[Zurück]

G. Pototschnig, S. Hering, M.D. Mihovilovic:
"Scaffold Optimization Of The Gabaa Receptor Ligand Valerenic Acid";
Vortrag: 4th Meeting of the Paul Ehrlich MedChem Euro-PhD Network, Hradec Kralove; 20.06.2014 - 22.06.2014; in: "Book of Abstracts", (2014), S. 29.

Anxiety disorders are amongst the most common mental diseases worldwide. Benzodiazepines represent
one of the most prescribed drugs to address anxiety and panic disorders. However, benzodiazepines are
known to cause severe side effects like confusion, fatigue and drug addiction.
Valerenic acid, a sesquiterpenoidal compound isolated from roots of Valeriana officinalis, acts as
subtype selective allosteric ligand on the GABAA receptor.1 The highly pronounced selectivity for β2/3
over β1 subunits allows for addressing anxiety rather than sedation in animal models.2
Different regions of the complex original structure were modified to gain insight into the so far unknown
binding mode and mode of action of this class of GABAA ligands (Fig. 1). Molecules with expanded
ring size as well as partially planarized structures were synthesized; steric demand in the receptor was
investigated via variation of R2 and R3.

valerenic acid; GABAA Receptor

http://publik.tuwien.ac.at/files/PubDat_230076.pdf