Nimodipine inhibits [3H]nitrobenzylthioinosine binding to the adenosine transporter in human brain

Jürgen Deckert, B. Bereznai, Anja Hennemann, Wieland Gsell, Mario Götz, Jürgen Fritze, Peter Riederer

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

The inhibition of [3H]nitrobenzylthioinosine ([3H]NBI) binding to human parietal cortex membranes by adenosine transport inhibitors, adenosine receptor agonists and antagonists and dihydropyridines was investigated. While the adenosine transport inhibitors inhibited [3H]NBI binding with Ki values in the low nanomolar range and the adenosine A1 receptor agonist, cyclopentyladenosine, with a Ki in the low micromolar range, no IC50 values could be obtained for the adenosine receptor antagonists at concentrations up to 100,000 nM. Among the dihydropyridines (+)-nimodipine was the most potent with a Ki of 201±55 nM. Inhibition of adenosine transport thus may contribute to the clinical effects of nimodipine in the central nervous system.

Original languageEnglish
Pages (from-to)131-133
Number of pages3
JournalEuropean Journal of Pharmacology
Volume238
Issue number1
DOIs
Publication statusPublished - Jul 6 1993

Fingerprint

Nimodipine
Adenosine
Dihydropyridines
Purinergic P1 Receptor Antagonists
Brain
Adenosine A1 Receptor Agonists
Purinergic P1 Receptor Agonists
Parietal Lobe
Inhibitory Concentration 50
Central Nervous System
Membranes
adenosine transporter

Keywords

  • Adenosine transporters
  • Nimodipine
  • Parietal cortex (human)
  • [H]Nitrobenzylthioinosine binding

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Nimodipine inhibits [3H]nitrobenzylthioinosine binding to the adenosine transporter in human brain. / Deckert, Jürgen; Bereznai, B.; Hennemann, Anja; Gsell, Wieland; Götz, Mario; Fritze, Jürgen; Riederer, Peter.

In: European Journal of Pharmacology, Vol. 238, No. 1, 06.07.1993, p. 131-133.

Research output: Contribution to journalArticle

Deckert, Jürgen ; Bereznai, B. ; Hennemann, Anja ; Gsell, Wieland ; Götz, Mario ; Fritze, Jürgen ; Riederer, Peter. / Nimodipine inhibits [3H]nitrobenzylthioinosine binding to the adenosine transporter in human brain. In: European Journal of Pharmacology. 1993 ; Vol. 238, No. 1. pp. 131-133.
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