MetabotropicGABAReceptors

Abstract

We provide an overview on the current knowledge on protein interactions with GABA B receptors. Furthermore, we review recent studies that tried to establish a link between polymorphisms in GABA B genes and congenital human diseases. Taking recent developments in the field into account, we also touch on the most promising indications for GABA B drugs. Last but not least, the cloned receptors were used to establish high‐throughput compound screens based on functional assays, which yielded the first allosteric compounds acting at GABA B receptors. The features of these compounds will be discussed.

GABA‐induced uncoupling of GABA/benzodiazepine site interactions is associated with increased phosphorylation of the GABAA receptor

“…Because GABA B receptor activation can modulate PKA and PKC activities (for review see Gassmann and Bettler, ), we asked whether GABA‐induced uncoupling is mediated by GABA B receptors. Results from binding experiments (Fig.…”

“…The slow inhibition via GABA B receptors plays an important role in the cerebral cortex, regulating network activity (Kohl and Paulsen, ). Because activation of GABA B receptors can modulate the activity of PKA and PKC (Gassmann and Bettler, ), we tested whether GABA‐induced uncoupling is mediated by binding of GABA to these receptors. Our results (Fig.…”