Evidence map›Paper›PMID 24900840›Full record

ArticleACS medicinal chemistry letters2014

Enhancing a CH-π Interaction to Increase the Affinity for 5-HT1A Receptors.

Jean-François Liégeois, Marc Lespagnard, Elsa Meneses Salas, Floriane Mangin, Jacqueline Scuvée-Moreau, Sébastien Dilly

Abstract read
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In one paragraph

Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Article
  2. Article
  3. 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

6 authors.

Jean-François LiégeoisLaboratory of Medicinal Chemistry and C.I.R.M., University of Liège , avenue de l'Hôpital, 1 (B36), B-4000 Liège 1, Belgium.
Marc LespagnardLaboratory of Medicinal Chemistry and C.I.R.M., University of Liège , avenue de l'Hôpital, 1 (B36), B-4000 Liège 1, Belgium.
Elsa Meneses SalasLaboratory of Medicinal Chemistry and C.I.R.M., University of Liège , avenue de l'Hôpital, 1 (B36), B-4000 Liège 1, Belgium.
Floriane ManginLaboratory of Medicinal Chemistry and C.I.R.M., University of Liège , avenue de l'Hôpital, 1 (B36), B-4000 Liège 1, Belgium.
Jacqueline Scuvée-MoreauLaboratory of Pharmacology and GIGA-Neuroscience, University of Liège , avenue de l'Hôpital, 1 (B36), B-4000 Liège 1, Belgium.
Sébastien DillyLaboratory of Medicinal Chemistry and C.I.R.M., University of Liège , avenue de l'Hôpital, 1 (B36), B-4000 Liège 1, Belgium ; Laboratory of Pharmacology and GIGA-Neuroscience, University of Liège , avenue de l'Hôpital, 1 (B36), B-4000 Liège 1, Belgium.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

An electrostatic interaction related to a favorable position of the distal phenyl ring and a phenylalanine residue in the binding pocket would explain the higher 5-HT1A affinity of a 4-phenyl-1,2,3,6-tetrahydropyridine (THP) analogue compared to the corresponding 4-phenylpiperazine analogue. To explore a possible reinforcement of this interaction to increase the affinity for 5-HT1A receptors, different 4-substituted-phenyl analogues were synthesized and tested. The most important increase of affinity is obtained with two electron-donating methyl groups in positions 3 and 5.

Indexed as

arylpiperazinecarboxamideCH−π interactiondockingelectron-donatingquinoxaline

Identifiers

PMID24900840
PMCPMC4027751

What OpenQuestion holds

Textmetadata
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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.