Evidence map›Paper›PMID 28820054›Full record

ReviewCurrent neuropharmacology2018

QSAR Modeling of Histamine H3R Antagonists/inverse Agonists as Future Drugs for Neurodegenerative Diseases.

Michelle Fidelis Correa, Joao Paulo Dos Santos Fernandes

Open access · greenAbstract readReview
In one paragraph

Review in Current neuropharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.5field-weighted citation impact, top 39% 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

4 citing papers in PubMed, 9 citations in OpenAlex.

  1. Review
  2. Review
  3. Review
  4. Article
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

2 authors at 1 institution in 1 country.

Michelle Fidelis CorreaDepartamento de Ciencias Farmaceuticas, Universidade Federal de Sao Paulo, Rua Sao Nicolau 210, Centro 09913- 030, Diadema-SP, Brazil.
Joao Paulo Dos Santos FernandesDepartamento de Ciencias Farmaceuticas, Universidade Federal de Sao Paulo, Rua Sao Nicolau 210, Centro 09913- 030, Diadema-SP, Brazil.
Universidade Federal de São Paulo · BR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundHistamine H3 receptor (H3R) is associated with several neuropsychological diseases, and thus it is an important target involved in several CNS disorders, such as narcolepsy, attention deficit hyperactivity disorder and schizophrenia. Since QSAR modeling is a feasible approach to explain the role of the molecular substituents in the biological activity, it can help in improving the design of better H3R ligands for these conditions.

methodsThis article reviews papers previously published in literature to show the current status of the contribution from QSAR modeling to reach H3R antagonists/inverse agonists.

resultsClassical and 3D-QSAR models were retrieved, showing that the steric and hydrophobic properties of the H3R ligands are most important to reach good affinity.

conclusionAlthough QSAR methods are valuable to design better H3R antagonists/inverse agonists, pharmacokinetics should also be considered in future models to ensure good CNS penetration.

Indexed as

Quantitative Structure-Activity RelationshipAnimalsHistamine AgonistsHistamine H3 AntagonistsHumansModels, MolecularNeurodegenerative DiseasesHistamine AgonistsHistamine H3 AntagonistsH3R antagonistsH3 receptorH3R inverse agonistsneurodegenerative diseasesneuropsychiatric disordersQSARstructure-activity relationship.

Identifiers

PMID28820054
PMCPMC6080103
OpenAlexW2777592446

What OpenQuestion holds

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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.