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Excitatory neurosteroids

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Current revision (10:53, 9 January 2023) (edit) (undo)
 
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<StructureSection load='5o8f' size='340' side='right' caption='Structure of a chimaeric beta3-alpha5 GABAA receptor in complex with pregnanolone (based on [[5o8f]]) scene='89/896619/Cv/3'>
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<StructureSection load='5o8f' size='340' side='right' caption='Structure of a chimaeric beta3-alpha5 GABAA receptor in complex with pregnanolone (based on [[5o8f]])' scene='89/896619/Cv/3'>
These neurosteroids have excitatory effects on neurotransmission. They act as potent negative allosteric modulators of the [[GABAA receptor]], weak positive allosteric modulators of the NMDA receptor, and/or agonists of the σ1 receptor, and mostly have antidepressant, anxiogenic, cognitive and memory-enhancing, convulsant, neuroprotective, and neurogenic effects. Major examples include the pregnanes pregnenolone sulfate (PS), epipregnanolone, and isopregnanolone (sepranolone), the androstanes dehydroepiandrosterone (DHEA; prasterone), and dehydroepiandrosterone sulfate (DHEA-S; prasterone sulfate), and the cholestane 24(S)-hydroxycholesterol (NMDA receptor-selective; very potent).
These neurosteroids have excitatory effects on neurotransmission. They act as potent negative allosteric modulators of the [[GABAA receptor]], weak positive allosteric modulators of the NMDA receptor, and/or agonists of the σ1 receptor, and mostly have antidepressant, anxiogenic, cognitive and memory-enhancing, convulsant, neuroprotective, and neurogenic effects. Major examples include the pregnanes pregnenolone sulfate (PS), epipregnanolone, and isopregnanolone (sepranolone), the androstanes dehydroepiandrosterone (DHEA; prasterone), and dehydroepiandrosterone sulfate (DHEA-S; prasterone sulfate), and the cholestane 24(S)-hydroxycholesterol (NMDA receptor-selective; very potent).
*<scene name='89/896619/Cv/5'>Pregnenolone alone</scene>.
*<scene name='89/896619/Cv/5'>Pregnenolone alone</scene>.

Current revision

Structure of a chimaeric beta3-alpha5 GABAA receptor in complex with pregnanolone (based on 5o8f)

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References

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Alexander Berchansky, Michal Harel

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