Decreased Brain GABAA-Benzodiazepine Receptor Binding in Panic Disorder

Decreased brain GABA(A)-benzodiazepine receptor binding in panic disorder: preliminary results from a quantitative PET study.

BACKGROUND Positron emission tomography (PET) allows the measurement of benzodiazepine-gamma-aminobutyric acidA (GABA(A)) receptor kinetics. We employed flumazenil radiolabeled with carbon 11, a radioligand that labels the benzodiazepine site on the GABA(A) receptor, and fully quantitative, high-sensitivity PET to test the hypothesis that central benzodiazepine site binding is decreased in medi...

Different residues in the GABAA receptor benzodiazepine binding pocket mediate benzodiazepine efficacy and binding.

Benzodiazepines (BZDs) exert their therapeutic actions by binding to the GABA(A) receptor (GABA(A)R) and allosterically modulating GABA-induced chloride currents (I(GABA)). A variety of ligands with divergent structures bind to the BZD site, and the structural mechanisms that couple their binding to potentiation of I(GABA) are not well understood. In this study, we measured the effects of indiv...

[11c]FLUMaZeNIL gabaA-beNZoDIaZepINe receptor bINDINg IN MAjOR DEPRESSIvE DISORDER vERSUS HEALTHY CONTROLS

Ligands of the GABAA Receptor Benzodiazepine Binding Site

Benzodiazepine (BZ) binding site ligands are important central nervous system (CNS) drugs. Their numbers and our knowledge of how they interact with the BZ-binding site of GABAA receptors are both rapidly expanding. The GABAA receptor is a member of the ligand-gated ion channel superfamily. In general, it consists of an assembly of transmembrane pentamers of different subunit compositions (1). ...

Decreased GABAA receptors and benzodiazepine binding sites in the anterior cingulate cortex in autism.

The anterior cingulate cortex (ACC; BA 24) via its extensive limbic and high order association cortical connectivity to prefrontal cortex is a key part of an important circuitry participating in executive function, affect, and socio-emotional behavior. Multiple lines of evidence, including genetic and imaging studies, suggest that the ACC and gamma-amino-butyric acid (GABA) system may be affect...