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Mechanism of the anticonvulsant action of diazepam

  • Pharmacology
  • Published:
Bulletin of Experimental Biology and Medicine Aims and scope

Abstract

Diazepam is highly effective in the prevention of convulsions induced by thiosemicarbazide (TSC), i.e., due to γ-aminobutyric acid (GABA) deficiency. Electrophysiological experiments to record the recovery cycle of the interzonal response of the cat motor cortex showed that diazepam reduces the amplitude of the test response, indicating the strengthening of inhibition. This test revealed antagonism of diazepam to bicuculline, specifically blocking GABA-ergic receptors, and to TSC. Diazepam was shown to be capable of increasing the GABA concentration in the brain by inhibiting the activity of GABA transaminase in the mitochondrial fraction of brain tissue.

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Authors
  1. R. U. Ostrovskaya
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  2. G. M. Molodavkin
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  3. R. P. Porfir'eva
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  4. A. M. Zubovskaya
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Ostrovskaya, R.U., Molodavkin, G.M., Porfir'eva, R.P. et al. Mechanism of the anticonvulsant action of diazepam. Bull Exp Biol Med 79, 270–273 (1975). https://doi.org/10.1007/BF00804212

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  • DOI: https://doi.org/10.1007/BF00804212

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