Benzodiazepines are weak inhibitors of [3H]nitrobenzylthioinosine binding to adenosine uptake sites in brain.
Saturable, specific, high affinity binding of the potent adenosine uptake inhibitor [3H]nitrobenzylthioinosine ([3H]NBI) to brain membranes has been demonstrated. In an effort to test the hypothesis that benzodiazepine action may be due to the inhibition of adenosine uptake, the inhibition of [3H]NBI binding by diazepam, clonazepam and chlordiazepoxide was tested. The benzodiazepines are very weak inhibitors of [#H]NBI binding, having IC50 values several orders of magnitude above their therapeutic levels.
D000241:Adenosine / Q000378:metabolism*; D000818:Animals; D001569:Benzodiazepines / Q000494:pharmacology*; D001665:Binding Sites; D001921:Brain / Q000378:metabolism* / Q000648:ultrastructure; D002462:Cell Membrane / Q000378:metabolism; D007288:Inosine / Q000031:analogs & derivatives*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013574:Synaptosomes / Q000378:metabolism; D013868:Thioinosine / Q000031:analogs & derivatives* / Q000378:metabolism; D014316:Tritium
D014316:Tritium; D001569:Benzodiazepines; D013868:Thioinosine; D007288:Inosine; C001789:4-nitrobenzylthioinosine; D000241:Adenosine