Evidence map›Paper›PMID 23734673›Full record

ArticleJournal of medicinal chemistry2013

Chemistry, pharmacology, and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile. Part II.

Han-Kun Zhang, Li-Fang Yu, J Brek Eaton, Paul Whiteaker, Oluseye K Onajole, Taleen Hanania, Daniela Brunner, Ronald J Lukas, Alan P Kozikowski

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 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. Review
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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.

Han-Kun ZhangDepartment of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago , 833 South Wood Street, Chicago, Illinois 60612, United States.
Li-Fang Yu
J Brek Eaton
Paul Whiteaker
Oluseye K Onajole
Taleen Hanania
Daniela Brunner
Ronald J Lukas
Alan P Kozikowski

Funding

Design and Study of New Nicotinic Analogs for Use in DepressionU19MH085193 · NIMH · UNIVERSITY OF ILLINOIS AT CHICAGO · PI KOZIKOWSKI, ALAN P. · 2009 to 2013
$4.5M
NIMH NIH HHS U19 MH085193NIMH NIH HHS U19MH085193
6 · The paper itself

Abstract

A 3-pyridyl ether scaffold bearing a cyclopropane-containing side chain was recently identified in our efforts to create novel antidepressants that act as partial agonists at α4β2-nicotinic acetylcholine receptors. In this study, a systematic structure-activity relationship investigation was carried out on both the azetidine moiety present in compound 3 and its right-hand side chain, thereby discovering a variety of novel nicotinic ligands that retain bioactivity and feature improved chemical stability. The most promising compounds, 24, 26, and 30, demonstrated comparable or enhanced pharmacological profiles compared to the parent compound 4, and the N-methylpyrrolidine analogue 26 also exhibited robust antidepressant-like efficacy in the mouse forced swim test. The favorable ADMET profile and chemical stability of 26 further indicate this compound to be a promising lead as a drug candidate warranting further advancement down the drug discovery pipeline.

Indexed as

AnimalsAntidepressive AgentsBinding, CompetitiveCaco-2 CellsCell LineCell Line, TumorCyclopropanesCytochrome P-450 Enzyme InhibitorsCytochrome P-450 Enzyme SystemDrug StabilityHumansMaleMiceMice, Inbred BALB CMicrosomes, LiverModels, ChemicalAntidepressive AgentsCyclopropanesCytochrome P-450 Enzyme InhibitorsCytochrome P-450 Enzyme SystemNicotinic Agonistsnicotinic receptor alpha4beta2Receptors, Nicotinic

Identifiers

PMID23734673
PMCPMC3843973

What OpenQuestion holds

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Registered trials

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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.