Publisher
Florida Atlantic University
Description
Dysfunction of GABAB-receptor (GABAB-R)-mediated synaptic transmission underlies various nervous system disorders including epilepsy, depression, schizophrenia, and addiction. Currently, only one GABAB-R orthosteric ligand is in clinical use. However, side effects such as sedation, tolerance, and motor impairment limit its use. A dissociation of the therapeutic effects from the side effects may be achievable with drugs enhancing the endogenous physiological cellular response. The development of GABAB-R allosteric modulators has provided new modes of efficacy that may facilitate the development of novel therapeutic agents. In the present study, we investigated the effects of novel, newly synthesized GABAB-R allosteric ligands using a HEK-293 cell line stably expressing human GABAB1(b)/human GABAB(2) subunits using a cell-based cAMP HTRF assay. One compound was identified and characterized as a potential novel GABAB-R positive allosteric modulator (PAM), and will be subjected to further in vitro and in vivo analyses.
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Copyright © is held by the author, with permission granted to Florida Atlantic University to digitize, archive and distribute this item for non-profit research and educational purposes. Any reuse of this item in excess of fair use or other copyright exemptions requires permission of the copyright holder.
Title Plain
Development of cell-based functional assays to identify and characterize novel GABAb receptor allosteric modulators
Use and Reproduction
Copyright © is held by the author, with permission granted to Florida Atlantic University to digitize, archive and distribute this item for non-profit research and educational purposes. Any reuse of this item in excess of fair use or other copyright exemptions requires permission of the copyright holder.
Physical Location
Florida Atlantic University Libraries
Title
Development of cell-based functional assays to identify and characterize novel GABAb receptor allosteric modulators
Other Title Info
Development of cell-based functional assays to identify and characterize novel GABAb receptor allosteric modulators