Date of Award
2013
Document Type
Dissertation/Thesis
Submission Date
October 2026
Thesis/Dissertation Advisor [Chair]
McDonald, Patricia
Thesis/Dissertation Co-Chair
Quintyne, Nicholas
Abstract
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.
Recommended Citation
Aitken, Maria de Lourdes, "Development of cell-based functional assays to identify and characterize novel GABAb receptor allosteric modulators" (2013). Harriet L Wilkes Honors College Theses 2010 - 2019. 136.
https://digitalcommons.fau.edu/etd_honors_2/136
Extent
47 p.
Identifier
FA00003502
Comments
Includes bibliography.