Synthesis of C3, C5, and C7 pregnane derivatives and their effect on NMDA receptor responses in cultured rat hippocampal neurons

Eva Stastna; Hana Chodounska; Vladimir Pouzar; Vojtech Kapras; Jirina Borovska; Ondrej Cais; Ladislav Vyklicky Jr

doi:10.1016/j.steroids.2008.11.011

Synthesis of C3, C5, and C7 pregnane derivatives and their effect on NMDA receptor responses in cultured rat hippocampal neurons

Steroids. 2009 Feb;74(2):256-63. doi: 10.1016/j.steroids.2008.11.011. Epub 2008 Nov 24.

Authors

Eva Stastna¹, Hana Chodounska, Vladimir Pouzar, Vojtech Kapras, Jirina Borovska, Ondrej Cais, Ladislav Vyklicky Jr

Affiliation

¹ Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i.,166 10 Prague 6, Czech Republic.

PMID: 19071149
DOI: 10.1016/j.steroids.2008.11.011

Abstract

The synthesis of several novel 5alpha- and 5beta-20-oxo-pregnane derivatives substituted in the position 3 and 7 of the steroid skeleton is described. Activity of synthesized compounds was studied in voltage-clamped cultured rat hippocampal neurons. Substituted derivatives inhibited NMDA-elicited neuronal activity. The relationship between biological activity and structure is discussed.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Cells, Cultured
Electric Conductivity
Hippocampus / cytology*
Inhibitory Concentration 50
Neurons / drug effects*
Neurons / metabolism
Patch-Clamp Techniques
Pregnanes / chemical synthesis*
Pregnanes / chemistry
Pregnanes / pharmacology*
Rats
Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*

Substances

Pregnanes
Receptors, N-Methyl-D-Aspartate