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Interaction between methylxanthines and the benzodiazepine receptor.

Roger Weir, Robert E. Hruska

Open publisher page 35 citations

Abstract

3H-Flunitrazepam (500 pM) was used to estimate the inhibitory effects of caffeine, theophylline, theobromine and 3-methylxanthine on binding to rat brain homogenates. Caffeine and theophylline showed a low affinity competitive type of inhibition in vitro, but no inhibition in vivo. Low concentrations of caffeine failed to show clear inhibitory capabilities against low concentrations of 3H-flunitrazepam. The results suggest that only the toxic central nervous system effects of methylxanthines are mediated via the benzodiazepine receptor.

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What this paper is about

3H-Flunitrazepam (500 pM) was used to estimate the inhibitory effects of caffeine, theophylline, theobromine and 3-methylxanthine on binding to rat brain homogenates. Caffeine and theophylline showed a low affinity competitive type of inhibition in vitro, but no inhibition in vivo. Low concentrations of caffeine failed to show clear inhibitory capabilities against low concentrations of 3H-flunitrazepam. The results suggest that only the toxic central nervous system effects of methylxanthines are mediated via the benzodiazepine receptor.

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Available abstract

3H-Flunitrazepam (500 pM) was used to estimate the inhibitory effects of caffeine, theophylline, theobromine and 3-methylxanthine on binding to rat brain homogenates. Caffeine and theophylline showed a low affinity competitive type of inhibition in vitro, but no inhibition in vivo. Low concentrations of caffeine failed to show clear inhibitory capabilities against low concentrations of 3H-flunitrazepam. The results suggest that only the toxic central nervous system effects of methylxanthines are mediated via the benzodiazepine receptor.

Key concepts: Caffeine, Theophylline, Theobromine, Flunitrazepam, Pharmacology, Chemistry, Inhibitory postsynaptic potential, Benzodiazepine

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