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

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

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish (US)
Pages (from-to)441-447
Number of pages7
JournalEuropean Journal of Pharmacology
Volume106
Issue number2
DOIs
StatePublished - Nov 13 1984

Keywords

  • Barbiturate
  • Benzodiazepine
  • Convulsant
  • Picrotoxin
  • Sedative

ASJC Scopus subject areas

  • Pharmacology

Fingerprint

Dive into the research topics of 'Barbiturate recognition site on the GABA/benzodiazepine receptor complex is distinct from the picrotoxinin/TBPS recognition site'. Together they form a unique fingerprint.

Cite this