Evidence map›Paper›PMID 16005216›Full record

ArticleBioorganic & medicinal chemistry letters2005

The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion.

Roger L Papke, Guangrong Zheng, Nicole A Horenstein, Linda P Dwoskin, Peter A Crooks

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
0.6field-weighted citation impact, top 34% 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

8 citing papers in PubMed, 14 citations in OpenAlex.

  1. Review
  2. Therapeutic Targeting ofPharmacological reviews · 2021
    Review
  3. Article
  4. Expeditious synthesis ofTetrahedron letters · 2011
    Article
  5. High throughput electrophysiology with Xenopus oocytes.Combinatorial chemistry & high throughput screening · 2009
    Review
  6. Article
  7. Article
  8. 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

5 authors at 2 institutions in 1 country.

Roger L PapkeUniversity of Florida, College of Medicine, 1600 SW Archer Road, Gainesville, FL 32610, USA. rlpapke@ufl.edu
Guangrong Zheng
Nicole A Horenstein
Linda P Dwoskin
Peter A Crooks
University of Kentucky · USUniversity of Florida · US

Funding

THE ROLE OF ENDOGENOUS OPIOIDS IN SUDDEN INFANT DEATHP50DA005274 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI DELORENZO, ROBERT JOHN · 1988 to 2011
$12.6M
Targeting of Alpha7 nAChR for therapeutic effectsR01GM057481 · NIGMS · UNIVERSITY OF FLORIDA · PI PAPKE, ROGER L · 2000 to 2023
$7.6M
Developmemt of Novel Treatments for Nicotine AddictionU19DA017548 · NIDA · UNIVERSITY OF KENTUCKY · PI DWOSKIN, LINDA P · 2003 to 2007
$6.0M
NIDA NIH HHS DA-017548NIDA NIH HHS DA-05274NIDA NIH HHS P50 DA005274NIDA NIH HHS U19 DA017548NIGMS NIH HHS GM57481-01A2NIGMS NIH HHS R01 GM057481
6 · The paper itself

Abstract

The alpha7 nAChR subtype is of particular interest as a potential therapeutic target since it has been implicated as a mediator of both cognitive and neuroprotective activity. The rigid nicotine analog ACME and the N-cyanoborane conjugate ACME-B are selective partial agonists of rat alpha7 receptors expressed in Xenopus oocytes, with no significant activation of either alpha3beta4 or alpha4beta2 receptors. ACME-B is both more potent and efficacious than ACME. The efficacies of ACME-B and ACME are approximately 26% and 10% of the efficacy of ACh, respectively. Similar N-conjugation of S(-)nicotine with cyanoborane decreased efficacy for alpha3beta4 and alpha4beta2 receptors, as well as for alpha7 nAChR. Structural comparison of ACME with the benzylidene anabaseines, another class of previously identified alpha7-selective agonists, suggests that they share a similar structural motif that may be applicable to other alpha7-selective agonists.

Indexed as

alpha7 Nicotinic Acetylcholine ReceptorAnimalsBoronBrainElectrophysiologyHumansNicotineNicotinic AgonistsOocytesProtein BindingRadioligand AssayRatsReceptors, NicotinicStructure-Activity RelationshipTransfectionXenopusalpha7 Nicotinic Acetylcholine ReceptorBoronChrna7 protein, humanChrna7 protein, ratNicotineNicotinic Agonistsnicotinic receptor alpha3beta4nicotinic receptor alpha4beta2Receptors, Nicotinic

Identifiers

PMID16005216
PMCPMC3593044
OpenAlexW2059638712

What OpenQuestion holds

Textmetadata
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.