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Record W4223462931 · doi:10.1139/cjpp-2021-0729

Structure–activity relationship of three new piperazine derivates with anxiolytic-like and antidepressant-like effects

2022· article· en· W4223462931 on OpenAlexvenueno aff
Ianca Gontijo Cavalcante Santana, Lorena de Souza Almeida, Lorrane Kelle da Silva Moreira, Flávio Silva de Carvalho, Ricardo Menegatti, André Luís Batista da Rocha, Thais Aline Mazurok, Boniek G. Vaz, Luciano M. Lião, Adriane Ferreira de Brito, James Oluwagbamigbe Fajemiroye, Élson Alves Costa, Pablinny Moreira Galdino

Bibliographic record

VenueCanadian Journal of Physiology and Pharmacology · 2022
Typearticle
Languageen
FieldNeuroscience
TopicNeurotransmitter Receptor Influence on Behavior
Canadian institutionsnot available
FundersConselho Nacional de Desenvolvimento Científico e Tecnológico
KeywordsAntidepressantAnxiolyticTolerabilityMedicinePharmacologyAntagonistSerotonergicFlumazenilAnxietyBenzodiazepineOpen fieldAnesthesiaInternal medicineAdverse effectPsychiatrySerotoninReceptor

Abstract

fetched live from OpenAlex

Anxiety and depression are common mental disorders affecting millions of people worldwide. Unsatisfactory clinical outcomes with the use of the available pharmacological interventions among some patients demand newer drugs with proven efficacy, safety, and tolerability profile. In this study, the LQFM211, LQFM213, and LQFM214 were designed from the piperazine scaffold and administered orally in mice. These mice were later evaluated in the open field, elevated plus maze, and forced swimming tests to assess the exploratory, anxiolytic, and antidepressant-like activities, respectively. The mechanism of action of these new derivatives was evaluated using flumazenil (benzodiazepine antagonist) and WAY100635 (5-HT1A receptor antagonist). Unlike LQFM214, the LQFM211 and LQFM213 elicited anxiolytic and antidepressant-like effects. The blockade of the effect of LQFM213 by WAY100635 suggests the involvement of the serotonergic pathway.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame machine prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: metacan-v3-hybrid-931329e0061cValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.002
Threshold uncertainty score0.006

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0020.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.024
GPT teacher head0.270
Teacher spread0.245 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations4
Published2022
Admission routes1
Has abstractyes

Explore more

Same venueCanadian Journal of Physiology and Pharmacology→Same topicNeurotransmitter Receptor Influence on Behavior→French-language works237,207→