Benzodiazepine inhibition of adenosine uptake is not prevented by benzodiazepine antagonists.
Uptake of [3H]adenosine into rat cerebral cortex synaptosomes was studied. Hexobendine (10(-5) M) and the benzodiazepine agonists diazepam (10(-5) M) and flurazepam (10(-4) M) significantly inhibited this uptake, but only if the compounds were pre-incubated for 10 min in the case of the benzodiazepines. The benzodiazepine antagonists Ro15-1788 (10(-5) M) and CGS 8216 (10(-5) M) failed to reverse the action of benzodiazepine agonists or hexobendine on [3H]adenosine uptake. The results add weight to the view that inhibition of adenosine uptake processes by benzodiazepines do not contribute to their behavioural effects.
D000241:Adenosine / Q000378:metabolism*; D000818:Animals; D001569:Benzodiazepines / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D001570:Benzodiazepinones / Q000494:pharmacology; D001921:Brain / Q000378:metabolism*; D003975:Diazepam / Q000494:pharmacology; D005442:Flumazenil; D005479:Flurazepam / Q000494:pharmacology; D006592:Hexobendine / Q000494:pharmacology; D066298:In Vitro Techniques; D011720:Pyrazoles / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013574:Synaptosomes / Q000378:metabolism; D013696:Temperature
D001570:Benzodiazepinones; D011720:Pyrazoles; D001569:Benzodiazepines; D005442:Flumazenil; C033830:2-phenylpyrazolo(4,3-c)quinolin-3(5H)-one; D006592:Hexobendine; D005479:Flurazepam; D000241:Adenosine; D003975:Diazepam