Abstract
γ-Aminobutyric acid (GABA), one of the most ubiquitous inhibitory neurotrasmitter in the central nervous system (CNS), binds to its recognition sites, GABA receptor, and decreases neuronal excitability by increasing membrane chloride conductance. GABAA receptors are supermolecular receptor-chloride channel complexes of multiple subunits (α, β and γ) with distinct but interacting recognition sites for the neurotrasmitter, for convulsants (such as picrotoxin and bicyclophosphorothionates), and for depressants (such as benzodiazepines, barbiturates and neurosteroids) (MacDonald and Olsen, 1994).
This is a preview of subscription content, log in via an institution to check access.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
Reference
Bianucci A.M., Da Settimo A., Da Settimo F., Primofiore G., Martini C., Giannaccini G. and Lucacchini A., 1992, Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives, J Med Chem35: 2214.
Da Settimo A., Primofiore G., Da Settimo F., Lucacchini A., Martini C. and Senatore G., 1993, Benzodiazepine receptor affinity of new indole derivatives, Farmaco48: 285.
MacDonald R.L. and Olsen R.W., 1994, GABAA receptor channels, Annu Rev Neurosci17: 569.
Primofiore G., Marini A.M., Da Settimo F., Martini C., Bardellini A., Giannaccini G. and Lucacchini A., 1989, Specific inhibition of benzodiazepine receptor binding by some N-(indol-3-ylglyoxylyl)amino acid derivatives: stereoselective interactions, J Med Chem32: 2514.
Zhang W., Koehler K.F., Zhang P. and Cook J.M., 1995, Development of a comprehensive pharmacophore model for the benzodiazepine receptor, Drug Design and Discovery12: 193.
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1996 Plenum Press, New York
About this chapter
Cite this chapter
Da Settimo, A. et al. (1996). Indole Derivatives as Probes to Study the Benzodiazepine Binding Site in Gaba Receptor Complex. In: Filippini, G.A., Costa, C.V.L., Bertazzo, A. (eds) Recent Advances in Tryptophan Research. Advances in Experimental Medicine and Biology, vol 398. Springer, Boston, MA. https://doi.org/10.1007/978-1-4613-0381-7_109
Download citation
DOI: https://doi.org/10.1007/978-1-4613-0381-7_109
Publisher Name: Springer, Boston, MA
Print ISBN: 978-1-4613-8026-9
Online ISBN: 978-1-4613-0381-7
eBook Packages: Springer Book Archive