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Barbiturate recognition site on the GABA/benzodiazepine receptor complex is distinct from the picrotoxinin/TBPS recognition site

1984; Elsevier BV; Volume: 106; Issue: 2 Linguagem: Inglês

10.1016/0014-2999(84)90737-4

1879-0712

Rosario Rich Trifiletti, Adele M. Snowman, Solomon H. Snyder,

Receptor Mechanisms and Signaling

The cage convulsant [35S]tert-butylbicyclophosphorothionate ([35S]TBPS) labels a presumed sedative-convulsant receptor complex. The relative potencies of barbiturates in competing for [35S]TBPS binding parallels their potencies in enhancing benzodiazepine receptor binding. Barbiturates inhibit [35S]TBPS binding in a complex, mixed competitive fashion, leading to a decrease in both the apparent affinity of TBPS for its sites and the apparent number of TBPS sites. All of the barbiturates examined markedly accelerate the dissociation of [35S]TBPS from its recognition sites, while picrotoxinin does not affect the dissociation. These results suggest that the barbiturate and picrotoxinin/TBPS recognition sites are distinct but allosterically linked.