Bicíková M, Hampl R
Endokrinologický ústav, Praha.
Cas Lek Cesk. 2007;146(3):223-6.
Neurosteroids are steroid structure hormones with neuroactive function. Neurosteroids have rapid, non-genomic actions in CNS. Non-conjugated metabolites of progesterone such as allopregnanolone, are potent positive modulators of GABAA receptors. They open ion channels for Cl- with analgetic, hypnotic, anxiolytic and anticonvulsant effects. By sulphatation the modulation on GABAA receptors is changed to negative with opposite effect. 19-C-steroids as dehydroepiandrosterone and its sulphate are negative modulators of GABAA receptors acting as an excitant and proconvulsant. They are able to modulate positively N-methyl-D-aspartate (NMDA) receptors and open ion canals for Ca2+. Changed (lowered) neurosteroid levels can be involved in many pathological processes as premenstrual syndrome, stress, depression, some forms of epilepsy, Alzheimer disease etc. Future study targeted on regulation of their production and metabolism and understanding of the mechanism of their actions will help to use them therapeutically.
神经甾体是具有神经活性功能的甾体结构激素。神经甾体在中枢神经系统中具有快速的非基因组作用。孕酮的非共轭代谢产物如别孕烯醇酮是GABAA受体的强效正性调节剂。它们打开氯离子离子通道,具有镇痛、催眠、抗焦虑和抗惊厥作用。通过硫酸化作用,对GABAA受体的调节变为负性,产生相反的效果。19-C-甾体如脱氢表雄酮及其硫酸盐是GABAA受体的负性调节剂,起兴奋和促惊厥作用。它们能够正向调节N-甲基-D-天冬氨酸(NMDA)受体并打开钙离子离子通道。神经甾体水平的改变(降低)可能与许多病理过程有关,如经前综合征、应激、抑郁、某些形式的癫痫、阿尔茨海默病等。针对其产生和代谢的调节以及对其作用机制的理解的未来研究将有助于将它们用于治疗。