Evidence map›Paper›PMID 29178785›Full record

ArticleJournal of medicinal chemistry2017

Highly Selective and Potent α4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats.

Jinhua Wu, Andrea Cippitelli, Yaohong Zhang, Ginamarie Debevec, Jennifer Schoch, Akihiko Ozawa, Yongping Yu, Huan Liu, Wenteng Chen, Richard A Houghten and 3 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.4field-weighted citation impact, top 36% 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

6 citing papers in PubMed, 11 citations in OpenAlex.

  1. Article
  2. Isolation and characterization of five novel disulfide-poor conopeptides fromThe journal of venomous animals and toxins including tropical diseases · 2022
    Article
  3. Article
  4. Review
  5. Article
  6. 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

13 authors at 3 institutions in 2 countries.

Jinhua WuTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.ORCID 0000-0003-3733-5616
Andrea CippitelliTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
Yaohong ZhangTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
Ginamarie DebevecTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
Jennifer SchochTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
Akihiko OzawaTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
Yongping YuTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
Huan LiuInstitute of Materia Medica, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou 310058, P. R. China.
Wenteng ChenInstitute of Materia Medica, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou 310058, P. R. China.
Richard A HoughtenTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
Gregory S WelmakerTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
Marc A GiulianottiTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
Lawrence TollTorrey Pines Institute for Molecular Studies , 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
Torrey Pines Institute For Molecular Studies · USZhejiang University · CNShaoxing University · CN

Funding

Novel selective alpha4beta2 nicotinic receptor antagonists for smoking cessationR44DA036968 · NIDA · ASSUAGE PHARMACEUTICALS, INC. · PI WU, JINHUA · 2015 to 2016
$997k
Novel selective alpha4beta2 nicotinic receptor antagonists for smoking cessationR43DA036968 · NIDA · ASSUAGE PHARMACEUTICALS, INC. · PI WU, JINHUA · 2014 to 2014
$150k
NIDA NIH HHS R43 DA036968NIDA NIH HHS R44 DA036968
6 · The paper itself

Abstract

The α4β2 nAChR is the most predominant subtype in the brain and is a well-known culprit for nicotine addiction. Previously we presented a series of α4β2 nAChR selective compounds that were discovered from a mixture-based positional-scanning combinatorial library. Here we report further optimization identified highly potent and selective α4β2 nAChR antagonists 5 (AP-202) and 13 (AP-211). Both compounds are devoid of in vitro agonist activity and are potent inhibitors of epibatidine-induced changes in membrane potential in cells containing α4β2 nAChR, with IC

Indexed as

Receptors, NicotinicAnimalsBlood-Brain BarrierDrug Evaluation, PreclinicalDrug-Seeking BehaviorMaleNicotineNicotinic AntagonistsRats, Sprague-DawleyReinforcement, PsychologySelf AdministrationStructure-Activity RelationshipNicotineNicotinic Antagonistsnicotinic receptor alpha4beta2Receptors, Nicotinic

Identifiers

PMID29178785
PMCPMC6697865
OpenAlexW2770272581

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.