Effects of 3α-Amino-5α-pregnan-20-one on GABAA Receptor: Synthesis, Activity and Cytotoxicity

descriptionPublicationkeyboard_double_arrow_right Article 01 Jan 2004 Spain English Publisher:Institute of Organic Chemistry & BiochemistryJournal:Collection of Czechoslovak Chemical Communications, volume 69, pages 1,506-1,516 (issn: 0010-0765, eissn: 1212-6950,

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Authors: Matyáš, Libor; Kasal, Alexander; Babot, Zoila; Suñol, Cristina;

doi: 10.1135/cccc20041506

handle: 10261/270883

Effects of 3α-Amino-5α-pregnan-20-one on GABAA Receptor: Synthesis, Activity and Cytotoxicity

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Abstract

The 3α-hydroxy function has been considered essential for the biological activity of neurosteroids at the GABAA receptor. It was found that 3α-amino-5α-pregnan-20-one (3) increased the binding of [3H]flunitrazepam at the GABAA receptor in the primary culture of cortical neurons. This derivative did not display cytotoxicity at relevant neuroactive concentrations, and its structure enabled us to gain further insight into possible functional group modifications in position 3α. Various synthetic methods were investigated in search for the most suitable synthetic approach.

Country

Spain

Related Organizations

Institute of Biomedical Research of Barcelona
Spain
Spanish National Research Council
Spain
Czech Academy of Sciences
Czech Republic

Keywords

Cytotoxicity, GABAA receptor, Steroids, MoO3, Allopregnanolone, Neurosteroids, [3H]Flunitrazepam, 3α-Amino-5α-pregnan-20-one

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