Detailansicht
A novel automated screening system for characterization of GABAA receptor ligands
Igor Baburin
Art der Arbeit
Dissertation
Universität
Universität Wien
Fakultät
Fakultät für Physik
Betreuer*in
Steffen Hering
DOI
10.25365/thesis.4093
URN
urn:nbn:at:at-ubw:1-29981.03680.940063-8
Link zu u:search
(Print-Exemplar eventuell in Bibliothek verfügbar)
Abstracts
Abstract
(Deutsch)
Vom Verfasser nicht angegeben
Abstract
(Englisch)
In the present work, I describe a newly developed system for drug screening on voltage- and ligand-gated ion channels during two-microelectrode voltage clamp (TEVC) experiments on Xenopus oocytes. The method combines the advantages of fast perfusion ("concentration jump" drug applications) and automation of drug delivery. The basic features of the novel system are illustrated in experiments on muscle type nicotinic acetylcholine (nACh) receptors and Kv1.1 channels. Based on this technique in combination with high-performance liquid chromatography - photodiode-array detection - mass spectrometry (HPLC-PDA-MS), an efficient approach for screening and subsequent activity profiling of plant and fungal extracts on GABAA receptors was established. In a first application the assay was used to screen an extract library consisting of 704 plants and fungi. Subsequently the method was applied to investigate the pharmacological properties of GABAA receptors containing a1, b2 and g1 subunits. Being expressed only in a few areas of the brain, g1-containing receptors represent an interesting drug target. In continuation of this work, we developed an approach for estimation of benzodiazepine (BZD) efficiency that accounts for mixed population of a1b2- and a1b2g2S(g1)-containing GABAA receptors.
Schlagwörter
Schlagwörter
(Englisch)
GABAA receptor Xenopus oocytes Benzodiazepine Two-microelectrode voltage clamp screening
Schlagwörter
(Deutsch)
GABAA Rezeptor Xenopus Oozyten Benzodiazepine Zwei-Mikroelektroden Spannungsklemmtechnik Screening
Autor*innen
Igor Baburin
Haupttitel (Englisch)
A novel automated screening system for characterization of GABAA receptor ligands
Paralleltitel (Deutsch)
Ein neues, automatisches Screening-System für die Charakterisierung von GABAA Rezeptor Liganden
Publikationsjahr
2009
Umfangsangabe
96 S. : Ill., graph. Darst.
Sprache
Englisch
Beurteiler*innen
Erwin Sigel ,
Hanns Möhler
Klassifikation
30 Naturwissenschaften allgemein > 30.03 Methoden und Techniken in den Naturwissenschaften
AC Nummer
AC05039848
Utheses ID
3616
Studienkennzahl
UA | 091 | 411 | |