Abstract
We have characterized the γ-aminobutyric acid-A (GABA A) and benzodiazepine (BZ) receptors in in vitro living slices of adult rat neocortex using [ 3H]SR95531, a GABA A antagonist, and [ 3H]flunitrazepam (FNZ), a BZ ligand. [ 3H]SR95531 labelled a single population of GABA A receptors with a B max of 1030.7 fmol/mg protein and a K d of 43.5 nM. [ 3H]FNZ also labelled a single binding site with a B max of 4239 fmol/mg protein and a K d of 22 nM. The GABA A receptor labelled using [ 3H]SR95531 could be down-regulated by 2 h preincubations in GABA and the GABA A agonist muscimol (8% and 11%, respectively). Increases in cellular electrical activity induced by a combination of veratridine and glutamate led to an average increase in GABA A receptor number of 58%. The BZ binding site labelled with [ 3H]FNZ was down-regulated by clonazepam (−55%), increased by GABA (+17%), but not altered by changes in electrical activity. The present results demonstrate the rapid differential regulation of a ligand-gated receptor by agonist stimulation or increases in bioelectric activity. Such regulation may provide clues to the nature of the modification which occur following changes in cellular activity in the cortex.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
