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  • Syvänen, StinaUppsala universitet,Geriatrik,Rudbeck Laboratory (author)

[C-11]quinidine and [C-11]laniquidar PET imaging in a chronic rodent epilepsy model : Impact of epilepsy and drug-responsiveness

  • Article/chapterEnglish2013

Publisher, publication year, extent ...

  • Elsevier BV,2013
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:uu-207645
  • https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-207645URI
  • https://doi.org/10.1016/j.nucmedbio.2013.05.008DOI

Supplementary language notes

  • Language:English
  • Summary in:English

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  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • Introduction: To analyse the impact of both epilepsy and pharmacological modulation of P-glycoprotein on brain uptake and kinetics of positron emission tomography (PET) radiotracers [C-11]quinidine and [C-11]laniquidar.Methods: Metabolism and brain kinetics of both [C-11]quinidine and [C-11]laniquidar were assessed in naive rats, electrode-implanted control rats, and rats with spontaneous recurrent seizures. The latter group was further classified according to their response to the antiepileptic drug phenobarbital into "responders" and "non-responders". Additional experiments were performed following pre-treatment with the P-glycoprotein modulator tariquidar.Results: [C-11]quinidine was metabolized rapidly, whereas [C-11]laniquidar was more stable. Brain concentrations of both radiotracers remained at relatively low levels at baseline conditions. Tariquidar pre-treatment resulted in significant increases of [C-11]quinidine and [C-11]laniquidar brain concentrations. In the epileptic subgroup "non-responders", brain uptake of [C-11]quinidine in selected brain regions reached higher levels than in electrode-implanted control rats. However, the relative response to tariquidar did not differ between groups with full blockade of P-glycoprotein by 15 mg/kg of tariquidar. For [C-11]laniquidar differences between epileptic and control animals were only evident at baseline conditions but not after tariquidar pretreatment.Conclusions: We confirmed that both [C-11]quinidine and [C-11]laniquidar are P-glycoprotein substrates. At full P-gp blockade, tariquidar pre-treatment only demonstrated slight differences for [C-11]quinidine between drug-resistant and drug-sensitive animals.

Subject headings and genre

  • Positron emission tomography
  • [C-11]quinidine
  • [C-11]laniquidar
  • P-glycoprotein
  • Epilepsy

Added entries (persons, corporate bodies, meetings, titles ...)

  • Russmann, Vera (author)
  • Verbeek, Joost (author)
  • Eriksson, JonasDepartment of Nuclear Medicine & PET Research, VU University Medical Center, Amsterdam, The Netherlands(Swepub:uu)joeri542 (author)
  • Labots, Maaike (author)
  • Zellinger, Christina (author)
  • Seeger, Natalie (author)
  • Schuit, Robert (author)
  • Rongen, Marissa (author)
  • van Kooij, Rolph (author)
  • Windhorst, Albert D. (author)
  • Lammertsma, Adriaan A. (author)
  • de Lange, Elizabeth C. (author)
  • Voskuyl, Rob A. (author)
  • Koepp, Matthias (author)
  • Potschka, Heidrun (author)
  • Uppsala universitetGeriatrik (creator_code:org_t)

Related titles

  • In:Nuclear Medicine and Biology: Elsevier BV40:6, s. 764-7750969-80511872-9614

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