Evidence map›Paper›PMID 20359531›Full record

ArticleEuropean journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences2010

Pharmacokinetic screening of soluble epoxide hydrolase inhibitors in dogs.

Hsing-Ju Tsai, Sung Hee Hwang, Christophe Morisseau, Jun Yang, Paul D Jones, Takeo Kasagami, In-Hae Kim, Bruce D Hammock

Abstract read
In one paragraph

Article in European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 58 papers.

0numbers the graph read from it
0cells of the map it votes in
58citing papers in PubMed
6.8field-weighted citation impact, top 3% 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

58 citing papers in PubMed, 81 citations in OpenAlex.

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  12. Soluble Epoxide Hydrolase Inhibition byInternational journal of molecular sciences · 2020
    Article
  13. Soluble epoxide hydrolase inhibitor, TPPU, increases regulatory T cells pathway in an arthritis model.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2020
    Article
  14. Article
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  16. Review
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  18. Drug-Target Residence Time AffectsACS central science · 2019
    Article
  19. Article
  20. Frontiers in pharmacology · 2019
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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

8 authors at 1 institution in 1 country.

Hsing-Ju TsaiDepartment of Entomology and Cancer Center, University of California, Davis, CA 95616, USA.
Sung Hee Hwang
Christophe Morisseau
Jun Yang
Paul D Jones
Takeo Kasagami
In-Hae Kim
Bruce D Hammock
University of California, Davis · US

Funding

Workshop on Environmental Technology Transfer and EntrepreneurshipP42ES004699 · NIEHS · UNIVERSITY OF CALIFORNIA DAVIS · PI HAMMOCK, BRUCE D · 1987 to 2021
$50.1M
HYDROLYTIC ENZYMES IN THE METABOLISM OF TOXINSR01ES002710 · NIEHS · UNIVERSITY OF CALIFORNIA DAVIS · PI HAMMOCK, BRUCE D · 1985 to 2018
$4.0M
OXYGENASE METABOLITES AND RENAL VASCULAR ACTIVITYR01HL059699 · NHLBI · TULANE UNIVERSITY OF LOUISIANA · PI IMIG, JOHN D · 1999 to 2011
$3.0M
Howard Hughes Medical InstituteNHLBI NIH HHS R01 HL059699NHLBI NIH HHS R01 HL59699-06A1NIEHS NIH HHS P42 ES004699NIEHS NIH HHS P42 ES04699NIEHS NIH HHS R01 ES002710NIEHS NIH HHS R01 ES02710
6 · The paper itself

Abstract

Epoxyeicosatrienoic acids that have anti-hypertensive and anti-inflammatory properties are mainly metabolized by soluble epoxide hydrolase (sEH, EC 3.3.2.3). Therefore, sEH has emerged as a therapeutic target for treating various cardiovascular diseases and inflammatory pain. N,N'-Disubstituted ureas are potent sEH inhibitors in vitro. However, in vivo usage of early sEH inhibitors has been limited by their low bioavailability and poor physiochemical properties. Therefore, a group of highly potent compounds with more drug-like physiochemical properties were evaluated by monitoring their plasma profiles in dogs treated orally with sEH inhibitors. Urea compounds with an adamantyl or a 4-trifluoromethoxyphenyl group on one side and a piperidyl or a cyclohexyl ether group on the other side of the urea function showed pharmacokinetic profiles with high plasma concentrations and long half lives. In particular, the inhibitor trans-4-[4-(3-adamantan-1-yl-ureido)-cyclohexyloxy]-benzoic acid (t-AUCB) not only is very potent with good physiochemical properties, but also shows high oral bioavailability for doses ranging from 0.01 to 1mg/kg. This compound is also very potent against the sEH of several mammals, suggesting that t-AUCB will be an excellent tool to evaluate the biology of sEH in multiple animal models. Such compounds may also be a valuable lead for the development of veterinary therapeutics.

Indexed as

AnimalsBenzoatesBiological AvailabilityChemistry, PharmaceuticalDogsDose-Response Relationship, DrugDrug Evaluation, PreclinicalEnzyme InhibitorsEpoxide HydrolasesFemaleInhibitory Concentration 50SolubilityStructure-Activity RelationshipUrea4-(4-(3-adamantan-1-ylureido)cyclohexyloxy)benzoic acidBenzoatesEnzyme InhibitorsEpoxide HydrolasesUrea

Identifiers

PMID20359531
PMCPMC3285443
OpenAlexW2142219464

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.