Evidence map›Paper›PMID 31817441›Full record

ArticleMolecules (Basel, Switzerland)2019

Synthesis and Pharmacological Evaluation of Hybrids Targeting Opioid and Neurokinin Receptors.

Karol Wtorek, Anna Adamska-Bartłomiejczyk, Justyna Piekielna-Ciesielska, Federica Ferrari, Chiara Ruzza, Alicja Kluczyk, Joanna Piasecka-Zelga, Girolamo Calo', Anna Janecka

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2019. 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
0.7field-weighted citation impact, top 36% 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, 10 citations in OpenAlex.

  1. 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

9 authors at 4 institutions in 2 countries.

Karol WtorekDepartment of Biomolecular Chemistry, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
Anna Adamska-BartłomiejczykDepartment of Biomolecular Chemistry, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
Justyna Piekielna-CiesielskaDepartment of Biomolecular Chemistry, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
Federica FerrariDepartment of Medical Sciences, Section of Pharmacology, University of Ferrara, 44121 Ferrara, Italy.
Chiara RuzzaDepartment of Medical Sciences, Section of Pharmacology, University of Ferrara, 44121 Ferrara, Italy.
Alicja KluczykFaculty of Chemistry, University of Wroclaw, 50-383 Wroclaw, Poland.ORCID 0000-0003-2943-2782
Joanna Piasecka-ZelgaInstitute of Occupational Medicine, Research Laboratory for Medicine and Veterinary Products in the GMP Head of Research Laboratory for Medicine and Veterinary Products, 91-348 Lodz, Poland.
Girolamo Calo'Department of Medical Sciences, Section of Pharmacology, University of Ferrara, 44121 Ferrara, Italy.
Anna JaneckaDepartment of Biomolecular Chemistry, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
Medical University of Lodz · PLUniversity of Ferrara · ITNofer Institute of Occupational Medicine · PLUniversity of Wrocław · PL

Funding

Medical University of Lodz 503/1-156-02/503-11-002National Science Centre 2015/17/B/ST5/00153
6 · The paper itself

Abstract

Morphine, which acts through opioid receptors, is one of the most efficient analgesics for the alleviation of severe pain. However, its usefulness is limited by serious side effects, including analgesic tolerance, constipation, and dependence liability. The growing awareness that multifunctional ligands which simultaneously activate two or more targets may produce a more desirable drug profile than selectively targeted compounds has created an opportunity for a new approach to developing more effective medications. Here, in order to better understand the role of the neurokinin system in opioid-induced antinociception, we report the synthesis, structure-activity relationship, and pharmacological characterization of a series of hybrids combining opioid pharmacophores with either substance P (SP) fragments or neurokinin receptor (NK1) antagonist fragments. On the bases of the in vitro biological activities of the hybrids, two analogs, opioid agonist/NK1 antagonist Tyr-[d-Lys-Phe-Phe-Asp]-Asn-d-Trp-Phe-d-Trp-Leu-Nle-NH

Indexed as

AnalgesicsNarcotic AntagonistsNeurokinin-1 Receptor AntagonistsOligopeptidesReceptors, Neurokinin-1Receptors, OpioidAnimalsCell LineDrug ToleranceMaleMiceMice, Inbred BALB CNociceptionAnalgesicsNarcotic AntagonistsNeurokinin-1 Receptor AntagonistsOligopeptidesReceptors, Neurokinin-1Receptors, Opioidfunctional assayneurokinin-1 receptoropioid receptorspeptide synthesisreceptor binding studiestolerancewrithing test

Identifiers

PMID31817441
PMCPMC6943619
OpenAlexW2994584647

What OpenQuestion holds

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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.