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Neurosteroids
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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>. | ||
| - | *<scene name='89/896619/Cv/4'>Pregnanolone binds beta3-alpha5 GABAA receptor</scene>. | + | *<scene name='89/896619/Cv/4'>Pregnanolone binds beta3-alpha5 GABAA receptor</scene> ([[5o8f]]). |
| + | *<scene name='89/896619/Cv/6'>Pregnanolone binding site is situated between 2 monomers</scene>. | ||
Neurosteroids such as DHEA and allopregnanolone. | Neurosteroids such as DHEA and allopregnanolone. | ||
Revision as of 11:35, 16 November 2021
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