Characterization of benzodiazepine and gamma-aminobutyric recognition sites and their endogenous modulators

摘要: The solubilization and partial purification from rat brain cortex homogenates of [3H]gamma-aminobutyric acid (GABA) [3H]diazepam recognition sites their endogenous modulators (GABA-modulin an compound which specifically bound [3H]diazepam) are reported. A high percentage GABA binding (virtually free benzodiazepine sites) was solubilized incubated at 0 degree C with 1% Triton X-100 a mixture protease inhibitors. large proportion in the absence apparent capacity by incubating crude synaptic membrane preparations 37 0.05% X-100. characteristics these two resemble those membrane-bound sites. However, unlike sites, insensitive to stimulation, while no longer protected benzodiazepines against heat inactivation. These results indicate that reside different molecules which, when membranes, can interact reciprocally modulate affinity for specific ligands.