Ass. Prof. Priv.-Doz. Dr. Margot Ernst, PhD

Department(s): Department of Pathobiology of the Nervous System (Center for Brain Research)
Position: Assistant Professor
Location: Spitalgasse 4
Telephone: 40160-34065
E-Mail:

Research Area:
Neuropharmacology

Research Interests:
Benzodiazepines, Molecular Structure, Receptors, GABA-A

Principle Investigator(s):

• Ernst, Margot (Head)

Interest Group(s):

• Neurobiology of Emotion and Cognition
• Neuroimaging
• Neuropsychopharmacology

Grant(s):

• Alpha6 GABAA receptors in neuropsychiatric disorders (Responsible)
• Identification of binding sites in GABA-A receptors (Responsible)
• Ligands for the GABA-A receptor alpha+/ beta- interface (Responsible)
• Molecular Drug Targets / Structural Studies and Ligand Development for GABA-A Receptor Subtypes (Responsible)
• NeuroDeRisk (Responsible)

GABA-A Receptor Pharmacology and Structure

Abstract:

We are interested in the molecular structure of allosteric the binding sites present on GABA-A receptor subtypes, in the identification and pharmacology of subtype selective compounds and the molecular mechanisms behind so-called functional selectivity. We collaborate with Medicinal Chemists and Pharmacoinformatics groups, as well as pharmacologists whose research techniques complement ours.

Techniques:

Expression of wild type and mutated recombinant GABA-A receptors in Xenopus laevis oocytes, HEK cells and other host cells, two electrode voltage clamp electrophysiology, radioligand binding assays; homology modelling, computational docking

Selected Publications:

1. Varagic Z, Wimmer L, Schnuerch M, Mihovilovic MD, Huang S, Rallapalli S, Cook JM, Mirheydari P, Ecker GF, Sieghart W, Ernst M (2013) Identification of novel positive allosteric modulators and null modulators at the GABA-a receptor alpha+beta-interface Br J Pharmacol, 169(2): 371-383
2. Varagic Z, Ramerstorfer J, Huang S, Rallapalli S, Sarto-Jackson I, Cook J, Sieghart W, Ernst M (2013) Subtype selectivity of alpha+beta-site ligands of GABA-A receptors - identification of the first highly specific positive modulators at alpha6beta2/3gamma2 receptors Br J Pharmacol, 169(2): 384-399
3. Richter L, de Graaf C, Sieghart W, Varagic Z, Mörzinger M, de Esch IJP, Ecker GF, Ernst M (2012) Diazepam-bound GABA-A receptor models identify new benzodiazepine binding site ligands Nature Chem Biol, 8: 455-464
4. Ramerstorfer J, Furtmüller R, Sarto-Jackson I, Varagic Z, Sieghart W, Ernst M (2011) The GABA-A receptor alpha+beta-interface: a novel target for subtype-selective drugs J Neurosci, 31: 870-877
5. Sieghart W, Ernst M (2005) Heterogeneity of GABA-A receptors: revived interest in the development of subtype-selective drugs Curr Med Chem - Centr Nervous Syst, 5: 217-242
   | Article (PDF) |

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