Allopregnanolone

Common card · No. 267692

Allopregnanolone (3α‑hydroxy‑5α‑pregnan‑20‑one) is an endogenous neuroactive steroid and potent positive allosteric modulator of the GABA𝐴 receptor. It is synthesized both peripherally from progesterone and locally within the brain, where it contributes to tonic inhibition, stress regulation, arousal, and mood. Fluctuations in allopregnanolone levels are associated with pregnancy, the postpartum period, chronic stress, anxiety disorders, major depressive disorder, and several neurological conditions. Allopregnanolone has significant clinical relevance as the prototype for neurosteroid‑based therapeutics. Its intravenous formulation, brexanolone, was approved in the United States in 2019 for postpartum depression and withdrawn in 2025. The orally active analog zuranolone was approved in 2023 for postpartum depression in the United States, United Kingdom, European Union, and Canada, and for major depressive disorder in Japan. Neurosteroid modulation of GABA𝐴 receptors is an active area...

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