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.