, derived from natural alkaloids like morphine, codeine and
thebaine, have long been pivotal in managing severe pain. However, their clinical utility is …

Cross‐Coupling‐Cyclocondensation Reaction Sequence to Access a Library of Ring‐C Bridged Pyrimidino‐tetrahydrothebaines and Pyrimidinotetrahydrooripavines

AO Finke, MY Ravaeva, VI Krasnov… - …, 2021 - Wiley Online Library
Abstract Ring‐C bridged 1‐(pyrimidinyl) tetrahydrothebaines were convenience synthesized
by a consecutive three‐component alkynylation–cyclocondensation sequence starting from …