A [18F]-FNECA széleskörúen alkalmazható radioligand a purinerg receptorexpresszió PET-vizsgálatához.

Translated title of the contribution: The [18F]-FNECA serves as a suitable radioligand for PET investigation of purinergic receptor expression

T. Márián, Szabolcs Lehel, Z. Lengyel, L. Balkay, Géza Horváth, Pál Mikecz, Tünde Miklovicz, I. Fekete, A. József Szentmiklósi

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

The well known and widely used P1 adenosine agonist, 5'-N-ethyl-carboxamidoadenosine (NECA), was labelled with 18F isotope for the in vivo PET investigation of A1, A2 and A3 adenosine receptor expression. The precursor 2-[18F]fluoroethylamine was reacted with 2',3'-O-isopropylideneadenosine-5'-uronic acid. Specific activity of the [18F]-FNECA was (2.3 +/- 1.1) TBq/mmol (60 Ci/mmol). Dynamic PET measurements were carried out in rabbits to study the in vivo kinetics of the receptor saturation with the labelled ligand. The time dependent accumulation was followed up in the heart, lungs, liver, brain and testis. The radiotracer uptake was rapid and reached its maximum in less than two minutes in the heart and testes after v. injection of the radiopharmaceutical, while it took about 6 minutes in the brain, lungs and liver. High [18F]-FNECA accumulation was detected in the intestines, too. The specific binding of the [18F]-FNECA was tested in competition experiments in brain and heart sections using autoradiographic technique. The outlined synthesis provided sufficient amounts of [18F]-FNECA to map adenosine receptor expression under physiological conditions.

Original languageHungarian
Pages (from-to)1319-1322
Number of pages4
JournalOrvosi Hetilap
Volume143
Issue number21 Suppl 3
Publication statusPublished - May 26 2002

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Purinergic Receptors
Testis
Brain
Adenosine A3 Receptors
Adenosine A2 Receptors
Uronic Acids
Adenosine A1 Receptors
Lung
Purinergic P1 Receptors
Radiopharmaceuticals
Liver
Isotopes
Adenosine
Intestines
Rabbits
Ligands
Injections

ASJC Scopus subject areas

  • Medicine(all)

Cite this

A [18F]-FNECA széleskörúen alkalmazható radioligand a purinerg receptorexpresszió PET-vizsgálatához. / Márián, T.; Lehel, Szabolcs; Lengyel, Z.; Balkay, L.; Horváth, Géza; Mikecz, Pál; Miklovicz, Tünde; Fekete, I.; Szentmiklósi, A. József.

In: Orvosi Hetilap, Vol. 143, No. 21 Suppl 3, 26.05.2002, p. 1319-1322.

Research output: Contribution to journalArticle

Márián, T, Lehel, S, Lengyel, Z, Balkay, L, Horváth, G, Mikecz, P, Miklovicz, T, Fekete, I & Szentmiklósi, AJ 2002, 'A [18F]-FNECA széleskörúen alkalmazható radioligand a purinerg receptorexpresszió PET-vizsgálatához.', Orvosi Hetilap, vol. 143, no. 21 Suppl 3, pp. 1319-1322.
Márián, T. ; Lehel, Szabolcs ; Lengyel, Z. ; Balkay, L. ; Horváth, Géza ; Mikecz, Pál ; Miklovicz, Tünde ; Fekete, I. ; Szentmiklósi, A. József. / A [18F]-FNECA széleskörúen alkalmazható radioligand a purinerg receptorexpresszió PET-vizsgálatához. In: Orvosi Hetilap. 2002 ; Vol. 143, No. 21 Suppl 3. pp. 1319-1322.
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