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 …

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 …

Morphinan derivatives with an oxabicyclo [3.2. 1] octane structure as dual agonists toward δ and κ opioid receptors

Y Uenohara, S Tsumura, S Hirayama, E Higashi… - Bioorganic & Medicinal …, 2022 - Elsevier
The κ opioid receptor (KOR) is one of the promising targets to develop analgesics lacking
morphine like side effects. To seek a novel KOR agonist we designed 6-amide derivatives …

Novel selective κ agonists SLL-039 and SLL-1206 produce potent antinociception with fewer sedation and aversion

Y Wei, Y Ma, S Yao, L Kong, X Liu, J Chai… - Acta Pharmacologica …, 2022 - nature.com
Abstract SLL-039 (N-cyclopropylmethyl-7α− 4′-(N'-benzoyl) amino-phenyl-6, 14-
endoethano-tetrahydronorthebaine) and SLL-1206 (N-cyclopropylmethyl-7α− 3′-(p …

Synthesis and pharmacology of a novel κ opioid receptor (KOR) agonist with a 1, 3, 5-trioxazatriquinane skeleton

S Hirayama, N Wada, T Nemoto, T Iwai… - ACS Medicinal …, 2014 - ACS Publications
We designed and synthesized the 1, 3, 5-trioxazatriquinane derivatives with m-
hydroxyphenyl groups. These compounds include the phenethylamine structure within them …

The pharmacological heterogeneity of nepenthone analogs in conferring highly selective and potent κ-opioid agonistic activities

W Li, JD Long, YY Qian, Y Long, XJ Xu… - ACS Chemical …, 2017 - ACS Publications
To develop novel analgesics with no side effects or less side effects than traditional opioids
is highly demanded to treat opioid receptor mediated pain and addiction issues. Recently, κ …

A cell-based, high-throughput homogeneous time-resolved fluorescence assay for the screening of potential κ-opioid receptor agonists

Y Wang, M Yan, G Zheng, L He, H Yang - Acta Pharmacologica Sinica, 2014 - nature.com
Aim: The aim of this study was to identify κ-opioid receptor (KOR) agonists from a library of
80 000 small-molecule compounds and provide the experimental basis for the development …

Synthesis of 6, 14-epoxymorphinan derivatives and their pharmacologies

T Nemoto, N Yamamoto, A Watanabe, H Fujii… - Bioorganic & medicinal …, 2011 - Elsevier
A novel 6, 14-epoxymorphinan benzamide derivative (NS22) that was previously reported
showed opioid κ receptor agonistic activity and analgesic activity. The unsatisfactory κ …