Triethyllead decreases central benzodiazepine receptor binding in rat cerebellum ex vivo

Add time:07/26/2019    Source:sciencedirect.com

Effect of triethyllead on the specific [3H]flunitrazepam binding was studied in rat cortical and cerebellar P2 fractions in vitro and in tissue homogenates of several rat brain regions ex vivo after 5 daily subcutaneous doses of 1.9 mg/kg triethyllead acetate to rats. Up to concentration of 100 μM, triethyllead did not significantly the specific [3H]flunitrazepam binding but attenuated marginally (14–18%) the GABAA receptor agonist, muscimol-induced elevation of [3H]flunitrazepam binding in cerebellar tissue. After the subacute treatment of rats with triethyllead, the specific [3H]flunitrazepam binding was 27% lower in cerebellum compared to control animals. In other brain regions the receptor binding was not changed. The data suggest that triethyllead modified the cerebellar GABAA receptor complex causing decreased binding in the benzodiazepine site. Such an inhibitory effect in the GABAA receptor complex may decrease cerebellarinhibitory output and augment the triethyllead induced convulsions and tremor.

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