Inhibitory neurosteroids

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.

Major examples include (THDOC; from 5osb), the androstane 3α-androstanediol, the cholestane cholesterol and the pregnanes pregnanolone (eltanolone), allopregnanolone (3α,5α-THP).


Mouse GLIC-GABAA receptor complex with corticosterone derivative, acetate and Cl- ion (PDB code 5osb)

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ReferencesReferences

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Alexander Berchansky, Michal Harel