J. Deckert et al., NIMODIPINE INHIBITS [H-3] NITROBENZYLTHIOINOSINE BINDING TO THE ADENOSINE TRANSPORTER IN HUMAN BRAIN, European journal of pharmacology, 238(1), 1993, pp. 131-133
The inhibition of [H-3]nitrobenzylthioinosine ([H-3]NBI) binding to hu
man parietal cortex membranes by adenosine transport inhibitors, adeno
sine receptor agonists and antagonists and dihydropyridines was invest
igated. While the adenosine transport inhibitors inhibited [H-3]NBI bi
nding with K(i) values in the low nanomolar range and the adenosine A1
receptor agonist, cyclopentyladenosine, with a K(i) in the low microm
olar range, no IC50 values could be obtained for the adenosine recepto
r antagonists at concentrations up to 100,000 nM. Among the dihydropyr
idines (+)-nimodipine was the most potent with a K(i) of 201 +/- 55 nM
. Inhibition of adenosine transport thus may contribute to the clinica
l effects of nimodipine in the central nervous system.