Evidence map›Paper›PMID 34493813›Full record

ArticleActa pharmacologica Sinica2022

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

Yuan-Yuan Wei, Yan Ma, Song-Yu Yao, Ling-Hui Kong, Xiao Liu, Jing-Rui Chai, Jing Chen, Wei Li, Yu-Jun Wang, Li-Ming Shao and 1 more

Open access · bronzeAbstract read
In one paragraph

Article in Acta pharmacologica Sinica, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.6field-weighted citation impact, top 33% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

5 citing papers in PubMed, 11 citations in OpenAlex.

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  5. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

11 authors at 5 institutions in 1 country.

Yuan-Yuan Wei *School of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Yan Ma *Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
Song-Yu YaoKey Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
Ling-Hui KongDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China.
Xiao LiuDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China.
Jing-Rui ChaiKey Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
Jing ChenKey Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
Wei LiDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China. wei-li@fudan.edu.cn.
Yu-Jun WangKey Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China. yjwang@mail.simm.ac.cn.
Li-Ming ShaoDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China. limingshao@fudan.edu.cn.
Jing-Gen LiuSchool of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing, 210009, China. jgliu@simm.ac.cn.
Fudan University · CNChinese Academy of Sciences · CNNanjing University of Chinese Medicine · CNShanghai Institute of Materia Medica · CNChina Pharmaceutical University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

SLL-039 (N-cyclopropylmethyl-7α-4'-(N'-benzoyl) amino-phenyl-6,14-endoethano-tetrahydronorthebaine) and SLL-1206 (N-cyclopropylmethyl-7α-3'-(p-methoxybenzyl) amino-phenyl-6,14-endoethano-tetrahydronorthebaine) are two 4,5-epoxymorphinan-based high selective κ receptor agonists that we recently discovered. In the present study we characterized their pharmacological properties in comparison with arylacetamide-based typical κ agonist U50,488H. We showed that both SLL-039 and SLL-1206 produced potent and long-lasting antinociceptive actions in three different rodent models of pain via activation of κ opioid receptor. In hot-plate assay, the antinociceptive potency of SLL-039 and SLL-1206 increased about 11-and 17.3-fold compared to U50,488H and morphine, respectively, with ED

Indexed as

AntipruriticsReceptors, Opioid, kappa3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-IsomerAnalgesicsBenzylaminesMorphinansMorphineThebaine3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-IsomerAnalgesicsAntipruriticsBenzylaminesMorphinansMorphineReceptors, Opioid, kappaSLL-039SLL-1206Thebaine4,5-expoxymorphinanantinociceptionconditioned place aversionmorphineNor-BNIsedationU50,488Hβ-FNAκ-opioid receptor agonist

Identifiers

PMID34493813
PMCPMC9160296
OpenAlexW3197816901

What OpenQuestion holds

Textmetadata
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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.