Evidence map›Paper›PMID 22608919›Full record

ArticleBioorganic & medicinal chemistry2012

5-(5-(6-[(11)C]methyl-3,6-diazabicyclo[3.2.0]heptan-3-yl)pyridin-2-yl)-1H-indole as a potential PET radioligand for imaging cerebral α7-nAChR in mice.

Yongjun Gao, Hayden T Ravert, Heather Valentine, Ursula Scheffel, Paige Finley, Dean F Wong, Robert F Dannals, Andrew G Horti

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2012. 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
0.8field-weighted citation impact, top 30% 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, 8 citations in OpenAlex.

  1. Trial
  2. Review
  3. Review
  4. Article
  5. 18F-ASEM, a radiolabeled antagonist for imaging the α7-nicotinic acetylcholine receptor with PET.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2014
    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

8 authors at 2 institutions in 1 country.

Yongjun GaoDivision of Nuclear Medicine, Department of Radiology, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287-0816, USA. ygao5@jhmi.edu
Hayden T Ravert
Heather Valentine
Ursula Scheffel
Paige Finley
Dean F Wong
Robert F Dannals
Andrew G Horti
Johns Hopkins Medicine · USJohns Hopkins University · US

Funding

Development of PET radioligands for cerebral cannabinoid receptor (CB1)R33MH079017 · NIMH · JOHNS HOPKINS UNIVERSITY · PI HORTI, ANDREW G · 2009 to 2011
$1.2M
Development of radioligands with improved brain kinetics for imaging nAChR by PETR21DA020777 · NIDA · JOHNS HOPKINS UNIVERSITY · PI HORTI, ANDREW G · 2008 to 2009
$492k
Development of PET radioligands for cerebral cannabinoid receptor (CB1)R21MH079017 · NIMH · JOHNS HOPKINS UNIVERSITY · PI HORTI, ANDREW G · 2007 to 2008
$435k
NIDA NIH HHS DA020777NIDA NIH HHS R21 DA020777NIMH NIH HHS MH079017NIMH NIH HHS R21 MH079017NIMH NIH HHS R33 MH079017
6 · The paper itself

Abstract

The radiosynthesis and in vivo evaluation of 5-(5-(6-[(11)C]methyl-3,6-diazabicyclo[3.2.0]heptan-3-yl)pyridin-2-yl)-1H-indole [(11)C]rac-(1), a potential PET tracer for α7 nicotinic acetylcholine receptors (α7-nAChR), are described. Syntheses of the nonradioactive standard rac-1 and corresponding desmethyl precursor 7 were achieved in several reaction steps. Radiomethylation of 7 with [(11)C]CH(3)I afforded [(11)C]rac-1 in an average radiochemical yield of 30 ± 5% (n=5) with high radiochemical purity and an average specific radioactivity of 444 ± 74 GBq/μmol (n=5). The total synthesis time was 30 min from end-of-bombardment. Biodistribution studies in mice showed that [(11)C]rac-1 penetrates the blood-brain barrier and specifically labels neuronal α7-nAChRs.

Indexed as

IndolesPositron-Emission TomographyPyridinesRadiopharmaceuticalsalpha7 Nicotinic Acetylcholine ReceptorAnimalsBrainBridged Bicyclo Compounds, HeterocyclicLigandsMiceMice, Inbred StrainsMolecular StructureQuinuclidinesReceptors, Nicotinic5-(5-(6-((11)C)methyl-3,6-diazabicyclo(3.2.0)heptan-3-yl)pyridin-2-yl)-1H-indolalpha7 Nicotinic Acetylcholine ReceptorBridged Bicyclo Compounds, HeterocyclicChrna7 protein, mouseIndolesLigandsN-(1-azabicyclo(2.2.2)oct-3-yl)furo(2,3-c)pyridine-5-carboxamidePyridinesQuinuclidinesRadiopharmaceuticalsReceptors, Nicotinic

Identifiers

PMID22608919
PMCPMC3527104
OpenAlexW1993074106

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.