Evidence map›Paper›PMID 26016546›Full record

ArticleMolecules (Basel, Switzerland)2015

Practical Radiosynthesis and Preclinical Neuroimaging of [11C]isradipine, a Calcium Channel Antagonist.

Benjamin H Rotstein, Steven H Liang, Vasily V Belov, Eli Livni, Dylan B Levine, Ali A Bonab, Mikhail I Papisov, Roy H Perlis, Neil Vasdev

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecules (Basel, Switzerland), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. The Hantzsch reaction for nitrogen-13 PET: preparation of [Chemical communications (Cambridge, England) · 2021
    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

9 authors.

Benjamin H RotsteinDepartment of Radiology, Harvard Medical School, Division of Nuclear Medicine and Molecular Imaging and Center for Advanced Medical Imaging Sciences, Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA. rotstein.benjamin@mgh.harvard.edu.
Steven H LiangDepartment of Radiology, Harvard Medical School, Division of Nuclear Medicine and Molecular Imaging and Center for Advanced Medical Imaging Sciences, Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA. liang.steven@mgh.harvard.edu.
Vasily V BelovDepartment of Radiology, Harvard Medical School, Division of Nuclear Medicine and Molecular Imaging and Center for Advanced Medical Imaging Sciences, Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA. vbelov@mgh.harvard.edu.
Eli LivniDepartment of Radiology, Harvard Medical School, Division of Nuclear Medicine and Molecular Imaging and Center for Advanced Medical Imaging Sciences, Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA. elivni@mgh.harvard.edu.
Dylan B LevineDepartment of Radiology, Harvard Medical School, Division of Nuclear Medicine and Molecular Imaging and Center for Advanced Medical Imaging Sciences, Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA. dblevine@mgh.harvard.edu.
Ali A BonabDepartment of Radiology, Harvard Medical School, Division of Nuclear Medicine and Molecular Imaging and Center for Advanced Medical Imaging Sciences, Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA. bonab@pet.mgh.harvard.edu.
Mikhail I PapisovDepartment of Radiology, Harvard Medical School, Division of Nuclear Medicine and Molecular Imaging and Center for Advanced Medical Imaging Sciences, Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA. papisov@helix.mgh.harvard.edu.
Roy H PerlisDepartment of Psychiatry and Center for Experimental Drugs and Diagnostics, Massachusetts General Hospital, 185 Cambridge Street, Boston, MA 02114, USA. rperlis@mgh.harvard.edu.
Neil VasdevDepartment of Radiology, Harvard Medical School, Division of Nuclear Medicine and Molecular Imaging and Center for Advanced Medical Imaging Sciences, Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA. vasdev.neil@mgh.harvard.edu.

Funding

New PET tracers for neuroimaging of FAAH in endocannabinoid signalingK01DA038000 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2014 to 2018
$927k
NIDA NIH HHS K01 DA038000
6 · The paper itself

Abstract

In the interest of developing in vivo positron emission tomography (PET) probes for neuroimaging of calcium channels, we have prepared a carbon-11 isotopologue of a dihydropyridine Ca2+-channel antagonist, isradipine. Desmethyl isradipine (4-(benzo[c][1,2,5]oxadiazol-4-yl)-5-(isopropoxycarbonyl)-2,6-dimethyl-1,4-dihydropyridine -3-carboxylic acid) was reacted with [11C]CH3I in the presence of tetrabutylammonium hydroxide in DMF in an HPLC injector loop to produce the radiotracer in a good yield (6 ± 3% uncorrected radiochemical yield) and high specific activity (143 ± 90 GBq·µmol-1 at end-of-synthesis). PET imaging of normal rats revealed rapid brain uptake at baseline (0.37 ± 0.08% ID/cc (percent of injected dose per cubic centimeter) at peak, 15-60 s), which was followed by fast washout. After pretreatment with isradipine (2 mg·kg-1, i.p.), whole brain radioactivity uptake was diminished by 25%-40%. This preliminary study confirms that [11C]isradipine can be synthesized routinely for research studies and is brain penetrating. Further work on Ca2+-channel radiotracer development is planned.

Indexed as

AnimalsBrainCalcium Channel BlockersCalcium ChannelsCarbon RadioisotopesDimethylformamideDrug Evaluation, PreclinicalHalf-LifeHydrocarbons, IodinatedIsotope LabelingIsradipineMaleNeuroimagingPermeabilityPositron-Emission TomographyQuaternary Ammonium CompoundsCalcium Channel BlockersCalcium ChannelsCarbon RadioisotopesDimethylformamideHydrocarbons, IodinatedIsradipinemethyl iodideQuaternary Ammonium CompoundsRadiopharmaceuticalstetrabutylammoniumcalcium channel blockercarbon-11isradipineneuroimagingpositron emission tomographyradiosynthesis

Identifiers

PMID26016546
PMCPMC4870226

What OpenQuestion holds

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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.