Evidence map›Paper›PMID 34387471›Full record

ArticleJournal of medicinal chemistry2021

Evaluation of Amide Bioisosteres Leading to 1,2,3-Triazole Containing Compounds as GPR88 Agonists: Design, Synthesis, and Structure-Activity Relationship Studies.

Md Toufiqur Rahman, Ann M Decker, Lucas Laudermilk, Rangan Maitra, Weiya Ma, Sami Ben Hamida, Emmanuel Darcq, Brigitte L Kieffer, Chunyang Jin

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
2.5field-weighted citation impact, top 10% 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

12 citing papers in PubMed, 30 citations in OpenAlex.

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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

9 authors at 3 institutions in 3 countries.

Md Toufiqur RahmanCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.ORCID 0000-0003-2752-6822
Ann M DeckerCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Lucas LaudermilkCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.
Rangan MaitraCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.ORCID 0000-0001-6663-6800
Weiya MaDouglas Research Center, Department of Psychiatry, McGill University, Montréal, Quebec H4H 1R3, Canada.
Sami Ben HamidaDouglas Research Center, Department of Psychiatry, McGill University, Montréal, Quebec H4H 1R3, Canada.
Emmanuel DarcqDouglas Research Center, Department of Psychiatry, McGill University, Montréal, Quebec H4H 1R3, Canada.
Brigitte L KiefferDouglas Research Center, Department of Psychiatry, McGill University, Montréal, Quebec H4H 1R3, Canada.
Chunyang JinCenter for Drug Discovery, Research Triangle Institute, Research Triangle Park, North Carolina 27709, United States.ORCID 0000-0001-6733-3094
RTI International · USInserm · FRMcGill University · CA

Funding

Nr4a1 and GPR88 as novel gene targets for alcoholism: mouse genetic approachesU01AA016658 · NIAAA · UNIVERSITE DE STRASBOURG · PI LAURA ADELA HARSAN · 2006 to 2026
$3.8M
GPR88 Agonist for Alcoholism TreatmentR01AA026820 · NIAAA · RESEARCH TRIANGLE INSTITUTE · PI JIN, CHUNYANG, KIEFFER, BRIGITTE L. · 2018 to 2022
$2.4M
Preparation and characterization of radioligands for the orphan receptor GPR88R03AA029013 · NIAAA · RESEARCH TRIANGLE INSTITUTE · PI HESK, DAVID, JIN, CHUNYANG · 2020 to 2020
$220k
NIAAA NIH HHS R01 AA026820NIAAA NIH HHS R03 AA029013NIAAA NIH HHS U01 AA016658
6 · The paper itself

Abstract

The orphan receptor GPR88 has been implicated in a number of striatal-associated disorders, yet its endogenous ligand has not been discovered. We have previously reported that the amine functionality in the 2-AMPP-derived GPR88 agonists can be replaced with an amide (e.g.,

Indexed as

AnimalsBenzeneacetamidesBlood-Brain BarrierCorpus StriatumDrug DesignMaleMiceMice, Inbred C57BLMice, KnockoutMolecular StructureOxadiazolesReceptors, G-Protein-CoupledStructure-Activity RelationshipTriazolesBenzeneacetamidesGpr88 protein, mouseOxadiazolesReceptors, G-Protein-CoupledTriazoles

Identifiers

PMID34387471
PMCPMC8395584
OpenAlexW3192786658

What OpenQuestion holds

Textmetadata
LicenceTDM
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.