CGS 8216 treatment decreases central-type benzodiazepine receptors in rat brain.
Central- and peripheral-type benzodiazepine receptors were analyzed in several brain areas of rats (n = 8-9) that had been treated for five days with CGS 8216 (20 mg/kg per day). Twenty-four hours after cessation of drug treatment a significant decrease of central-type benzodiazepine receptors as labeled by [3H]beta-carboline-3-carboxylate ethyl ester ([3H]beta CCE) and [3H]flunitrazepam ([3H]FNZ), but not of peripheral-type benzodiazepine receptors as labeled by [3H]RO 5-4864 could be observed in the animals treated with CGS 8216.
Deckert
J
J
Unit on Neurochemistry, NIMH, Bethesda, MD 20892.
Estall
L B
LB
Marangos
P J
PJ
Cooper
S J
SJ
D000818:Animals; D001569:Benzodiazepines / Q000037:antagonists & inhibitors*; D001570:Benzodiazepinones / Q000378:metabolism; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D002243:Carbolines / Q000378:metabolism; D003292:Convulsants / Q000378:metabolism; D005445:Flunitrazepam / Q000378:metabolism; D008297:Male; D011720:Pyrazoles / Q000494:pharmacology*; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects*
D001570:Benzodiazepinones; D002243:Carbolines; D003292:Convulsants; D011720:Pyrazoles; D011963:Receptors, GABA-A; D001569:Benzodiazepines; C028513:4'-chlorodiazepam; D005445:Flunitrazepam; C024915:beta-carboline-3-carboxylic acid ethyl ester; C033830:2-phenylpyrazolo(4,3-c)quinolin-3(5H)-one