Evidence map›Paper›PMID 28644418›Full record

ArticleInternational journal of molecular sciences2017

New MT₂ Melatonin Receptor-Selective Ligands: Agonists and Partial Agonists.

Jean A Boutin, Anne Bonnaud, Chantal Brasseur, Olivier Bruno, Nolwenn Lepretre, Peter Oosting, Sophie Coumailleau, Philippe Delagrange, Olivier Nosjean, Céline Legros

Open access · goldAbstract read
In one paragraph

Article in International journal of molecular sciences, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
1.1field-weighted citation impact, top 27% 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

1 citing paper in PubMed, 15 citations in OpenAlex.

  1. 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

10 authors at 1 institution in 1 country.

Jean A BoutinPôle d'Expertise Biotechnologie, Chimie, Biologie, Institut de Recherches SERVIER, 78290 Croissy-sur-Seine, France. jean.boutin@servier.com.
Anne BonnaudPôle d'Expertise Biotechnologie, Chimie, Biologie, Institut de Recherches SERVIER, 78290 Croissy-sur-Seine, France. anne.bonnaud@servier.com.
Chantal BrasseurPôle d'Expertise Biotechnologie, Chimie, Biologie, Institut de Recherches SERVIER, 78290 Croissy-sur-Seine, France. chantal.brasseur@servier.com.
Olivier BrunoPôle d'Expertise Biotechnologie, Chimie, Biologie, Institut de Recherches SERVIER, 78290 Croissy-sur-Seine, France. olivier.bruno@servier.com.
Nolwenn LepretreDIVERCHIM S.A., 95700 Roissy-en-France, France. nolwenn.lepretre@diverchim.com.
Peter OostingDIVERCHIM S.A., 95700 Roissy-en-France, France. peter.oosting@diverchim.com.
Sophie CoumailleauPôle d'Expertise Biotechnologie, Chimie, Biologie, Institut de Recherches SERVIER, 78290 Croissy-sur-Seine, France. sophie.coumailleau@servier.com.
Philippe DelagrangePôle d'Innovations Thérapeutiques en Neurosciences, Institut de Recherches, SERVIER, 78290 Croissy-sur-Seine, France. philippe.delagrange@servier.com.
Olivier NosjeanPôle d'Expertise Biotechnologie, Chimie, Biologie, Institut de Recherches SERVIER, 78290 Croissy-sur-Seine, France. olivier.nosjean@servier.com.
Céline LegrosPôle d'Expertise Biotechnologie, Chimie, Biologie, Institut de Recherches SERVIER, 78290 Croissy-sur-Seine, France. celine.legros@servier.com.
Plateforme Technologique d'Innovation Biomédicale · FR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The search for melatonin receptor agonists and antagonists specific towards one of the receptor subtypes will extend our understanding of the role of this system in relaying circadian information to the body. A series of compounds derived from a hit compound discovered in a screening process led to powerful agonists specific for one of the isoform of the melatonin receptor namely, MT₂. The compounds are based on a poorly explored skeleton in the molecular pharmacology of melatonin. By changing the steric hindrance of one substituent (i.e., from a hydrogen atom to a tributylstannyl group), we identified a possible partial agonist that could lead to antagonist analogues. The functionalities of these compounds were measured with a series of assays, including the binding of GTPγS, the inhibition of the cyclic AMP production, the β-arrestin recruitment, and the cell shape changes as determined by cellular dielectric spectroscopy (CellKey

Indexed as

Animalsbeta-ArrestinsCHO CellsCricetulusCyclic AMPDrug DiscoveryGuanosine 5'-O-(3-Thiotriphosphate)HumansLigandsReceptor, Melatonin, MT2Small Molecule Librariesbeta-ArrestinsCyclic AMPGuanosine 5'-O-(3-Thiotriphosphate)LigandsReceptor, Melatonin, MT2Small Molecule Librariesagonistfunctional assaysmelatonin receptorsmolecular pharmacologypartial agonist

Identifiers

PMID28644418
PMCPMC5535840
OpenAlexW2633964621

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.