Evidence map›Paper›PMID 23574807›Full record

ArticleChemical biology & drug design2013

Synthesis, antidepressant evaluation and docking studies of long-chain alkylnitroquipazines as serotonin transporter inhibitors.

Mari Gabrielsen, Karol Wołosewicz, Anna Zawadzka, Jerzy Kossakowski, Gabriel Nowak, Małgorzata Wolak, Katarzyna Stachowicz, Agata Siwek, Aina W Ravna, Irina Kufareva and 8 more

Abstract read
In one paragraph

Article in Chemical biology & drug design, 2013. 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
–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

5 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Oncotoxic Properties of Serotonin Transporter Inhibitors and 5-HTInternational journal of molecular sciences · 2018
    Article
  5. 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

18 authors.

Mari GabrielsenMedical Pharmacology and Toxicology, Department of Medical Biology, Faculty of Health Sciences, University of Tromsø, 9037 Tromsø, Norway.
Karol Wołosewicz
Anna Zawadzka
Jerzy Kossakowski
Gabriel Nowak
Małgorzata Wolak
Katarzyna Stachowicz
Agata Siwek
Aina W Ravna
Irina Kufareva
Lech Kozerski
Elżbieta Bednarek
Jerzy Sitkowski
Wojciech Bocian
Ruben Abagyan
Andrzej J Bojarski
Ingebrigt Sylte
Zdzisław Chilmonczyk

Funding

Project 3U54GM094618 · NIGMS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI STEVENS, RAYMOND C · 2010 to 2014
$17.1M
Structure, Dynamics and Activation Mechanisms of Chemokine ReceptorsU01GM094612 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI HANDEL, TRACY M · 2010 to 2014
$4.5M
Macromolecular DockingR01GM071872 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI ABAGYAN, RUBEN · 2004 to 2017
$4.2M
A Chemical Biology Network for Personalized MedicineRC2LM010994 · NLM · NEW YORK UNIVERSITY SCHOOL OF MEDICINE · PI CARDOZO, TIMOTHY J, MA'AYAN, AVI · 2010 to 2010
$2.1M
NIGMS NIH HHS R01 GM071872NIGMS NIH HHS U01 GM094612NIGMS NIH HHS U54 GM094618NLM NIH HHS RC2 LM 010994NLM NIH HHS RC2 LM010994
6 · The paper itself

Abstract

Twelve alkyl analogues (1-12) of the high-affinity serotonin transporter (SERT) inhibitor 6-nitroquipazine (6-NQ) were synthesized and studied using in vitro radioligand competition binding assays to determine their binding affinity (Ki ). The putative antidepressant activity of five of the binders with the highest SERT binding affinities was studied by the forced swim and locomotor activity mouse tests. The three-dimensional (3D) structures of 8 and 9 were determined using NOE NMR technique. Flexible docking of the compounds was undertaken to illustrate the binding of the compounds in the SERT model. Our results showed that several of the 6-NQ analogues are high-affinity SERT inhibitors and indicated that the octyl (8), decyl (10) and dodecyl (12) 6-NQ analogues exhibit moderate antidepressant activity.

Indexed as

AnimalsAntidepressive AgentsBinding SitesMaleMiceMolecular Docking SimulationMotor ActivityProtein BindingProtein Structure, TertiaryQuipazineReceptor, Serotonin, 5-HT1ASelective Serotonin Reuptake InhibitorsSerotonin Plasma Membrane Transport Proteins6-nitroquipazineAntidepressive AgentsQuipazineReceptor, Serotonin, 5-HT1ASelective Serotonin Reuptake InhibitorsSerotonin Plasma Membrane Transport Proteins

Identifiers

PMID23574807
PMCPMC3665732

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.