Inhibition of adenosine accumulation by a CNS benzodiazepine antagonist (Ro 15-1788) and a peripheral benzodiazepine receptor ligand (Ro 05-4864).
Although benzodiazepines can inhibit adenosine uptake into central neurones, this effect is not antagonized by behaviourally effective 'benzodiazepine antagonists' such as Ro 15-1788. We now report that Ro 15-1788 and the 'peripheral' benzodiazepine ligand Ro 05-4864 themselves inhibit adenosine accumulation by rat brain synaptosomes. The inhibition of adenosine accumulation may thus underlie those behavioural effects of benzodiazepines which are mimicked but not antagonized by Ro 15-1788.
D000241:Adenosine / Q000037:antagonists & inhibitors*; D000818:Animals; D001569:Benzodiazepines / Q000037:antagonists & inhibitors*; D001570:Benzodiazepinones / Q000494:pharmacology*; D002490:Central Nervous System / Q000187:drug effects*; D003975:Diazepam / Q000494:pharmacology; D005442:Flumazenil; D005479:Flurazepam / Q000494:pharmacology; D006592:Hexobendine / Q000494:pharmacology; D008297:Male; D051381:Rats; D013574:Synaptosomes / Q000378:metabolism; D013997:Time Factors
D001570:Benzodiazepinones; D001569:Benzodiazepines; C028513:4'-chlorodiazepam; D005442:Flumazenil; D006592:Hexobendine; D005479:Flurazepam; D000241:Adenosine; D003975:Diazepam