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Increase in tritium labeled flunitrazepam binding in vitro and in vivo to rat brain benzodiazepine receptors by tofisopam a 3 4 benzodiazepine

Increase in tritium labeled flunitrazepam binding in vitro and in vivo to rat brain benzodiazepine receptors by tofisopam a 3 4 benzodiazepine

Pharmacological Research Communications 13(1): 75-86

3H-flunitrazepam binding was measured in rat brain homogenates and the effect of the anxiolytic tofisopam, a 3,4-benzodiazepine, and diazepam, a 1,4-benzodiazepine on the binding was studied. Diazepam displaced the labeled ligand from receptors concentration-dependently, but tofisopam increased the binding by 5-10% at concentrations 0.1 nM-1 .mu.M. When administered in vivo to rats, tofisopam (300 mg/kg p.o. (per os)) increased the binding of i.v. injected 3H-flunitrazepam by 26.3%, while the binding in diazepam 925 mg/kg p.o.) pretreated rats decreased by 27.7%. When the binding studies were performed with 3H-tofisopam as ligand, no specific binding could be seen in vitro. Tofisopam does not bind to benzodiazepine receptors in vitro or in vivo after acute treatment and does not have such specific binding sites as 1,4-benzodiazepines in rat brain. Tofisopam increases the binding of 3H-flunitrazepam, a 1,4-benzodiazepine, to rat brain benzodiazepine receptors in vitro and in vivo after acute treatment.

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Accession: 005661854

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