Evidence map›Paper›PMID 25182564›Full record

ArticleBioorganic & medicinal chemistry letters2014

Synthesis and evaluation of arylpiperazines derivatives of 3,5-dioxo-(2H,4H)-1,2,4-triazine as 5-HT1AR ligands.

J S Dileep Kumar, Vattoly J Majo, Jaya Prabhakaran, J John Mann

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
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

2 citing papers in PubMed.

  1. Article
  2. 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

4 authors.

J S Dileep KumarDivision of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, USA; Department of Psychiatry and Behavior Science, Stony Brook University, New York, USA. Electronic address: kumardi@nyspi.columbia.edu.
Vattoly J MajoDivision of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, USA.
Jaya PrabhakaranColumbia University College of Physicians and Surgeons, New York, USA.
J John MannDivision of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, USA; Columbia University College of Physicians and Surgeons, New York, USA.

Funding

THE NEUROBIOLOGY OF SUICIDAL BEHAVIORP50MH062185 · NIMH · NEW YORK STATE PSYCHIATRIC INSTITUTE DBA RESEARCH FOUNDATION FOR MENTAL HYGIENE, INC · PI MANN, JOSEPH JOHN · 2000 to 2009
$21.7M
Development of Agonist PET Probes for Quantifying 5-HT1A Receptor BindingR21MH077161 · NIMH · COLUMBIA UNIVERSITY HEALTH SCIENCES · PI VATTOLY JOSEPH, MAJO · 2006 to 2007
$392k
NIMH NIH HHS MH062185NIMH NIH HHS MH077161NIMH NIH HHS P50 MH062185NIMH NIH HHS R21 MH077161
6 · The paper itself

Abstract

5-HT1AR agonist or partial agonists are established drug candidates for psychiatric and neurological disorders. We have reported the synthesis and evaluation of a series of high affinity 5-HT1AR partial agonist PET imaging agents with greater selectivity over α-1AR. The characteristic of these molecules are 3,5-dioxo-(2H,4H)-1,2,4-triazine skeleton tethered to an arylpiperazine unit through an alkyl side chain. The most potent 5-HT1AR agonistic properties were found to be associated with the molecules bearing C-4 alkyl group as the linker. Therefore development of 3,5-dioxo-(2H,4H)-1,2,4-triazine bearing arylpiperazine derivatives may provide high affinity selective 5-HT1AR ligands. Herein we describe the synthesis and evaluation of the binding properties of a series of arylpiperazine analogues of 3,5-dioxo-(2H,4H)-1,2,4-triazine.

Indexed as

Dose-Response Relationship, DrugHumansLigandsMolecular StructurePiperazinesReceptor, Serotonin, 5-HT1ASerotonin 5-HT1 Receptor AgonistsStructure-Activity RelationshipTriazinesLigandsPiperazinesReceptor, Serotonin, 5-HT1ASerotonin 5-HT1 Receptor AgonistsTriazines5-HT5-HT(1A)RAgonistArylpiperazineα-1AR

Identifiers

PMID25182564
PMCPMC4294696

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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.