Neurosteroids: Can a 2alpha,3alpha-epoxy ring make up for the 3alpha-hydroxyl group?
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- 作者：Alexander Kasala ; Kasal@uochb.cas.cz" class="auth_mail" title="E-mail the corresponding author ; Kasal.Alexander@volny.cz" class="auth_mail" title="E-mail the corresponding author ; Milo&scaron ; Budě&scaron ; í ; nský ; a ; Pavel Mare&scaron ; b ; Zdena Kri&scaron ; tofí ; ková ; c ; Alcino J. Leitã ; od ; e ; Maria Luisa Sá ; e Melod ; e ; Maria Manuel C. Silvad ; e
- 关键词：Neurosteroids ; NMR spectrometry ; GABAA receptor ; TBPS-test ; Pentylenetetrazol (PTZ) model ; Epileptic seizures ; Epoxidation
- 刊名：Steroids
- 出版年：2016
- 出版时间：January 2016
- 年：2016
- 卷：105
- 期：Complete
- 页码：12-18
- 全文大小：545 K
文摘
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2α,3α-epoxy-5α-pregnan-20-one lacks the 3α-hydroxyl.
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Still it binds GABAAR receptor 2α,3α-epoxides 4 and 7 exhibit moderate dose-dependent action in 12 day old rats.
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The above GABAA-like activity is reduced in more polar analogues.