Neurosteroids
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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/ | + | <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'> |
Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with ligand-gated ion channels and other cell surface receptors. | Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with ligand-gated ion channels and other cell surface receptors. | ||
| - | + | '''[[Inhibitory neurosteroids]]''' | |
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| + | These neurosteroids exert inhibitory actions on neurotransmission. They act as positive allosteric modulators of the [[GABAA receptor]] (especially δ subunit-containing isoforms), and possess, in no particular order, antidepressant, anxiolytic, stress-reducing, rewarding, prosocial, antiaggressive, prosexual, sedative, pro-sleep, cognitive and memory-impairing, analgesic, anesthetic, anticonvulsant, neuroprotective, and neurogenic effects. | ||
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| + | Major examples include <scene name='89/896619/Cv/7'>tetrahydrodeoxycorticosterone</scene> (THDOC; from [[5osb]]), the androstane 3α-androstanediol, the cholestane cholesterol and the pregnanes pregnanolone (eltanolone), allopregnanolone (3α,5α-THP). | ||
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| + | '''[[Excitatory 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). | ||
| + | *<scene name='89/896619/Cv/5'>Pregnenolone alone</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>. | ||
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| + | '''Mixed''' | ||
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| + | Cholesterol: cholest-5-en-3β-ol – NMDA receptor positive allosteric modulator, possible GABAA receptor positive allosteric modulator, many other actions. | ||
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| + | Epipregnanolone sulfate: 5β-pregnan-3β-ol-20-one 3β-sulfate – GABAA and NMDA receptor negative allosteric modulator, Transient receptor potential cation channel subfamily M member 3 (TRPM3) agonist. | ||
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| + | '''[[Pheromones]]''' | ||
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| + | Pheromones are neurosteroids that influence brain activity, notably hypothalamic function, via activation of vomeronasal receptor cells. | ||
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| + | They include the androstanes androstadienol, androstadienone, androstenol ([[1xnx]]), and androstenone and the estrane estratetraenol. | ||
</StructureSection> | </StructureSection> | ||
| + | SEE ALSO: | ||
| + | *[[Steroids]] | ||
| + | *[[Lipid signaling]] | ||
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== References == | == References == | ||
<references/> | <references/> | ||
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SEE ALSO:
