Valerenic acid derivatives as novel subunit-selective GABAA receptor ligands - in vitro and in vivo characterization

Khom, S.; Strommer, B.; Ramharter, J.; Schwarz, T.; Schwarzer, C.; Erker, T.; Ecker, G. F.; Mulzer, J.; Hering, S.

British Journal of Pharmacology  (2010),  161(1),  65-78.

Valerenic acid derivatives with higher efficacy and affinity can be generated. Greater in vitro action of the amide derivative correlated with a more pronounced anxiolytic effect in vivo. The data give further confidence in targeting β₃ subunit containing GABA_A receptors for development of anxiolytics.