Evidence map›Paper›PMID 29614224›Full record

ArticleJournal of medicinal chemistry2018

Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain.

René Blöcher, Karen M Wagner, Raghavender R Gopireddy, Todd R Harris, Hao Wu, Bogdan Barnych, Sung Hee Hwang, Yang K Xiang, Ewgenij Proschak, Christophe Morisseau and 1 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.9field-weighted citation impact, top 16% 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

7 citing papers in PubMed, 22 citations in OpenAlex.

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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

11 authors at 3 institutions in 2 countries.

René BlöcherDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center , University of California Davis , One Shields Avenue , Davis , California 95616 , United States.
Karen M WagnerDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center , University of California Davis , One Shields Avenue , Davis , California 95616 , United States.
Raghavender R GopireddyDepartment of Pharmacology , University of California Davis , One Shields Avenue , Davis , California 95616 , United States.
Todd R HarrisDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center , University of California Davis , One Shields Avenue , Davis , California 95616 , United States.
Hao WuDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center , University of California Davis , One Shields Avenue , Davis , California 95616 , United States.
Bogdan BarnychDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center , University of California Davis , One Shields Avenue , Davis , California 95616 , United States.
Sung Hee HwangDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center , University of California Davis , One Shields Avenue , Davis , California 95616 , United States.
Yang K XiangDepartment of Pharmacology , University of California Davis , One Shields Avenue , Davis , California 95616 , United States.
Ewgenij ProschakInstitute of Pharmaceutical Chemistry , Goethe-University Frankfurt , Max-von-Laue-Strasse 9 , D-60438 Frankfurt am Main , Germany.ORCID 0000-0003-1961-1859
Christophe MorisseauDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center , University of California Davis , One Shields Avenue , Davis , California 95616 , United States.
Bruce D HammockDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center , University of California Davis , One Shields Avenue , Davis , California 95616 , United States.ORCID 0000-0003-1408-8317
UC Davis Comprehensive Cancer CenterVA Northern California Health Care System · USGoethe University Frankfurt · DE

Funding

Workshop on Environmental Technology Transfer and EntrepreneurshipP42ES004699 · NIEHS · UNIVERSITY OF CALIFORNIA DAVIS · PI HAMMOCK, BRUCE D · 1987 to 2021
$50.1M
ENVIRONMENTAL TOXICOLOGYT32ES007059 · NIEHS · UNIVERSITY OF CALIFORNIA DAVIS · PI Laura S Van Winkle · 1985 to 2026
$7.9M
Training Program In Basic & Translational Cardiovascular ScienceT32HL086350 · NHLBI · UNIVERSITY OF CALIFORNIA AT DAVIS · PI Martin Cadeiras, David A. Liem · 2008 to 2026
$7.1M
HYDROLYTIC ENZYMES IN THE METABOLISM OF TOXINSR01ES002710 · NIEHS · UNIVERSITY OF CALIFORNIA DAVIS · PI HAMMOCK, BRUCE D · 1985 to 2018
$4.0M
FUNCTIONAL PROPERTIES OF CA PUMPS IN HAIR CELLR01DC004215 · NIDCD · UNIVERSITY OF CINCINNATI · PI YAMOAH, EBENEZER N. · 1999 to 2003
$1.0M
Training Program in Basic and Clinical Communication ScienceT32DC008072 · NIDCD · UNIVERSITY OF CALIFORNIA AT DAVIS · PI YAMOAH, EBENEZER N · 2008 to 2012
$939k
NHLBI NIH HHS T32 HL086350NIDCD NIH HHS R01 DC004215NIDCD NIH HHS T32 DC008072NIEHS NIH HHS P42 ES004699NIEHS NIH HHS R01 ES002710NIEHS NIH HHS T32 ES007059
6 · The paper itself

Abstract

Inspired by previously discovered enhanced analgesic efficacy between soluble epoxide hydrolase (sEH) and phosphodiesterase 4 (PDE4) inhibitors, we designed, synthesized and characterized 21 novel sEH/PDE4 dual inhibitors. The best of these displayed good efficacy in in vitro assays. Further pharmacokinetic studies of a subset of four selected compounds led to the identification of a bioavailable dual inhibitor N-(4-methoxy-2-(trifluoromethyl)benzyl)-1-propionylpiperidine-4-carboxamide (MPPA). In a lipopolysaccharide induced inflammatory pain rat model, MPPA rapidly increased in the blood ( T

Indexed as

Administration, OralAnalgesicsAnimalsEpoxide HydrolasesHEK293 CellsHumansInflammationLipopolysaccharidesMaleMolecular StructurePainPhosphodiesterase 4 InhibitorsPiperidinesRats, Sprague-DawleyAnalgesicsEPHX2 protein, humanEphx2 protein, mouseEPHX2 protein, ratEpoxide HydrolasesLipopolysaccharidesPhosphodiesterase 4 InhibitorsPiperidines

Identifiers

PMID29614224
PMCPMC5933862
OpenAlexW2796173020

What OpenQuestion holds

Textmetadata
LicenceTDM
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.