Synthesis of C3, C5, and C7 pregnane derivatives and their effect on NMDA receptor responses in cultured rat hippocampal neurons.
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.
Stastna
Eva
E
Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i.,166 10 Prague 6, Czech Republic.
Chodounska
Hana
H
Pouzar
Vladimir
V
Kapras
Vojtech
V
Borovska
Jirina
J
Cais
Ondrej
O
Vyklicky
Ladislav
L
D000818:Animals; D002478:Cells, Cultured; D004553:Electric Conductivity; D006624:Hippocampus / Q000166:cytology*; D020128:Inhibitory Concentration 50; D009474:Neurons / Q000187:drug effects* / Q000378:metabolism; D018408:Patch-Clamp Techniques; D011278:Pregnanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*
D011278:Pregnanes; D016194:Receptors, N-Methyl-D-Aspartate