ArticleNuclear medicine and biology2011
Effect of cyclosporin A on the uptake of D3-selective PET radiotracers in rat brain.
Article in Nuclear medicine and biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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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.
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Who cites it
8 citing papers in PubMed, 14 citations in OpenAlex.
- Nanoparticles in Medicine: Current Status in Cancer Treatment.International journal of molecular sciences · 2023Review
- Evaluation of [Pharmaceuticals (Basel, Switzerland) · 2023Article
- Absorbed radiation dosimetry of the DAmerican journal of nuclear medicine and molecular imaging · 2016Article
- A potent and selective C-11 labeled PET tracer for imaging sphingosine-1-phosphate receptor 2 in the CNS demonstrates sexually dimorphic expression.Organic & biomolecular chemistry · 2015Article
- Characterization of [(3) H]LS-3-134, a novel arylamide phenylpiperazine D3 dopamine receptor selective radioligand.Journal of neurochemistry · 2014Article
- Synthesis andMedChemComm · 2013Article
- Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter.Journal of medicinal chemistry · 2013Article
- Synthesis and characterization of selective dopamine D₂ receptor ligands using aripiprazole as the lead compound.Bioorganic & medicinal chemistry · 2011Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
introductionFour benzamide analogs having a high affinity and selectivity for D(3) versus D(2) receptors were radiolabeled with (11)C or (18)F for in vivo evaluation.
methodsPrecursors were synthesized, and the four D(3) selective benzamide analogs were radiolabeled. The tissue distribution and brain uptake of the four compounds were evaluated in control rats and rats pretreated with cyclosporin A, a modulator of P-glycoprotein and an inhibitor of other ABC efflux transporters that contribute to the blood brain barrier. Micro-positron emission tomographic (PET) imaging was carried out for [(11)C]6 in a control and a cyclosporin A pretreated rat.
resultsAll four compounds showed low brain uptake in control rats at 5 and 30 min post-injection; despite recently reported rat behavioral studies conducted on analogs 6 (WC-10) and 7 (WC-44). Following administration of cyclosporin A, increased brain uptake was observed with all four PET radiotracers at both 5 and 30 min post-intravenous injection. An increase in brain uptake following modulation/inhibition of the ABC transporters was also observed in the microPET study.
conclusionsThese data suggest that D3 selective conformationally-flexible benzamide analogs which contain a N-2-methoxyphenylpiperazine moiety are substrates for P-glycoprotein or other adenosine triphosphate (ATP)-binding cassette transporters expressed at the blood-brain barrier, and that PET radiotracers containing this pharmacophore may display low brain uptake in rodents due to the action of these efflux transporters.
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