Evidence map›Paper›PMID 25816912›Full record

ArticleActa pharmacologica Sinica2015

Novel κ-opioid receptor agonist MB-1C-OH produces potent analgesia with less depression and sedation.

Le-sha Zhang, Jun Wang, Jian-chun Chen, Yi-min Tao, Yu-hua Wang, Xue-jun Xu, Jie Chen, Yun-gen Xu, Tao Xi, Xiao-wu Hu and 2 more

Open access · bronzeAbstract read
In one paragraph

Article in Acta pharmacologica Sinica, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.

0numbers the graph read from it
0cells of the map it votes in
20citing papers in PubMed
1.5field-weighted citation impact, top 18% 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

20 citing papers in PubMed, 35 citations in OpenAlex.

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  14. Strategies for DevelopingThe Journal of pharmacology and experimental therapeutics · 2020
    Review
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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

12 authors at 4 institutions in 1 country.

Le-sha ZhangState Key Laboratory of Drug Research, Shanghai Institute of Materia Medica and Collaborative Innovation Center for Brain Science, Chinese Academy of Sciences, Shanghai 201203, China.
Jun Wang1] State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica and Collaborative Innovation Center for Brain Science, Chinese Academy of Sciences, Shanghai 201203, China [2] Biotechnology Center, School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China.
Jian-chun ChenDepartment of Neurosurgery, Changhai Hospital, Second Military Medical University, Shanghai 200433, China.
Yi-min TaoState Key Laboratory of Drug Research, Shanghai Institute of Materia Medica and Collaborative Innovation Center for Brain Science, Chinese Academy of Sciences, Shanghai 201203, China.
Yu-hua Wang1] Biotechnology Center, School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China [2] School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
Xue-jun XuState Key Laboratory of Drug Research, Shanghai Institute of Materia Medica and Collaborative Innovation Center for Brain Science, Chinese Academy of Sciences, Shanghai 201203, China.
Jie ChenState Key Laboratory of Drug Research, Shanghai Institute of Materia Medica and Collaborative Innovation Center for Brain Science, Chinese Academy of Sciences, Shanghai 201203, China.
Yun-gen XuBiotechnology Center, School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China.
Tao XiBiotechnology Center, School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China.
Xiao-wu HuDepartment of Neurosurgery, Changhai Hospital, Second Military Medical University, Shanghai 200433, China.
Yu-jun WangState Key Laboratory of Drug Research, Shanghai Institute of Materia Medica and Collaborative Innovation Center for Brain Science, Chinese Academy of Sciences, Shanghai 201203, China.
Jing-gen LiuState Key Laboratory of Drug Research, Shanghai Institute of Materia Medica and Collaborative Innovation Center for Brain Science, Chinese Academy of Sciences, Shanghai 201203, China.
Shanghai Institute of Materia Medica · CNChina Pharmaceutical University · CNChanghai Hospital · CNSecond Military Medical University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

aimTo characterize the pharmacological profiles of a novel κ-opioid receptor agonist MB-1C-OH.

methods[(3)H]diprenorphine binding and [(35)S]GTPγS binding assays were performed to determine the agonistic properties of MB-1C-OH. Hot plate, tail flick, acetic acid-induced writhing, and formalin tests were conducted in mice to evaluate the antinociceptive actions. Forced swimming and rotarod tests of mice were used to assess the sedation and depression actions.

resultsIn [(3)H]diprenorphine binding assay, MB-1C-OH did not bind to μ- and δ-opioid receptors at the concentration of 100 μmol/L, but showed a high affinity for κ-opioid receptor (Ki=35 nmol/L). In [(35)S]GTPγS binding assay, the compound had an Emax of 98% and an EC50 of 16.7 nmol/L for κ-opioid receptor. Subcutaneous injection of MB-1C-OH had no effects in both hot plate and tail flick tests, but produced potent antinociception in the acetic acid-induced writhing test (ED50=0.39 mg/kg), which was antagonized by pretreatment with a selective κ-opioid receptor antagonist Nor-BNI. In the formalin test, subcutaneous injection of MB-1C-OH did not affect the flinching behavior in the first phase, but significantly inhibited that in the second phase (ED50=0.87 mg/kg). In addition, the sedation or depression actions of MB-1C-OH were about 3-fold weaker than those of the classical κ agonist (-)U50,488H.

conclusionMB-1C-OH is a novel κ-opioid receptor agonist that produces potent antinociception causing less sedation and depression.

Indexed as

Analgesics, OpioidAnimalsBehavior, AnimalBinding, CompetitiveCHO CellsCricetulusDepressionDisease Models, AnimalDose-Response Relationship, DrugHumansIsoquinolinesLigandsMaleMiceMotor ActivityPainAnalgesics, OpioidIsoquinolinesLigandsMB-1C-OHReceptors, Opioid, kappa

Identifiers

PMID25816912
PMCPMC4422940
OpenAlexW1976994417

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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.