(3H)dipyridamole and (3H)nitrobenzylthioinosine binding sites at the human parietal cortex and erythrocyte adenosine transporter: A comparison

Jürgen Deckert, Anja Hennemann, Benjamin Bereznai, Jürgen Fritze, Reinhard Vock, Paul J. Marangos, Peter Riederer

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

We compared the binding sites of the adenosine transport inhibitors (3H)dipyridamole (DPR) and (3H)nitrobenzylthioinosine (NBI) in human parietal cortex and erythrocytes. In comparison with guinea pig (3H)DPR marked only slightly more binding sites than (3H)NBI with a Bmax of 1080±29 and 780±7 fmol/mg protein respectively in parietal cortex and 24288±2725 and 20875±1905 fmol/mg protein respectively in erythrocytes. NBI displaced (3H)DPR binding completely from its binding sites at about KD/2 concentrations in parietal cortex as well as erythrocytes with inhibition constants comparable to its dissociation constants. Lineweaver-Burke analysis in erythrocytes indicated a competitive inhibition of (3H)DPR binding by NBI. Pharmacological characterization of (3H)DPR binding sites in human erythrocytes is consistent with their localization on adenosine transporters. These findings provide evidence that as opposed to guinea pig (3H)DPR and (3H)NBI largely label binding sites to the same adenosine transporter in human erythrocytes and parietal cortex.

Original languageEnglish
Pages (from-to)1675-1682
Number of pages8
JournalLife Sciences
Volume55
Issue number21
DOIs
Publication statusPublished - 1994

Keywords

  • (H)dipyridamole
  • (H)nitrobenzylthioinosine
  • adenosine transporter
  • erythrocyte
  • parietal cortex

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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