Abstract
A quantitative relationship between the efficacy (i.e. maximum enhancement) of Cl − to increase [ 3H]flunitrazepam binding and the density of [ 35S] -t- butylbicyclophosphorothionate binding sites was observed in well-washed membrane fragments of rat cerebral cortex previously exposed to phospholipase A 2. This relationship (described by the equation y = AB x ) was maintained when [ 3H]flunitrazepam was assayed at Cl − concentrations between 100 and 600 mM, and was not qualitatively altered by the presence of 100 μM pentobarbital. However, under experimental conditions that reduced the ratio of [ 35S]TBPS binding sites/benzodiazepine receptors, the effects of pentobarbital suggest that the conductance state of benzodiazepine receptor-coupled chloride channels may be the primary determinant of Cl − enhanced [ 3H]flunitrazepam binding.
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