Up-regulation of brain [3H]diazepam binding sites in chronic caffeine treated rats.
Brain [3H]diazepam and [3H]L-phenylisopropyladenosine binding sites in caffeine treated (75 mg/kg/day, i.p. 12 days) and caffeine withdrawn (30 days) rats were examined. Treatment with caffeine (75 mg/kg/day) for 12 days increases the Bmax (maximum binding capacity) for [3H]diazepam binding by 30.9% whereas the same treatment increases the Bmax for [3H]L-PIA binding by 165%. The Bmax for [3H]diazepam binding sites returns to slightly below control levels but [3H]L-PIA binding sites remain elevated after 30 days of caffeine withdrawal. These findings suggest that the up-regulation of [3H]diazepam binding sites seen in caffeine treated rats may not be adequately explained by a direct antagonism of caffeine on benzodiazepine receptors. Other modes of interaction therefore must be considered.
D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D002110:Caffeine / Q000494:pharmacology*; D003975:Diazepam / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D010660:Phenylisopropyladenosine / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000187:drug effects; D011983:Receptors, Purinergic / Q000187:drug effects
D011963:Receptors, GABA-A; D011983:Receptors, Purinergic; D010660:Phenylisopropyladenosine; D002110:Caffeine; D003975:Diazepam