Upregulation of adenosine A1 receptors and forskolin binding sites following chronic treatment with caffeine or carbamazepine: a quantitative autoradiographic study.
The effects of feeding a diet enriched in caffeine or carbamazepine (CBZ) were investigated in rats in a quantitative autoradiographic study of adenosine A1 receptors (labeled by [3H]cyclohexyladenosine, [3H]CHA) and adenylate cyclase (labeled by [3H]forskolin). Although regional distribution of [3H]CHA and [3H]forskolin binding sites differed in some areas, chronic CBZ as well as chronic caffeine upregulated both of them. The changes in receptor densities occurred in the same brain microregions, suggesting that caffeine and CBZ act as antagonists at similar subpopulations of adenosine A1 receptors and [3H]forskolin binding sites. Therefore, a selective interaction of these two drugs with distinct adenosine A1 receptors (and adenylate cyclase) probably does not explain the differential effects of caffeine and CBZ on neuronal activity.
Daval
J L
JL
Unit on Neurochemistry, National Institute of Mental Health, Bethesda, Maryland 20892.
Deckert
J
J
Weiss
S R
SR
Post
R M
RM
Marangos
P J
PJ
D000241:Adenosine / Q000031:analogs & derivatives / Q000378:metabolism; D000818:Animals; D001345:Autoradiography; D001665:Binding Sites / Q000187:drug effects; D002110:Caffeine / Q000494:pharmacology; D002220:Carbamazepine / Q000494:pharmacology; D005576:Colforsin / Q000378:metabolism*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011983:Receptors, Purinergic / Q000378:metabolism*; D013997:Time Factors
D011983:Receptors, Purinergic; D005576:Colforsin; D002220:Carbamazepine; C027513:N(6)-cyclohexyladenosine; D002110:Caffeine; D000241:Adenosine